BR112013006269A2 - Nanocápsulas polimericamente revestidas, processo para a preparação de nanocápsulas polimericamente revestidas, composição cosmética, farmacêutica e/ou alimentícia e uso da composição cosmética, farmacêutica e/ou alimentícia - Google Patents
Nanocápsulas polimericamente revestidas, processo para a preparação de nanocápsulas polimericamente revestidas, composição cosmética, farmacêutica e/ou alimentícia e uso da composição cosmética, farmacêutica e/ou alimentícia Download PDFInfo
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Abstract
nanocápsulas contendo miroemulsões sistema de entrega baseado em nanocápsulas poliméricas que contêm microemulsões e seu uso na preparação de composições farmacêuticas, cosméticas e/ou alimentícias.
Description
NANOCÁPSULAS POLIMERICAMENTE REVESTIDAS, PROCESSO PARA A PREPARAÇÃO DE NANOCÁPSULAS POLIMERICAMENTE REVESTIDAS, COMPOSIÇÃO COSMÉTICA, FARMACÊUTICA E/OU ALIMENTÍCIA E USO DA COMPOSIÇÃO COSMÉTICA, FARMACÊUTICA E/OU ALIMENTÍCIA
CAMPO DA INVENÇÃO
Essa invenção refere-se a um novo sistema de entrega para ingredientes ativos farmacêuticos, cosméticos e/ou alimentícios baseados em nanocápsulas poliméricas que contêm microemulsões de água em óleo (a/o) e que compreendem pelo menos um ingrediente hidrofilicamente ativo dissolvido na fase aquosa.
ANTECEDENTES DA INVENÇÃO
As nanoparticulas lipidicas sólidas (SLN) constituem uma alternativa a outros sistemas de particulado para a entrega de ingredientes ativos, como emulsões, lipossomos, micelas, microparticulas e/ou nanoparticulas poliméricas. As SLN são geradas substituindo-se o lipidio liquido nas emulsões por um lipidio sólido, que significa que as SLN são sólidas à temperatura ambiente bem como à temperatura corpórea.
O uso de SLN como sistemas de entrega permite o uso de lipideos fisiologicamente aceitáveis, a possibilidade de evitar o uso de solventes orgânicos em sua preparação, e uma ampla faixa de rotas de administração, que inclui através da pele, oralmente ou de modo intravenoso. Além de mostrar biodisponibilidade satisfatória, suas principais vantagens são:
1. Proteção do ingrediente ativo contra degradação química. A matriz lipidica de SLN pode proteger ingredientes ativos lábeis contra hidrólise e/ou oxidação, como tocoferol, retinol e coenzima Q10 [Gohla, S. et al. J. Microencapsul. 18: 149 a 158 (2001 ); Schaf er-Korting, M. et al. Adv. Drug Del. Rev. 59: 427 a 443 (2007)].
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2. Baseado na composição das partículas lipídicas, as mesmas oferecem controle da velocidade de liberação de ingrediente ativo e, portanto, a possibilidade de alcançar perfis de liberação prolongada [Mehnert, W. et al. Eur. J. Pharm. Biopharm. 45: 149 a 155 (1998)].
3. Controle de desidratação da pele devido a um efeito oclusivo [Muller, R.H. et al. J. Cosm. Sei. 52: 313 a 323 (2001 )].
4. De acordo com seus componentes, as mesmas podem atuar como filtros de radiação ultravioleta [Muller, R.H. et al. Int. J. Cosm. Sei. 23: 233 a 243 (2001 )].
Uma nova geração de nanoparticulas lipídicas sólidas são os carreadores lipidicos nanoestruturados (NLC). Esses sistemas têm as mesmas vantagens que os SLN, e também minimizam ou evitam alguns problemas possíveis associados à SLN, como a baixa capacidade de carregamento e expulsão de ingrediente ativo durante armazenamento. Em contraste ao estado pelo menos parcialmente cristalino da fase lipídica em SLN, NLC mostram uma matriz lipídica sólida menos organizada. No caso de NLC, há compostos sólidos e líquidos na matriz, dessa forma, a maior desorganização leva à existência de um número maior de furos como o aumento subsequente na capacidade de encapsular ingredientes ativos. Para a preparação de NLC, moléculas estericamente muito diferentes de lipídeos são juntamente misturadas, misturas de lipídeos sólidos a lipídios ou óleos líquidos [Müller, R. H. et al. Adv. Drug Deliv. Rev. 54 (Supl. 1 ) : S131 a S155 (2002) ] .
As SLN e NLC têm tamanho de 50 a 1.000 nm e são mantidas estabilizadas em uma suspensão aquosa por tensoativos ou polímeros hidrofílicos. As NLC e SLN são veículos muito adequados para liberar ingredientes ativos através da pele. Uma penetração mais satisfatória de ingredientes ativos é alcançada quando os mesmos são
3/67 incorporados a SLN ou NLC que quando os mesmos são aplicados à pele sob a forma de uma solução ou uma emulsão.
As SLN têm um núcleo lipidico sólido que pode dissolver fármacos lipofílicos, que é o caso mais comum para uso. No entanto, a possibilidade de incorporação de peptídeos em partículas lipidicas poderia constituir uma proteção do ingrediente ativo contra a degradação proteolítica no aparelho gastrointestinal. No entanto, há poucas referências do uso de lipideos como materiais de matriz para formulações de peptídeos e proteínas, devido à natureza hidrofóbica da matriz lipídica, que torna isso mais apropriado para incorporação de ingredientes ativos lipofílicos que proteínas hidrofílicas. O uso de emulsões para incorporar ingredientes hidrofilicamente ativos como insulina em SLN é descrito [Gallarate, M. et al. J. Microencapsul. 26: 394 a 402 (2009) ] . Na publicação de Gallarate et al., o método de preparação de SLN implica o uso de solventes orgânicos, um fator que é problemático devido à possível retenção de seus resíduos. Gasco et al. incorpora pentapeptídeo de timopentina em nanopartículas lipidicas sólidas por dois métodos diferentes: a formação de um par de íons lipofílicos com hexadecilfosfato, ou pela formação de uma múltipla emulsão a/o/w que dissolve o peptídeo na fase aquosa interna [Gasco, M.R. et al. Int. J. Pharm. 132: 259 a 261 (1996)]; esse último método também é usado pelos mesmos autores para incorporar um polipeptídeo derivado de LHRH em SLN [Gasco, .R. et al. Int. J. Pharm. 105: Rl a R3 (1994) ] . Zhou et al. descreve um aumento na eficiência da encapsulação e a capacidade de carga na incorporação em SLN de diferentes proteínas usando-se PLGA (copolímero de ácido lático e glicólico) como um emulsificante [Zhou, W. et al. Colloids and Surfaces, B: Biointerfaces, 67: 199 a 204 (2008)].
A encapsulação de compostos hidrofílicos em SLN ou
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NLC apresenta outro problema, como seria a difusão do ingrediente ativo no sistema na direção de um meio onde seria mais solúvel, isto é, na direção do sistema aquoso no qual as nanoparticulas lipidicas estão em suspensão.
Embora as SLN e os NLC permitam que a estabilidade química dos ingredientes ativos incorporados seja aperfeiçoada, essa estabilização não é completa. De maneira surpreendente, os autores da presente invenção verificaram maior estabilização contra degradação de ingredientes ativos cosméticos e/ou farmacêuticos incorporados a SLN ou NLC quando as SLN ou NLC são polimericamente revestidos [pedido de patente espanhol ES P2010-30431].
Os procedimentos de preparação dos SLN e NLC, bem como o sistema de entrega descrito pelos autores no pedido de patente espanhol ES P2010-30431, implicam na exposição do ingrediente ativo a ser encapsulado às temperaturas dos pontos de fusão dos lipideos na matriz, que podem ser muito elevadas: acima de 50°C, e, na maioria dos casos, é usual aquecer as misturas a cerca de 80 a 90°C. No caso de ingredientes ativos termolábeis, como muitos compostos biológicos e outros de origem sintética como peptideos sintéticos, isso impede o uso de sistemas de entrega à base de lipideos sólidos. Os compostos hidrofilicos podem ser incorporados ao sistema de entrega de lipideo sob a forma de uma microemulsão estável, que, bem como a estabilização do ingrediente ativo, promove sua biodisponibilidade.
Uma microemulsão é definida como um sistema de água, óleo e um anfifilico que é uma solução opticamente isotrópica e termodinamicamente estável. As microemulsões são formadas espontaneamente. No entanto, as emulsões ordinárias exigem energia para sua formação e são termodinamicamente instáveis [Eastoe, J. Microemulsions, em Colloid Science: principles, methods and applications, Capitulo 5. Ed. T.
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Cosgrove, John Wiley & Sons, Ltd (2005)].
A presente invenção propõe um sistema de entrega baseado em nanocápsulas poliméricas contendo microemulsões de ingredientes hidrofilicamente ativos, que resolve as dificuldades apresentadas pelos sistemas descritos na técnica anterior. A substituição de lipideos sólidos por lipidios líquidos dentro das nanocápsulas evita a exposição dos ingredientes ativos termolábeis às altas temperaturas de fusão de muitos dentre os lipideos usados na preparação de SLN e NLC.
sistema de entrega da presente invenção permite a nanoencapsulação de ingredientes hidrofilicamente ativos termolábeis que evitam sua degradação durante o procedimento de preparação. Ademais, o sistema de entrega da presente invenção permite notável estabilização dos ingredientes ativos incorporados, evita a difusão de ingredientes hidrofilicamente ativos nas suspensões aquosas das nanocápsulas, e tem uma notável capacidade de penetração epidérmica.
DESCRIÇÃO DA INVENÇÃO
A presente invenção fornece uma solução para os problemas mencionados acima. Em um primeiro aspecto, essa invenção se refere a um novo sistema de entrega de nanocápsulas polimericamente revestidas que contêm microemulsões de água em óleos ou lipidios líquidos (a/o) e que compreendem pelo menos um ingrediente hidrofilicamente ativo dissolvido na fase aquosa interna.
As nanocápsulas da presente invenção compreendem uma matriz de lipidios ou óleos líquidos e um revestimento polimérico. Uma emulsão de água em óleo (a/o) de pelo menos um ingrediente hidrofilicamente ativo é incorporada à matriz lipidica. 0 revestimento das nanocápsulas constitui sua parte externa e fornece um revestimento completo e continuo da
6/67 matriz interna. Os termos óleo e lipidio liquido são usados indistintamente nessa invenção.
As nanocápsulas da presente invenção contêm ingredientes hidrofilicamente ativos incorporados a sua parte interna. Os ingredientes hidrofilicamente ativos incorporados às nanocápsulas da presente invenção podem ser, sem restrição, ingredientes ativos e/ou adjuvantes cosméticos, farmacêuticos e/ou alimentícios, dentre outros.
revestimento polimérico das nanocápsulas da presente invenção constitui a barreira externa das nanocápsulas; permite a encapsulação de seus componentes e também fornece proteção para os ingredientes ativos. Isso aumenta sua estabilidade contra a degradação química através da interação com outros componentes possíveis da composição, através da hidrólise e/ou da oxidação devido à presença de oxigênio e/ou luz. Ademais, no caso de ingredientes hidrofilicamente ativos como peptideos, isso evita a perda do ingrediente ativo por difusão na direção da fase aquosa externa, como acontece, com frequência, nas dispersões aquosas de SLN ou NLC. Uma maior penetração percutânea dos ingredientes ativos incorporados às nanocápsulas da invenção em relação às microemulsões, lipossomos, SLN e NLC também é alcançada.
Os procedimentos de preparação das nanocápsulas da presente invenção compreendem dois estágios: a) preparação da emulsão de água em óleo (a/o) de uma solução aquosa do ingrediente hidrofilicamente ativo em óleos ou lipidios líquidos, e b) encapsulação da microemulsão por meio de um revestimento polimérico.
Para a preparação das microcápsulas dos ingredientes hidrofilicamente ativos, a mistura de lipidios ou óleos líquidos, os ingredientes ativos, tensoativos, cotensoativos e/ou outros excipientes é microemulsifiçada com
7/67 água através da agitação. Subsequentemente, a microemulsão é polimericamente revestida.
Os métodos de homogeneização como homogeneização à pressão alta permitem que partículas menores sejam obtidas e usam uma quantidade menor de tensoativos.
Em uma modalidade particular, o tamanho das gotas da microemulsão interna se situa na faixa entre 0,1 e 80 nm, de preferência, entre 1 e 50 nm, e, com mais preferência, entre 10 e 20 nm.
Em outra modalidade particular, no processo de preparação das nanocápsulas da presente invenção, o revestimento polimérico pode ser produzindo seguindo os procedimentos usuais na técnica anterior: processos físicoquimicos (coacervação simples, coacervação complexa, coacervação simples ou complexa com mudança de pH durante reticulação, evaporação do solvente) e procedimentos químicos (policondensação interfacial). De preferência, o processo usado para a preparação das nanocápsulas da presente invenção é a coacervação.
Quando a encapsulação é executada por coacervação, a microemulsão que contém o ingrediente hidrofilicamente ativo dissolvido em sua fase aquosa é dispersa em uma dispersão ou solução aquosa externa que contém pelo menos um polímero do revestimento e pode conter opcionalmente outros ingredientes ativos, emulsificantes, polímeros e/ou outros excipientes. O processo pode ser executado em apenas um estágio se uma solução do agente de coacervação (coacervação simples) ou de outro polímero (coacervação complexa) for vertida sob agitação na mistura a/o/w anterior.
Em outra modalidade particular, na formação do revestimento polimérico das nanocápsulas da presente invenção, é usado um agente de reticulação. O agente de reticulação é selecionado, por exemplo e não restrito a, a
8/67 partir do grupo formado por aldeidos, glutaraldeido, formaldeido, transglutaminases, derivados de metilenobisacrilamida, N-N-metilenobisacrilamida, N-N-(1,2diidroxietileno)bisacrilamida, derivados de dimetacrilato de etileno glicol, diacrilato de etileno glicol, diacrilato de dietileno glicol, diacrilato de tetraetileno glicol, metacrilato de dietileno glicol, dimetacrilato de dietileno glicol, dimetacrilato de trietileno glicol, tripolifosfato sódico, ésteres e/ou imidoésteres de N-hidroxisuccinamida.
Em outra modalidade particular, a coacervação complexa pode ser executada aumentando-se o pH visto que o coacervato foi formado e antes da execução da reticulação. Isto é, o pH no qual a cápsula é reticulada é superior ao pH da coacervação, o que permite que cápsulas menores sejam obtidas [pedido de patente espanhol ES P2010-30432] .
As nanocápsulas da presente invenção podem ser coletadas pelas técnicas usuais, como filtração, centrifugação, secagem por aspersão e/ou liofilização.
Em outra modalidade particular, o tamanho das nanocápsulas da presente invenção oscila entre 10 e 5.000 nm, de preferência, entre 20 e 2.000 nm, e, com mais preferência, entre 50 a 1.000 nm.
percentual de incorporação do ingrediente ativo às nanocápsulas da presente invenção é quantitativo.
Em outra modalidade particular, o lipidio líquido das nanocápsulas da presente invenção tem um ponto de fusão abaixo de 4°C, e pode ser liquido ou semiliquido. O lipidio líquido é selecionado, sem restrição, a partir do grupo formado por óleos vegetais, como óleo de feijão-soja, óleo de girassol, óleo de milho, óleo de oliva, óleo de palma, óleo de semente de algodão, óleo de colza, óleo de amendoim, óleo de coco, óleo de rícino, óleo de linho, óleo de borragem, óleo de prímula da noite; óleos marinhos, como óleos de peixe
9/67 e óleos de alga; óleos derivados de petróleo, como óleo mineral, parafina liquida e vaselina; álcoois graxos de cadeia curta; álcoois graxos ramificados alifáticos de cadeia média; ésteres de ácidos graxos com álcoois de cadeia curta, como miristato isopropilico, palmitato isopropilico e estereato isopropilico e adipato isobutilico; triglicerideos de cadeia média (MCT) como triglicerideos cápricos e caprilicos (INCI: triglicerideos cápricos/caprilicos) e outros óleos na série Miglyol®; octanoatos C12-C16; éteres de álcool graxo, como éter de dioctila, e/ou misturas dos mesmos. Certos ingredientes ativos lipofilicos podem atuar também como matrizes lipidicas liquidas à temperatura ambiente, por exemplo e não restrito a, beta-caroteno, vitamina E e retinol, e/ou misturas dos mesmos.
Em outra modalidade particular, o tensoativo é selecionado do grupo formado por tensoativos não iônicos, tensoativos anfotéricos, tensoativos aniônicos, tensoativos catiônicos e/ou misturas dos mesmos. O tensoativo não iônico e/ou o tensoativo anfotérico é selecionado, sem restrição, a partir do grupo formado por lecitinas, alquil glicosideos com um grupo alquila que tem de 6 a 24 átomos de carbono, alquilmaltosideos com um grupo alquila que tem de 6 a 24 átomos de carbono, alquilfenóis etoxilados com um grupo alquila que tem de 6 a 24 átomos de carbono e de 5 a 30 unidades de óxido de etileno, alquilfenol polioxietileno éteres com um grupo alquila que tem de 6 a 24 átomos de carbono, álcoois graxos saturados e insaturados com um grupo alquila que tem de 8 a 24 átomos de carbono, poloxâmeros, polissorbatos, ésteres de ácido graxo com açúcares, ésteres de sorbitano, ésteres de ácido graxo de polietileno glicol, óleo de rícino, éteres de álcool graxo e polioxietileno, alcanolamidas de ácido graxo, óxidos de amina, betaínas de alquila com um grupo alquila que tem de 6 a 24 átomos de
10/67 carbono, betaínas de acil amido, alquilsulfobetaínas com um grupo alquila que tem de 6 a 24 átomos de carbono, derivados de glicina, digitonina, carbamato de inulin laurila e/ou misturas dos mesmos. Com mais preferência, o tensoativo não iônico e/ou tensoativo anfotérico é selecionado do grupo formado por octil glicosídeo, decil glicosídeo, lauril glicosídeo, octil frutosídeo, dodecil maltosídeo, decil maltosídeo, nonoxinol-9, polietileno glicol p-(l,l ,3,3tetrametilbutyl)fenil éter, álcool palmitílico, álcool oleílico, poloxâmero 188, poloxâmero 407, polissorbato 20, polissorbato 60, polissorbato 80, dioleato de metil glicose, monostearato de sorbitano ou Span 60, monolaurato de sorbitano ou Span 20, monopalmitato de sorbitano ou Span 20, olivato de sorbitano, estearato de polietileno glicol 40, estearato de polietileno glicol 50, estearato de polietileno glicol 100, éter de polioxietileno estearilico, éter de polioxietileno laurilico, cocamida monoetanolamina, cocamida dietanolamina, cocamida trietanolamina, lauramida dietanolamina, lauramida monoetanolamina, óxido de cocamidopropilamina, decil betaína, dodecil betaína, tetradecil betaína, cocoil betaína, cocamidopropil betaína, cocamidopropil hidroxissultaína, N-2-cocoil amidoetil hidroxietilglicinato e N-2-cocoil amidoetil hidroxietil carboxi glicinato e/ou misturas dos mesmos. O tensoativo aniônico é selecionado, sem restrição, a partir do grupo formado por sulfonatos como alquilbenzeno sulfonatos, alquil naftalenos sulfonatos, sulfonatos de álcool graxo etoxilado, sulfonatos alifáticos, hidroxi alcano sulfonatos, éteres sulfonato de alquil glicerila, sulfonato de perfluorooctano; alquil sulfossuccinatos, alquil sulfoacetatos; alquil sulfatos como sulfato de sódio e amônio laurilico, alquil sulfatos etoxilados; sulfatos de éster graxo; sulfatos de álcool graxo etoxilado; sulfatos de alquil éter; acil
11/67 isocianatos; pentafluorooctanoatos; carboxilatos; alquilfenóis etoxilados; sais de etanol amônio; dietanolamônio, metilamônio, dimetilamônio, trimetilamônio; alquil tauratos, acil ou ácidos graxos; alquil ou acil sarcosinatos; fosfatos como fosfato ésteres, alquil fosfatos, éter de polióxietileno laurilico fosfato; glutamatos; estearatos; ácidos biliares e seus sais, como ácido glicólico e glicolato de sódio, ácido taurocólico e taurocolato de sódio, taurodesoxicolato e/ou misturas dos mesmos. O tensoativo catiônico é selecionado, sem restrição, a partir do grupo formado por sais de amônio quaternário, como brometo de cetil trimetil amônio, cloreto de lauril trimetil amônio, cloreto de benzil dimetil hexadecil amônio, cloreto de distearil dimetil amônio, cloreto de dilauril dimetil amônio, cloreto de dimiristil dimetil amônio, cloreto de cetilpiridínio, cloreto benzalcônico, cloreto de benzetônio, cloreto de metil benzetônio e/ou misturas dos mesmos. Em outra modalidade particular, o cotensoativo é selecionado, sem restrição, a partir do grupo formado por álcoois e glicóis peso molecular baixo, como propanol, isopropanol, butanol e hexanol; ácidos graxos de cadeia longa, como ácido octanoico e ácido butirico; monoésteres de ácido fosfórico; álcool benzilico; sais de ácido biliar como colato de sódio, glicolato de sódio, taurocolato de sódio, taurodesoxicolato de sódio e/ou misturas dos mesmos.
Em outra modalidade particular, o antifloculante é selecionado, sem restrição, a partir do grupo formado por citrato de sódio, pirofosfato de sódio, sorbato de sódio, tensoativos anfotéricos, tensoativos catiônicos e/ou misturas dos mesmos.
Em outra modalidade particular, o viscosificante é selecionado, sem restrição, a partir do grupo formado por éteres e ésteres de celulose, como metil celulose,
12/67 hidroxietil celulose, hidroxipropil celulose e carboximetil celulose de sódio; derivados de polivinila, como álcool polivinilico, polivinilpirrolidona e acetato de polivinila; alginatos; poliacrilatos, xantanas; pectinas e/ou misturas dos mesmos.
Em outra modalidade particular, o polímero do revestimento polimérico das nanocápsulas da presente invenção é selecionado, sem restrição, a partir do grupo formado por proteínas, polissacarideos, poliésteres, poliacrilatos, policianoacrilatos, copolimeros e/ou misturas dos mesmos. De preferência, o polímero do revestimento das nanocápsulas é selecionado do grupo formado por gelatina, albumina, proteína de soja, proteína de ervilha, proteína de fava, proteína de batata, proteína de trigo, proteína de soro de leite, βlactoglobulina, caseinatos, amido de trigo, amido de milho, zeína, alginatos, carragenanas, pectinas, arabinogalactanos, goma arábica, goma xantana, goma de algaroba, goma tragacanto, galactomananos, goma guar, goma de semente de algaroba, guitosano, ágar, poli(L-lisina), dextrano sulfato de sódio, carboximetil galactomanano, carboximetil celulose, metil celulose, etil celulose, hidroxipropil metil celulose (HPMC), nitrato de celulose, butirato de acetato de celulose, ftalato acetato de celulose, ftalato de hidroxipropil metil de celulose, acetato succinato de hidroxipropil metil de celulose, ftalato de polivinil acetato, poli(ecaprolactona), poli(p-dioxanona), poli(5-valerolactona), poli(p-hidroxibutirato), poli(β-hidroxibutirato) e copolimeros de β-hidroxivalerato, poli(p-hidroxipropionato), copolimeros de ácido metilacrílico (Eudragit® L e S), copolimeros de dimetilaminoetil metacrilato (Eudragit® E) , copolimeros de trimetilamônio etil metacrilato (Eudragit® RL e RS), polímeros e copolimeros de ácido lático e glicólico, polímeros e copolimeros de ácido lático e glicólico e
13/67 polietileno glicol e misturas dos mesmos.
Dependendo das propriedades do polímero usado para o revestimento polimérico das nanocápsulas da presente invenção, é possível aumentar sua especificidade. Um polímero que fornece o revestimento polimérico com uma carga positiva permite que a ligação entre as nanocápsulas da presente invenção e o cabelo ou materiais têxteis seja mais forte. Opcionalmente, o polímero do revestimento das nanocápsulas da presente invenção pode ser um polímero catiônico. O polímero catiônico pode ser um polímero natural ou sintético, por exemplo e não restrito a, derivados catiônicos de celulose, como hidroxietil celulose quaternizada, que pode ser adquirida sob o nome Polymer JR 400™ por Amerchol; amidos catiônicos; copolímeros de sal de acrilamida e amônio dialila; polímeros de vinilpirrolidona/vinilimidazol quaternizados como Luviquat™ (BASF); produtos de condensação de poliglicóis e aminas; polímeros e copolímeros de poliquartênio; polímeros denominados Merquat de poliquartênio-6, poliquartênio-7, poliquartênio-16, poliquartênio-10; poliquartênio-4 copolímeros; dicocoiletilhidroxietilamônio, copolímeros de enxerto com um esqueleto de celulose e grupos amônio quaternário; polipeptideos de colágeno quaternizados como colágeno hidrolisado de laurdimônio hidroxipropil (Lamequat™ por Griinau); polipeptideos de trigo quaternizados; polietilenimina; polímeros de silicone catiônico como amidometicona ou quatêrnio-22 silicone; ácido adípico e copolímeros de dimetilamino hidroxipropil dietilenotriamina (Cartaretin™ por Sandoz); copolímeros de ácido acrílico com cloreto de dimetildialilamônio (Merquat™ 550 por Chemviron); derivados de quitina catiônica como quitosano e seus derivados; produtos de condensação de alquileno dihalógeno catiônico como dibromobutano com bisdialquilaminas; bis
14/67 dimetilamino-1 ,3-propano; derivados de goma guar catiônica como guar-hidroxipropiltrimônio, Jaguar™ CBS, Jaguar™ C-17, Jaguar™ C-16 por Celanese; polímeros de sal de amônio quaternário como Mirapol™A-15, Mirapol™AD-l, Mirapol™ AZ-1 por Miranol; polímeros de polissacarideo quaternizado de derivados naturais como azarose; proteínas catiônicas selecionadas de gelatina, goma arábica; polímeros catiônicos a partir do grupo formado por poliamidas, policianoacrilatos, poliláticos, poliglicólicos, polianilina, polipirrol, polivinilpirrolidona, polímeros e copolímeros de amino silicone, poliestireno, álcool polivinilico, poliestireno e copolímeros anidridos de ácido maleico, éter metil vinílico, resinas epóxi e estireno e copolímeros de metil metacrilato; dimetilamino metacrilato, poliacrilatos e polimetacrilatos catiônicos como Eudragit™ RL 30 D por Rohm; derivados de poliamina opcionaímente substituídos por derivados de polietileno glicol; ácidos de poliamino sob condições de pH em que os mesmos são catiônicos; polietilenoimina; derivados de polivinilpirrolidona quaternizada (PVP) e polímeros de uretano hidrofílico, bem como qualquer mistura dos grupos catiônicos mencionados acima.
Opcionaímente, o polímero do revestimento das nanocápsulas da presente invenção pode compreender um aditivo plastificante. O aditivo plastificante é selecionado, sem restrição, a partir do grupo formado por alquil ésteres de ácido cítrico como trietil citrato, tributil citrato, acetil tributil citrato e acetil trietil citrato, ftalatos como butil ftalato e dietil ftalato, glicerina, sorbitol, maltitol, propileno glicol, polietileno glicol, glicose, sacarose, lanolina, ácido palmítico, ácido oleico, ácido esteárico, sais de metal de ácido graxo como ácido esteárico ou ácido palmítico, estearato de sódio, estearato de potássio, monostearato de propileno glicol, monoglicerídeos
15/67 acetilados como monoacetil glicerina e glicerila triacetate ou triacetina, glicerila lecitina, glicerila monostearato, alquil sebacates come dibutil sebacate ou dietil sebacate, alquil fumarates, alquil succinatos, triglicerideos de cadeia média (MCT), óleo de rícino, óleos vegetais hidrogenados, ceras e/ou misturas dos mesmos.
Opcionalmente, outros aditivos técnicos do polímero podem ser adicionados que aperfeiçoam ou facilitam o processo de encapsulação como, por exemplo, fluidificantes, como talco, dióxido de silício coloidal, glicerina, polietileno glicol, glicerina monostearato e/ou sais de estearato metálico.
No contexto da presente invenção, o termo hidrofílico refere-se a substâncias que são solúveis em água, com uma solubilidade superior a 1 g por 100 ml de água a 20°C. Nessa invenção, os termos hidrofilicos e hidrossolúveis são usados indistintamente.
A natureza do ingrediente ativo e/ou adjuvante cosmético, farmacêutico e/ou alimentício hidrofílico pode ser sintética ou natural, ou vem de um procedimento biotecnológico ou de uma combinação de um procedimento sintético e um procedimento biotecnológico. De preferência, o ingrediente hidrofilicamente ativo das nanocápsulas da presente invenção é termolábil. No contexto da presente invenção, compreende-se que um ingrediente ativo termolábil seja aquele que apresenta uma degradação igual ou superior a 0,5% após ser submetido a uma temperatura de 80°C por duas horas.
Em uma modalidade particular, o ingrediente ativo cosmético, farmacêutico e/ou alimentício hidrofílico é selecionado, sem restrição, a partir do grupo formado por aminoácidos, peptídeos, proteínas, proteínas hidrolisadas, enzimas, hormônios, vitaminas, sais minerais, açúcares,
16/67 nucleotideos, ácidos nucleicos, moléculas e extratos de origem biológica e biotecnológica, vacinas, moléculas hidrofilicas sintéticas ou parcialmente sintéticas e/ou misturas dos mesmos.
Em uma modalidade particular, os aminoácidos, seus sais e/ou derivados, bem como as misturas comerciais que os contêm, são selecionados, por exemplo e não restrito a, a partir do grupo formado por serina, prolina, alanina, glutamato, arginina, glicina, metionina, citrulina, diacetato de metilglicina sódio (TRILON® M comercializado por BASE), derivados de aminoácidos que contêm cisteina, em particular, N-acetil cisteina, ergotioneina ou S-carboximetilcisteina, e/ou misturas dos mesmos. Em uma modalidade particular, os peptideos, ou as misturas comerciais que os contêm, são selecionados, por exemplo e não restrito a, a partir do grupo formado por peptideos de uso cosmético, como GHK [INCI: Tripeptideo-1], acetil-glutamil-metionil-alanil-isoleucina, acetil-arginil-fenilglicil-fenilglicina, Bodyfensine™ [INCI: Acetil Dipeptideo-3 Aminohexanoato], Relistase™ [INCI: Acetilarginiltriptofil Difenilglicina], acetil-arginilfenilglicil-valil-glicina, acetil-arginil-fenilglicil-valilfenilglicina, diaminopropionil-alanil-asparaginil-histidina, acetil-arginil-asparaginil-histidil-citrulina-amida, Aldenine® [INCI: Proteína de trigo hidrolisada, Proteína de soja hidrolisada, Tripeptideo-1], Decorinyl® [INCI: Tripeptideo-10 Citrulina], Serilesine® [INCI: hexapeptideo10], Peptideo AC29 [INCI: Acetil Tripeptideo-30 Citrulina], Vilastene™ [INCI: Lisina HCI, Lecitina, Tripeptideo-10 Citrulina], dGlyage™ [INCI: Lisina HCI, Lecitina,
Tripeptideo-9 Citrulina], Eyeseryl® [INCI: Acetil
Tetrapeptideo-5], Preventhelia® [INCI: Diaminopropionoil Tripeptideo-33], Argireline® [INCI: Acetil Hexapeptideo-8], SNAP-7 [INCI: Acetil Heptapeptideo-4], SNAP-8 [INCI: Acetil
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Octapeptídeo-3], Leuphasyl® [INCI: Pentapeptideo-18], Trylagen® [INCI: Extrato de Fermento de Pseudoalteromonas, Proteína de trigo hidrolisada, Proteína de soja hidrolisada, Tripeptideo-10 Citrulina, Tripeptideo-1], Inyline™ [INCI: Acetil Hexapeptideo-30], Melatime™ [INCI: Acetil Tripeptideo40], Thermostressine™ [INCI: Acetil Tetrapeptideo- 22] ou Liporeductyl® [INCI: Cafeína, Extrato de Raiz de Butcherbroom (Ruscus Aculeatus), TEA-Hidroiodo, Carnitina, Extrato de Era (Hedera Helix), Escina, Tripeptídeo-1] comercializado por Lipotec, Matrixyl® [INCI: Palmitoil Pentapeptideo-4], Matrixyl® 3000 [INCI: Palmitoil Tetrapeptideo-7, Palmitoil Oligopeptideo], Dermaxil [INCI: Palmitoil Oligopeptideo], Calmosensine™ [INCI: Acetil Dipeptideo-1], Biopeptideo CL™ [INCI: Gliceril Polimetacrilato, Propileno Glicol, Palmitoil Oligopeptideo] ou Biopeptideo EL™ [INCI: Palmitoil Oligopeptideo] comercializado por Sederma, pseudodipeptideos, IP 2000 [INCI: Dextrano, Trifluoroacetil Tripeptideo-2] comercializado por IEB e Atrium, Pepha®-Timp [INCI: Human Oligopeptideo-20], ECM-Protect® [INCI: água (Aqua), Dextrano, Tripeptideo-2] ou Melanostatine®-5 [INCI: Dextrano, Nonapeptideo-1] comercializado por Atrium Innovations, TimpPeptideo [INCI proposto: Acetil Hexapeptideo] , Bronzing S.F. [INCI proposto: Butiril Pentapeptídeo], BONT-L-Peptideo [INCI: Palmitoil Hexapeptideo-19] ou ECM Modulina [INCI proposto: Palmitoiltripeptideo] comercializado por Infinitec Activos, IP2000 [INCI: Dextrano, Trifluoroacetil tripeptideo2] comercializado por Institut Europeen de Biologie Cellulaire, Syn®-Coll [INCI: Palmitoil Tripeptideo-5] comercializado por Pentapharm, Neutrazen™ [INCI: Água, Butileno Glicol, Dextrano, Palmitoil Tripeptideo-8], ChroNOIine™ [INCI: Caprooil Tetrapeptideo-3] ou Thymulen-4 [INCI: Acetil Tetrapeptideo-2] comercializado por Atrium Innovations/Unipex Group, Meliprene® [INCI: Dextrano, Acetil
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Heptapeptídeo-1 ] ou Melitane® [INCI: Acetil Hexapeptideo-1] comercializado por Institut Europeen de Biologie Cellulaire/Unipex Group, Skinasensyl™ [INCI: Acetil Tetrapeptideo-15] comercializado por Laboratoires Serobiologiques/Cognis, Vialox® [INCI: Pentapeptideo-3], Syn®-Ake® [INCI: Dipeptideo Diaminobutiroil Benzilamida Diacetato], Syn®-Coll [INCI: Palmitoil Tripeptideo-5], Syniorage™ [INCI: Acetil Tetrapeptideo-11], Dermican™ [INCI: Acetil Tetrapeptideo-9] comercializado por Laboratoires Serobiologiques/Cognis, Kollaren® [INCI: Tripeptideo-1, Dextrano] comercializado por Institut Europeen de Biologie Cellulaire, Collaxyl® IS [INCI: Hexapeptideo-9], Laminixyl IS™ [INCI: Heptapeptideo], Quintescine™ IS [INCI: Dipeptideo4], UCPeptide™ V [INCI: Pentapeptideo] ou AT Peptide™ IS [INCI: Tripeptideo-3] comercializado por Vincience/ISP, glutationa, carnosina e/ou misturas dos mesmos; e peptideos de uso farmacêutico, como glucagon, leuprolida, goserelina, triptorelina, buserelina, nafarelina, deslorelina, histrelina, avorelina, abarelix, cetrorelix, ganirelix, degarelix, desmopressina, somatostatina e análogos de somatostatina como octreotideo, vapreotideo e lanreotideo, dentre outros.
Em outra modalidade particular, as proteínas, proteína hidrolisada, enzimas e hormônios, bem como as misturas comerciais que os contêm, são selecionadas, por exemplo e não restrito a, a partir do grupo formado por Elhibin® [INCI: Proteína de Soja (Feijão-soja) Glicina], Preregen® [INCI: Proteína de Soja (feijão-soja) Glicina, Óxido Reductases] ou Regu®-Age [INCI:Proteína de Farelo de Arroz Hidrolisada, Proteína de Soja (Feijão-soja) Glicina, Óxido Reductases] comercializada por Pentapharm/DSM, caderinas, integrinas, selectinas, receptores de ácido hialurônico, imunoglobulinas, fator de crescimento de
19/67 fibroblasto, fator de crescimento de tecido conectivo, fator de crescimento derivado de plaqueta, fator de crescimento endotelial vascular, fator de crescimento epidérmico, fator de crescimento similar à insulina, fator de crescimento de queratinócito, fator de crescimento de estimulo de colônia, fator beta de crescimento de transformação, fator alfa de necrose de tumor, interferonas, interleucinas, metaloproteinases de matriz, tirosina fosfatases de proteína receptora, proteínas vegetais hidrolisadas como proteína de trigo hidrolisada, proteína de soja hidrolisada ou proteína de soro de leite hidrolisada, Lipeptideo [INCI: Proteína vegetal hidrolisada] por Lipotec, Collalift® [INCI: Extrato de Malte Hidrolisado ] comercializado por Coletica/Engelhard, Colhibin [INCI: Proteína de Arroz Hidrolisada] comercializada por Pentapharm, Cytokínol® LS [INCI: Caseína Hidrolisada, Proteína de Levedura Hidrolisada, Lisina HCL] comercializada por Laboratoires Serobiologiques/Cognis, Liftline® [INCI: Proteína de Trigo Hidrolisada] ou Ridulisse C® [Proteína de Soja Hidrolisada] comercializada por Silab, catalase, superóxido dismutase, lactoperoxidase, glutationa peroxidase, lactoproteína, caseína, lactoperoxidase, lisozima, glicosidases, enzima quimotríptica de camada córnea ou SCCE, proteases como tripsina, quimotripsina, sutilaína, papaína ou bromelaína, enzimas de reparo de DNA como fotoliase ou T4 endonuclease V, lipase, hormônio de luteinização (LH), hormônio de estímulo de folículo (FSH), hormônio de crescimento, insulina e/ou misturas dos mesmos.
Em outra modalidade particular, as vitaminas são selecionadas, por exemplo e não restrito a, a partir do grupo formado por vitaminas hidrossolúveis, como vitamina C, vitamina BI , vitamina B2, vitamina B3, vitamina B5, vitamina B6, vitamina B7, vitamina B9, vitamina B12, carnitina e/ou misturas dos mesmos.
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Em outra modalidade particular, os extratos de origem biológica ou biotecnológica, que podem ser quimicamente modificados, bem como as misturas comerciais que os contêm, são selecionados, por exemplo e não restrito a, a partir do grupo formado por extratos vegetais, extratos marinhos, extratos celulares e extratos produzidos por microorganismos .
Os extratos vegetais são selecionados do grupo formado por extratos vegetais hidrossolúveis, por exemplo e não restrito a, extratos hidrossolúveis de camomila, hera, limão, ginseng, framboesa, amaranto torrado, Rehmannias radix, gardênia, cenoura, laranja, pêssego, abacaxi, genciana, flor de hibisco, folha de noz, abóbora, peônia, quinoa, boldo, trepadeiras ásperas, sálvia, romã, orégano, gengibre, manjerona, amora, uva, tomate, chá verde, chá preto, aloe vera (Aloe Barbadensis), Saphora japonica, mamão, abacaxi, abóbora, batata doce, Bupleurum Chinensis, Cecropia Obtusifolia, Gelosia Cristata, Centella Asiatica, Chenopodium Quinoa, Chrysanthellum Indicum, Citrus Aurantium Amara, Coffea Arabica, Coleus Forskohlii, Commiphora Myrrha, Crithmum Maritimum, Eugenia Caryophyllus, Ginkgo Biloba, Hedera Helix (hera), Hibiscus Sabdariffa, Ilex Paraguariensis, Laminana Digitata, Nelumbium Speciosum, Paullinia Cupana, Peumus Boldus, Phyllacantha Fibrosa, Prunella Vulgaris, Prunus Amygdalus Dulcis, Ruscus Aculeatus (extrato de Butcherbroom), Sambucus Nigra, Spirulina Platensis Algae, Uncaria Tomentosa, Verbena Officinalis, Opuntia ficus indica, Salix alba, Lupinus spp., Secale cereale, Tussilago farfara, Achillea millefolium, Aradirachta indica, Asmuna japonica, Autocarpus incisus, Bidens pilosa, Broussonetia papyrifera, Chlorella vulgaris, Cimicifuga racemosa, Emblica officinalis, Glycyrrhiza glabra, Glycyrrhiza uralensis, Ilex purpureia, Ligusticum lucidum,
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Ligusticum wallichii, Mitracarpus scaber, Morinda citrifolia, Morus alba, Morus bombycis, Naringi crenulata, Prunus domesticus, Pseudostellariae radix, Rumex crispus, Rumex occidentalis, Sapindus mukurossi, Saxifragia sarmentosa, Scutellaria Galericulate, Sedum sarmentosum Bunge, Stellaria medica, Triticum Vulgare, Uva ursi, Whitania somnifera, Aristoloquia clematis, Rosa moschata, Echinacea angustifolia, Symphytum officinale, Equisetum arvense, Hypericum perforatum, Mimosa tenuiflora, Persea gratíssima, Prunus africanum, Tormentilla erectea, Solanum tuberosum, Rosmarinus officinalis, Vaccinium angustifolium, Macrocystis pyrifera algae, Padina pavonica, Malpighia punicitolia, Cynara scolymus, Gossypium herbaceum, Panicum miliaceum, Morus nigra, Sesamum indicum, Glycine soja, Triticum vulgare, Glycine Max (soja), malte, linho, cravo vermelho, kakkon-to, tremoço branco, avelã, mais, ramos de árvore de faia, Trifolium pratense (cravo vermelho), Phormium tenax (linho da Nova Zelândia), Cinnamommum zeylanicum, Laminaria saccharina, Spiraea ulmaria, Raiz de Urtiga, Pygeum africanum, Avena Sativa, Arnica montana, Cinchona succirubra, Eugenia caryophyllata, Humulus lupulus, Hypericum perforatum, Mentha piperita, Rosmarinus officinalis, Thymus vulgaricus, extrato vegetal do gênero Silybum, extrato de sementes de legume, extratos de alga vermelha do gênero Porphyra, Phytovityl C® [INCI: Água, Extrato de Milho Verde (Zea Mays)] comercializado por Solabia, Micromerol™ [INCI: Extrato de Pyrus Malus] ou Extrato de Urze [INCI: Extrato de Calluna Vulgaris] comercializado por Coletica/Engelhard/BASF, Proteasyl® TP LS8657 [INCI: Extrato de Pisum Sativum] comercializado por Laboratoires Serobiologiques/Cognis, Radicaptol [INCI: Propileno Glicol, Água, Extrato de Flor de Passiflora Incarnata, Extrato de Folha de Ribes Nigrum (groselha negra), Extrato de Folha de Vitis Vinifera (uva)]
22/67 comercializado por Solabia ou ViaPure™ Boswellia [INCI: Extrato de Olivanum (Boswellia Serrata)] comercializado por Soliance, EquiStat [INCI Extrato de Fruto de Pyrus Malus, Extrato de Semente de Soja Glicina] comercializado por Coletica/Engelhard, Litchiderm™ [INCI: extrato de pericarpo de Litchi Chinensis] ou Arganyl™ [INCI: Extrato de Folha de Argania Spinosa] comercializado por Laboratories Serobiologiques/Cognis, Dakaline [INCI: Prunus amygdalus dulcis, extrato de casca de Anogeissus leiocarpus] comercializado por Soliance, Actimp 1.9.3® [INCI: Proteína de Lupina Hidrolisada] comercializada por Expanscience Laboratorios, Pronalen® Refirming HSC [INCI: Triticum vulgare, Silybum Marianum, Soja Glicina, Equisetum Arvense, Alchemilla Vulgaris, Medicago Sativa, Raphanus Sativus] ou Poliplant® Refirming [INCI: Coneflower, Asiatic Centella, Fucus, Fenugreek] comercializado por Provital, Lanablue® [INCI: Sorbitol, Extrato de Alga] comercializado por Atrium Innovations, Firmiderm® LS9120 [INCI: extrato de Folha de Terminalia Catappa, Extrato de Flor de Sambucus Negra, PVP, Ácido Tânico] comercializado por Laboratoires Serobiologiques/Cognis, dentre outros.
Os extratos celulares e os extratos produzidos por micro-organismos, ou misturas comerciais que os contêm, são selecionados do grupo formado por extratos hidrossolúveis celulares e extratos hidrossolúveis produzidos por microorganismos, por exemplo e não restrito a, Antarcticine® [INCI: Extrato de Fermento de Pseudoalteromonas] e Trylagen® [INCI: Extrato de Fermento de Pseudoalteromonas, Proteína de Trigo Hidrolisada, Proteína de Soja Hidrolisada, Tripeptídeo10 Citrulina, Tripeptídeo-1] comercializada por Lipotec, extrato de levedura, extrato de Saccharomyces cerivisiae e o produto da fermentação de leite com Lactobacillus Bulgaricus, dentre outros.
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A quantidade de ingrediente hidrofilicamente ativo contida no sistema de entrega da presente invenção se situa na faixa entre 0, 00001 e 50% em peso, de preferência, entre 0,0001 e 40% em peso, e, com mais preferência, entre 0,001 e 30% em peso.
Em outra modalidade particular, as nanocápsulas da presente invenção compreendem outros ingredientes ativos e/ou adjuvantes cosméticos e/ou alimentícios de qualquer natureza, hidrófobos, hidrófilos e anfífilos, que podem ser encontrados dentro das nanocápsulas em solução ou em suspensão na matriz lipídica, ou na fase aquosa da microemulsão. Em particular, os ingredientes ativos e/ou adjuvantes cosméticos e/ou alimentícios são selecionados, por exemplo e não restrito a, a partir do grupo formado por tensoativos, umectantes ou substâncias que retêm umidade, hidratantes ou emolientes, agentes que estimulam a cicatrização, agentes de cicatrização coadjuvantes, agentes que estimulam reepitelização, agentes de reepitelização coadjuvantes, agentes que sintetizam macromoléculas dérmicas ou epidérmicas, agentes de firmeza e/ou redensificação e/ou restruturação, fatores de crescimento de citocina, agentes que atuam na circulação capilar e/ou microcirculação, agentes antiglicação, sequestrantes de radical livre e/ou agentes de poluição antiatmosférica, sequestrantes de espécies de carbonila ativa, agentes de inibição de 5a redutase, agentes de inibição de lisil e/ou prolil redutase, agentes de estímulo de síntese de defensina, agentes bactericidas e/ou agentes bacteriostáticos e/ou agentes antimicrobianos e/ou agentes germicidas e/ou agentes fungicidas e/ou agentes fungistáticos e/ou agentes de inibição de germe, agentes antivirals, agentes antiparasitários, agentes anti-histamínicos, agentes de inibição de NO sintase, agentes de descamação ou agentes querotolíticos e/ou agentes esfoliantes, agentes
24/67 comedolíticos, agentes antipsoriase, agentes anticaspas, agentes anti-inflamatórios e/ou analgésicos, agentes anestésicos, agentes antirrugas e/ou antienvelhecimento, desodorantes para mascaramento de odor corpóreo e/ou cosmético e/ou absorvente, agentes antitranspirantes, substâncias para perfumar e/ou óleos perfumados e/ou compostos aromáticos isolados, agentes antioxidação, agentes que inibem permeabilidade vascular, enzimas epidérmicas hidroliticas, agentes de branqueamento ou despigmentação de pele, agentes que inibem enzimas de degradação de suor, agentes que têm a capacidade de filtrar Raios UV, agentes que estimulam ou regulam diferenciação de queratinócito, agentes anticoceira, agentes que estimulam ou inibem a síntese de melanina, agentes pró-pigmentação, agentes de autobronzeamento, agente de estimulo de proliferação de melanócito, propelentes líquidos, vitaminas, aminoácidos, proteínas, biopolímeros, polímeros gelificantes, agentes de relaxamento de pele, agentes que têm a capacidade de reduzir ou tratar bolsas sobre os olhos, agentes para o tratamento e/ou cuidado de pele sensível, agentes adstringentes, agentes que regulam produção de sebo, agentes antiestrias, agentes lipolíticos ou agentes que estimulam lipólise, agentes venotônicos, agentes anticelulite, agentes calmantes, agentes que atuam no metabolismo celular, agentes para aperfeiçoar a junção dérmica-epidérmica, agentes que induzem crescimento de cabelo ou retardantes de perda de cabelo, agentes que inibem ou retardam o crescimento de pelos, agentes de estimulo de síntese de proteína por choque térmico, relaxantes musculares, agentes de inibição de contração muscular, agentes que inibem agrupamento de receptor de acetilcolina, agentes colinérgicos, agentes inibidores de elastase, agentes inibidores de metaloproteinase da matriz, agentes quelantes, extratos vegetais, óleos essenciais, extratos marinhos, sais
25/67 minerais, extratos celulares, agentes emulsificantes, agentes que estimulam a síntese de lipídeos e componentes da camada córnea (ceramidas, ácidos graxos, etc.), agentes obtidos a partir de um processo de biofermentação e/ou misturas dos mesmos. A natureza desses ingredientes ativos e/ou adjuvantes cosméticos e/ou alimentícios pode ser sintética ou natural, como extratos vegetais, ou oriundos de um processo biotecnológico ou de uma combinação de um processo sintético e um processo biotecnológico. Exemplos adicionais podem ser encontrados no CTFA International Cosmetic Ingredient Dictionary & Handbook, 12^ Edição (2008). No contexto da presente invenção, compreende-se que um processo biotecnológico seja qualquer processo que produz o ingrediente ativo, ou parte do mesmo, em um organismo, ou em uma parte do mesmo.
Em uma modalidade particular, o umectante ou a substância que retém umidade, hidratante ou emoliente é selecionada, por exemplo e não restrito a, a partir do grupo formado por polióis e poliéteres como glicerina, etilhexilglicerina, caprilil glicol, pentileno glicol, butileno glicol, propileno glicol e seus derivados, trietileno glicol, polietileno glicol, Gliceret-26, Sorbet30; pantenol; ácido piroglutâmico e seus sais e derivados; aminoácidos, como serina, prolina, alanina, glutamato ou arginina; ectoína e seus derivados; N-(2hidroxietil)acetamida; ácido N-lauroil-pirrolidona carboxílico; N-lauroil-L-lisina; N-alfa-benzoil-L-arginina; ureia; creatina; ácidos α e β-hidróxi como ácido lático, ácido glicólico, ácido málico, ácido cítrico ou ácido salicíclico, e seus sais; acrilato de poliglicerila; açúcares e polissacarídeos, como glicose, isomerato de sacarídeo, sorbitol, pentaeritritol, inositol, xilitol, trealose e derivados dos mesmos, glucuronato de sódio, carragenatos
26/67 (Chondrus crispus) ou quitosano; glicosaminoglicanos como ácido hialurônico e derivados dos mesmos; aloe vera sob qualquer uma de suas formas; mel; colágeno solúvel; lecitina e fosfatidilcolina; ceramidas; colesterol e seus ésteres; tocoferol e seus ésteres, como acetato de tocoferila ou linoleato de tocoferila; álcoois de cadeia longa como álcool de cetearila, álcool de estearila, álcool de cetila, álcool oleílico, álcool de isocetila ou octadecan-2-ol; ésteres de álcool de cadeia longa como lactato de laurila, lactato de miristila ou benzoatos de alquila C12-C15; ácidos graxos como ácido esteárico, ácido isoesteárico ou ácido palmítico; ácidos graxos poli-insaturados (PUFAs); sorbitanos como distearato de sorbitano; glicerídeos como monoricinoleato de glicerila, monostearato de glicerila, citrato de glicerila estearato ou triglicerídeo de ácido caprílico e cáprico; ésteres de sacarose como palmitato de sacarose ou oleato de sacarose; ésteres de butileno glicol, como dicaprilato e dicaprato; ésteres de ácido graxo como isostearato de isopropila, palmitato de isobutila, estearato de isocetila, laurato de isopropila, laurato de hexila, oleato de decila, palmitato de cetila, sebacato de di-n-butila, miristato isopropílico, palmitato isopropílico, estereato isopropílico, estearato de butila, miristato de butila, linoleato de isopropila, palmitato de 2-etilhexila, cocoato de 2etilhexila, oleato de decila, miristato de miristila; esqualeno; óleo de marta; lanolina e seus derivados; álcoois de lanolina acetilada; derivados de silicone como ciclometicona, dimeticona ou dimetilpolissiloxano; Antarcticine® [INCI: Extrato de Fermento de Pseudoalteromonas] ou acetil-glutamil-metionil-alanilisoleucina, acetil-arginil-fenilglicil-fenilglicina ou acetil-arginil-6-aminohexanoil-alanina comercializada por Lipotec, petrolato; óleo mineral; ceras minerais e
27/67 sintéticas; cera de abelha (cera alba); parafina; ou ceras e óleos com origem vegetal como cera de candelila (Euphorbia cerifera) , cera de carnaúba (Copernicia cerifera), manteiga de karité (Butirospermum parkii), manteiga de cacau (Theobroma cacao), óleo de rícino (Ricinus communis), óleo de girassol (Helianthus annuus), óleo de oliva (Olea europaea), óleo de coco (Cocos nucifera), óleo de palma (Elaeis guineensis), óleo de germe de trigo (Triticum vulgare), óleo de amêndoa doce (Prunus amygdalus dulces), óleo de rosa de almiscar (Rosa moschata), óleo de feijão-soja (Glycine soja), óleo de semente de uva (Vitis vinifera) , óleo de calêndula (Calendula officinalis), óleo de jojoba (Simmonsis chinensis), óleo de manga (Mangifera indica), óleo de abacate (Persea gratíssima), e/ou misturas dos mesmos, dentre outros.
Da mesma forma, em outra modalidade particular, o agente que estimula cicatrização, o agente de cicatrização coadjuvante, o agente que estimula reepitelização e/ou o agente de reepitelização coadjuvante é selecionado, por exemplo e não restrito a, a partir do grupo formado por extratos de Aristoloquia clematis, Centella asiatica, Rosa moschata, Echinacea angustifolia, Symphytum officinale, Equisetum arvense, Hypericum perforatum, Mimosa tenuiflora, Persea gratisima, Prunus africanum, Tormentilla erectea, Aloe vera, Poliplant® Epithelizing [INCI: Calendula Officinalis, Hypericum Perforatum, Chamomilla Recutita, Rosmarinus Officinalis] comercializado por Provital, Cytokinol® LS 9028 [INCI: Caseina Hidrolisada, Proteína de Levedura Hidrolisada, Lisina HCI] comercializada por Laboratories Serobiologiques/Cognis ou Deliner® [INCI: Extrato de Núcleo de Zea May (Milho) ] comercializado por Coletica/Engelhard/BASF, alantoína, caderinas, integrinas, selectinas, receptores de ácido hialurônico, imunoglobulinas, fator de crescimento de fibroblasto, fator de crescimento de
28/67 tecido conectivo, fator de crescimento derivado de plaqueta, fator de crescimento endotelial vascular, fator de crescimento epidérmico, fator de crescimento similar à insulina, fator de crescimento de queratinócito, fatores de estimulo de colônia, fator beta de crescimento de transformação, fator alfa de necrose de tumor, interferonas, interleucinas, metaloproteinases de matriz, tirosina fosfatases de proteína receptora, Antarcticine® [INCI: Extrato de Fermento de Pseudoalteromonas], Decorinyl® [INCI: Tripeptídeo-10 Citrulina], Trylagen® [INCI: Extrato de Fermento de Pseudoalteromonas, Proteína de Trigo Hidrolisada, Proteína de Soja Hidrolisada, Tripeptídeo-10 Citrulina, Tripeptídeo-1], Bodyfensine™ [INCI: Acetil Dipeptídeo-3 Aminohexanoato], comercializado por Lipotec, dentre outros.
Em uma modalidade particular, o agente que estimula síntese macromolecular dérmica ou epidérmica é selecionado, por exemplo e não restrito a, a partir do grupo formado por agentes que estimulam síntese de colágeno, agentes que estimulam síntese de elastina, agentes que estimulam síntese de decorina, agentes que estimulam síntese de laminina, agentes que estimulam síntese de chaperona, agentes que estimulam síntese de sirtuína, agentes que estimulam síntese de ácido hialurônico, agentes que estimulam síntese de aquaporina, agentes que estimulam síntese de fibronectina, agentes que inibem degradação de colágeno, agentes que inibem
degradação de | elastina, agentes | que inibem | serina | proteases | |
como leucócito | elastase ou catepsina G, agentes que | estimulam | |||
proliferação | de | fibroblasto, | agentes | que | estimulam |
proliferação | de | adipócito, | agentes | que | estimulam |
diferenciação | de | adipócito, | agentes | que | estimulam |
angiogênese, | agentes que | estimulam | síntese de |
glicosaminoglicano, agentes de reparo de DNA e/ou agentes de proteção de DNA, por exemplo e não restrito a, extratos de
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Centella aslatlca, Saccharomyces cerevisiae, Solanum tuberosum, Rosmarinus officinalis, Vaccinium angustifolium, extrato das algas Macrocystls pyrifera, Radina pavonica, extrato das plantas soja, malte, linho, salva, cravo vermelho, kakkon-to, tremoço branco, extrato de avelã, extrato de milho, extrato de levedura, extrato de ramos de faia, extrato de sementes de leguminosas, extrato de hormônios vegetais como giberelinas, auxinas ou citocininas dentre outros, ou extrato de zooplâncton Salina, o produto da fermentação de leite com Lactobacillus Bulgaricus, asiaticosídeos e derivados dos mesmos, vitamina C e derivados dos mesmos, ácido cinâmico e derivados dos mesmos, Matrixyl® [INCI: Palmitoil, Pentapeptideo-3], Matrixyl® 3000 [INCI: Palmitoil Tetrapeptideo-3, Palmitoil Oligopeptídeo] ou Biopeptídeo CL™ [INCI: Gliceril Polimetacrilato, Propileno Glicol, Palmitoil Oligopeptídeo] comercializado por Sederma, Antarcticine® [INCI: Extrato de Fermento de Pseudalteromonas], Decorinyl® [INCI: Tripeptídeo-10 Citrulina], Serilesine® [INCI: Hexapeptídeo-10] , Lipeptídeo [INCI: Proteína Vegetal Hidrolisada], Aldenine® [INCI: Proteína de Trigo Hidrolisada, Proteína de Soja Hidrolisada, Tripeptídeo-1], Peptídeo AC29 [INCI: Acetil Tripeptídeo-30 Citrulina] comercializada por Lipotec, Drieline® PE [INCI:Betaglucano de Levedura] comercializado por Alban Muller, Phytovityl C® [INCI: Água, Extrato de Milho Verde (Zea Mays)] comercializado por Solabia, Collalift® [INCI: Extrato de Malte Hidrolisado] comercializado por Coletica/Engelhard, Phytocohesine® PSP [INCI proposto: BetaSitosterol Sulfato de Sódio] comercializado por Seporga, minerais como cálcio dentre outros, retinóides e derivados dos mesmos, isoflavonóides, carotenóides, em particular, licopeno, pseudodipeptídeos, retinóides e derivados dos mesmos como retinol ou palmitato de retinila, dentre outros,
30/67 ou heparinóides, dentre outros.
Em | uma | modalidade particular, | o agente que | inibe | |
degradação | de el | astina é selecionado, | por exemplo | e não | |
restrito | a, | a partir do grupo formado | por Elhibin® | [INCI: | |
Proteína | de | So j a | (Feijão-soja) Glicina | ] , Preregen® | [INCI: |
Proteína | de | So j a | (feijão-soja) Glicina, | Óxido Reductas | es ] ou |
Regu®-Age | [ | INCI:Proteína de Farelo de | Arroz Hidrol | isada, | |
Proteína | de | So j a | (Feijão-soja) Glicina | , Óxido Reductases] | |
comercializada | por Pentapharm/DSM, | Juvenesce | [INCI: |
Etoxidiglicol e Triglicerideo caprilico, Retinol, Ácido Ursólico, Fitonadiona, llomastat], Micromerol™ [INCI: Extrato de Pyrus Malus], Extrato de Urze [INCI: Extrato de Calluna Vulgaris], Extracellium® [INCI: Proteína de Batata Hidrolisada] ou Flavagrum™ PEG [INCI: PEG-6 Isostearato, Laurato de Hesperetina] comercializado por Coletica/Engelhard/BASF, Proteasyl® TP LS8657 [INCI: Extrato de Pisum Sativum] comercializado por Laboratoires Serobiologiques/Cognis, Relistase™ [INCI: Acetilarginiltriptofil Difenilglicina] comercializado por Lipotec, Sepilift DPHP [INCI: Dipalmitoil hidroxiprolina] comercializado por SEPPIC, Vitaderm® [INCI: Álcool, Água, Glicerina, Proteína de Arroz Hidrolisada, Extrato de Ilex Aquifolium, Ursolato de Sódio, Oleanolato de Sódio] comercializado por Rahn, Gatuline® Age Defense 2 [INCI: Extrato de Semente de Juglans Regia (Noz)] comercializado por Gattefosse, IP 2000 [INCI: Dextrano, Trifluoroacetil Tripeptídeo-2] comercializado por IEB e Atrium, Radicaptol [INCI: Propileno Glicol, Água, Extrato de Flor de Passiflora Incarnata, Extrato de Folha de Ribes Nigrum (groselha negra), Extrato de Folha de Vitis Vinifera (uva)] comercializado por Solabia ou ViaPure™ Boswellia [INCI: Extrato de Olivanum (Boswellia Serrata)] comercializado por Soliance, dentre outros.
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Em uma modalidade particular, o agente de inibição de metaloproteinase da matriz é selecionado, por exemplo e não restrito a, a partir do grupo formado por ácido ursólico, isoflavonas como genisteina, quercetina, carotenóides, licopeno, extrato de soja, extrato de amora, extrato de alecrim, extrato de Tri folium pratense (cravo vermelho), extrato de Phormium tenax (linho da Nova Zelândia), extrato de kakkon-to, extrato de salva, retinol e derivados dos mesmos, ácido retinoico e derivados dos mesmos, sapogeninas como diosgenina, hecogenina, esmilagenina, sarsapogenina, tigogenina, iamogenina e iucagenina dentre outros, Collalift® [INCI: Extrato de Malte Hidrolisado ], Juvenesce [INCI: Etoxidiglicol e Triglicerideo Caprilico, Retinol, Ácido Ursólico, Fitonadiona, llomastat] ou EquiStat [INCI Extrato de Fruto de Pyrus Malus, Extrato de Semente de Soja Glicina] comercializado por Coletica/Engelhard, Pepha®-Timp [INCI: Oligopeptideo-20 Humano], Regu-Age [INCI: Proteína de Farelo de Arroz Hidrolisada, Proteína de Glicina de Soja, Óxido Reductases] ou Colhibin [INCI: Proteína de Arroz Hidrolisada] comercializado por Pentapharm, Lipeptideo [INCI: Proteína vegetal hidrolisada], Peptídeo AC29 [INCI: Acetil Tripeptideo-30 Citrulina], acetil-arginil-asparaginilhistidil- citrulin-amida comercializado por Lipotec, Litchiderm™ [INCI: extrato de pericarpo de Litchi Chinensis] ou Arganyl™ [INCI: Extrato de Folha de Argania Spinosa] comercializado por Laboratories Serobiologiques/Cognis, MDI Complex® [INCI: glicosaminoglicanos] ou ECM-Protect® [INCI: água (Aqua), Dextrano, Tripeptideo-2] comercializado por Atrium Innovations, Dakaline [INCI: Prunus amygdalus dulcis, extrato de casca de Anogeissus leiocarpus] comercializado por Soliance, Homeostatina [INCI: Enteromorpha compressa, Caesalpinia Spinosa] comercializado por Provital, TimpPeptideo [INCI proposto: Acetil Hexapeptideo] ou ECM Modulina
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[INCI proposto: Palmitoiltripeptídeo] comercializado por Infinitec Activos, IP2000 [INCI: Dextrano, Trifluoroacetil tripeptideo-2] comercializado por Institut Europeen de Biologie Cellulaire, Actimp 1.9.3® [INCI: Proteína de Lupina Hidrolisada] comercializado por Expanscience Laboratories, Vitaderm® [INCI: Álcool, água (Agua), Glicerina, Proteína de Arroz Hidrolisada, Extrato de Ilex Aquifolium, Ursolato de Sódio, Oleanolato de Sódio] comercializado por Rahn, adapaleno, tetraciclinas e derivados dos mesmos como minociclina, rolitetraciclina, clortetraciclina, metaciclina, oxitetraciclina, doxiciclina, demeclociclina e seus sais, Batimastat [BB94; [4-(N-hidroxiamino)-2R-isobutil-3S(tiopheno-2-iltiometil)succinil]-L-fenilalanina-Nmetilamida], Marimastat [BB2516; [2S—[N4(R*) , 2R*, 3S]]-N4[2,2dimetil-1-[metilaminocarboni1]propil]-NI,2-dihidróxi-3-(2metilpropil)butanodiamida], dentre outros.
Em uma modalidade particular, o agente de firmeza e/ou redensificação e/ou restruturação é selecionado, por exemplo e não restrito a, a partir do grupo formado por extratos de Malpighia punicitolia, Cynara scolymus, Gossypium herbaceum, Aloe Barbadensis, Panícum miliaceum, Morus nigra, Sesamum indicum, Glycine soja, Triticum vulgare, Pronalen® Refirming HSC [INCI: Triticum vulgare, Silybum Marianum, Soja Glicina, Equisetum Arvense, Alchemilla Vulgaris, Medicago Sativa, Raphanus Sativus] ou Poliplant® Refirming [INCI: Coneflower, Asiatic Centetla, Fucus, Fenugreek] comercializado por Provital, Lanablue® [INCI: Sorbitol, Extrato de Alga] comercializado por Atrium Innovations, Pepha®-Nutrix [INCI: Fator de Nutrição Natural] comercializado por Pentapharm, ou extratos vegetais que contêm isoflavonas, Biopeptídeo EL™ [INCI: Palmitoil Oligopeptídeo], Biopeptídeo CL™ [INCI: Palmitoil
Oligopeptídeo], Vexel® [INCI: água (Agua), Propíleno Glicol,
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Lecitina, Cafeína, Palmitoil Carnitina], Matrixyl® [INCI: Palmitoil Pentapeptideo- 3], Matrixyl® 3000 [INCI: Palmitoil Tetrapeptideo-3, Palmitoil Oligopeptideo] ou Bio-Bustyl™ [INCI: Gliceril Polimetacrilato, Fermento de Proteína de soja de Rahnella, água (Aqua), Propileno Glicol, Glicerina, PEG-8, Palmitoil Oligopeptideo] comercializado por Sederma, Dermosaccharides® HC [INCI: Glicerina, água (Aqua), Glicosaminoglicanos, Glicogênio], Aglycal® [INCI: Manitol, Ciclodextrina, Glicogênio, Extrato de Folha de Aratostaphylos Uva Ursi], Cytokinol® LS [INCI: Caseina Hidrolisada, Proteína de Levedura Hidrolisada, Lisina HCI] ou Firmiderm® LS9120 [INCI: extrato de Folha de Terminalia Catappa, Extrato de Flor de Sambucus Negra, PVP, Ácido Tânico] comercializado por Laboratoires Serobiologiques/Cognis, Liftline® [INCI: Proteína de Trigo Hidrolisada], Raffermine® [INCI: Farinha de Soja Hidrolisada] ou Ridulisse C® [Proteína de Soja Hidrolisada] comercializado por Silab, Serilesine® [INCI: hexapeptídeo-10], Decorinyl™ [INCI: Tripeptídeo-10 Citrulina], Trylagen® [INCI: Extrato de Fermento de Pseudoalteromonas, Proteína de Trigo Hidrolisada, Proteína de Soja Hidrolisada, Tripeptídeo-10 Citrulina, Tripeptídeo-1], comercializado por Lipotec, Ursolisome® [INCI: Lecitina, Ácido Ursólico, Atelocolágeno, Goma xantana, Condroitina Sulfato de Sódio] ou Collalift® [INCI: Extrato de Malte Hidrolisado] comercializado por Coletica/Engelhard, Syn®-Coll [INCI: Palmitoil Tripeptídeo-5] comercializado por Pentapharm, Hydriame® [INCI: água (Agua), Glicosaminoglicanos, Goma de Esclerócio] comercializado por Atrium Innovations ou IP2000 [INCI: Dextrano, Trifluoroacetil tripeptídeo-2] comercializado por Institut Europeen de Biologie Cellulaire, dentre outros.
Em uma modalidade particular, o agente antiglicação é selecionado, por exemplo e não restrito a, a partir do
34/67 grupo formado por extratos de Vaccinium angustifolium, ergotioneina e derivados dos mesmos, lisina, Aldenine® [INCI: Proteína de Trigo Hidrolisada, Proteína de Soja Hidrolisada, Tripeptideo-1], Vilastene™ [INCI: Lisina HCI, Lecitina, Tripeptídeo-10 Citrulina], dGlyage™ [INCI: Lisina HCI, Lecitina, Tripeptídeo-9 Citrulina] ou Eyeseryl® [INCI: Acetil Tetrapeptídeo-5] comercializado por Lipotec, hidroxistilbenos e derivados dos mesmos, resveratrol ou 3,3' ,5,5'tetrahidroxistilbeno, dentre outros.
Em uma modalidade particular, o sequestrante de radical livre e/ou agente de antipoluição atmosférica, e/ou o sequestrante de espécies de carbonila reativa é selecionado, por exemplo e não restrito a, a partir do grupo formado por extrato de chá, extrato de folha de oliva, extrato de Rosmarinus officinalis ou extrato de Eichhornia crassipes, benzopirenos, vitamina C e derivados dos mesmos, vitamina E e derivados dos mesmos, em particular, acetato de tocoferila, ascorbil glicosideo, fenóis e polifenóis, em particular, taninas, ácido tânico e ácido elágico, galocatecol, antocianinas, ácido clorogênico, estilbenos, indóis, derivados de aminoácido contendo cisteina, em particular, Nacetilcisteína, ergotioneina, S-carboximetilcisteina, agentes quelantes, em particular, EDTA ou etilenodiaminas, carotenóides, bioflavonóides, ubiquinona, idebenona, catalase, superóxido dismutase, lactoperoxidase, glutationa peroxidase, glutationa, benzilideno cânfora, pidolatos, lignanos, melatonina, orizanol, carnosina e derivados dos mesmos, GHK [INCI: Tripeptideo-1] e seus sais e/ou derivados, Aldenine® [INCI: Proteína de Trigo Hidrolisada, proteína de soja hidrolisada, tripeptídeo-1], Preventhelia® [INCI: Diaminopropionoil Tripeptídeo-33], diaminopropionil-alanilasparaginil-histidina ou Lipochroman-6 [INCI: Dimetilmetoxi Cromanol] comercializado por Lipotec, dentre outros.
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Em uma modalidade particular, o agente de inibição de 5a redutase é selecionado, por exemplo e não restrito a, a partir do grupo formado por extrato de Cinnamommum zeylanicum, Laminaria saccharins, Spiraea ulmaria, Raiz de Urtiga, Pygeum africanum, Avena Sativa, Serenoa repens, extratos das plantas Arnica montana, Cinchona succirubra, Eugenia caryophyllata, Humulus lupulus, Hypericum perforatum, Mentha piperita, Rosmarinus officinalis, Salvia officinalis, Salvia officinalis, extrato de plantas do gênero Silybum, extrato de plantas que contêm sapogeninas e, em particular, extrato de plantas do gênero Dioscorea, fitosterdis, retinóides e, em particular, retinol, enxofre e derivados dos mesmos, sais de zinco e, em particular, lactato, gluconato, pidolato, carboxilato, salicilato ou cisteato de zinco, cloreto de selênio, vitamina B6, piridoxina, capriloil glicina, sarcosina, finasterida, dutasterida, izonsterida, turosterida e seus sais, dentre outros.
Da mesma forma, em outra modalidade particular, o agente de inibição de lisila e/ou prolila hidroxilase é selecionado, por exemplo e não restrito a, a partir do grupo formado por 2,4-diamiriopirimidina 3-óxido ou 2,4-diamino-6piperidinopirimidina 3-óxido, dentre outros.
Em outra modalidade particular, o agente de estimulo de síntese de defensina é selecionado, por exemplo e não restrito a, a partir do grupo formado por extratos de ou Aloe Vera, Amaranto torrado, Rehmannlas radix, arnica, gardênia, cenoura, laranja, pêssego, abacaxi, menta, genciana, flor de hibisco, folha de nogueira, calabaça, peônia, guinoa, boldo, trepadeira áspera, girassol, sabugueiro, erva marinha, milho hidrolisado, soja hidrolisada, arroz hidrolisado, valina hidrolisada e seus isômeros e derivados, cálcio e seus sais, σ-MSH e fragmentos contidos na sequência de aminoácidos de σ-MSH, vitamina A e
36/67 seus derivados e precursores, vitamina D3 e seus derivados, ácido jasmônico, ácido fumárico, ácido málico, ácido cítrico, ácido ascórbico, ácido lático, ácido acético, ácido adípico, ácido tartárico, ácido cinâmico, ácido glutâmico, ácido succínico, inulina, alquil glicosídeos, ácido poli-Dglutâmico, glicina, L-metionina, L-alanina, L-citrulina, lactoproteína, caseína, lactoperoxidase, lisozima, polifenol, alquil glicosídeos, extrato de Lactobacillus, extratos de fusobactéria ou bactérias não fotossintéticas e não frutíferas e Bodyfensine™ [INCI: Acetil Dipeptídeo-3 Aminohexanoato] comercializado por Lipotec, dentre outros.
Em outra modalidade particular, o agente bactericida e/ou bacteriostático e/ou agente antimicrobiano e/ou germicida e/ou agente fungicida e/ou agente fungistático e/ou agente de inibição de germe é selecionado, por exemplo e não restrito a, a partir do grupo formado por macrolídeos, piranosídeos, bloqueadores de canal de cálcio, por exemplo e não restrito a, cinarizina e diltiazem; hormônios, por exemplo e não restrito a, estrila, análogos do mesmo ou tiroxina e/ou seus sais, caprilil glicol, imidazolidinil ureia, metil 4-hidroxibenzoato [INCI: metilparabeno] , etil 4hidroxibenzoato [INCI: etilparabeno], propil 4hidroxibenzoato [INCI: propilparabeno] , butil 4hidroxibenzoato [INCI: butil parabeno], isobutil 4hidroxibenzoato [INCI: isobutilparabeno], 1,3bis(hidroximetil)-5,5-dimetilimidazolidina-2,4-diona [INCI: DMDM Hidantoína], benzil 4-hidroxibenzoato [INCI: benzilparabeno], álcool benzilico, ácido desidroacético, ácido benzoico, ácido sórbico, ácido salicíclico, ácido fórmico, ácido propiônico, 2-bromo-2-nitropropano-l,3-diol,
3-p-clorofenoxi-1,2-propanodiol [INCI: clorfenesina], álcool diclorobenzilico, iodopropinil butilcarbamato, cloreto benzalcônico, fungicidas de absorção de odor como ricinoleato
37/67 de zinco, ciclodextrinas, cloreto de benzetônico, clorhexidina, etanol, propanol, 1,3-butanodiol, 1,2-propileno glicol, ácido undecilênico, ácido desidroacético, Nmetilmorfolina acetonitrila (ΜΜΆ) , isopropanol, metanol, 1,2hexanediol, 1,2-octanodiol, pentileno glicol, laurato de glicerina, caprilato de glicerina, caprato de glicerina, peróxido de benzoíla, gluconato de clorhexidina, triclosan e derivados dos mesmos, fenoxietanol, terpinen-4-ol, oterpineol, resorcinol, estiemicina, eritromicina, neomicina, clindamicina e seus ésteres, tetraciclinas, metronidazol, ácido azelaico, tolnaftato, nistatina, clotrimazol, cetoconazol, derivados de zinco como piritionato de zinco ou tritionato, óxido de zinco e undecilenato de zinco, piroctona olamina, isotiazolinonas, selênio enxofre, benzil hemiformal, ácido bórico, borato de sódio, 6,6-dibromo-4,4-dicloro-2,2'metilenodifenol [INCI: bromoclorofeno], 5-bromo-5-nitro-l,3dioxano, tosilcloramida sódica [INCI: cloramina T], cloroacetamida, p-cloro-m-cresol, 2-benzil-4-clorofenol [INCI: clorofeno], dimetil oxazolidina, dodecil dimetil-2brometo de fenoxietil amônio [INCI: brometo de domifeno] , 7etil biciclooxazolidina, hexetidina, glutaraldeído, N-(4clorofenil)-N-[4-cloro-3-(trifluorometil)fenil]-ureia [INCI: cloflucarban], 2-hidróxi-4-isopropil-2,4,6-cicloheptatrieno-
1-ona [INCI: Hinokitiol], isopropilmetilfenol, sais de mercúrio, sais de alumínio, nisina, fenoxiisopropanol, ofenilfenol, iodeto de 3-heptil-2-[(3-heptil-4-metil-3Htiazol-2-ilideno)metil]-4-metiltiazol [INCI: Quatêrnio-73], cloreto de prata, iodeto de sódio, timol, ácido undecilênico, ácido dietilenotriaminapentacético, ácido etilenodiaminatetracético e etilenodiaminatetraacetatos, lactoperoxidase, glicose oxidase, lactoferrina, alquilaril sulfonatos, fenóis halogenados, acetato de fenol mercúrio e/ou misturas dos mesmos, benzamidinas, isotiazolinas,
38/67 derivados de ftalimida, derivados de piridina, guanidinas, quinolinas, 1,2-dibromo-2,4-dicianobutano, carbamato de iodo-
2-propilbutila, iodo, iodos domados, compostos de peroxo, 4cloro-3,5-dimetilfenol, 2,2'-metileno-bis(6-bromo-4clorofenol), 3-metil-4-(1-metiletil)fenol, 3-(4-clorofenoxi)1,2-propanodiol, 3,4,4'-triclorocarbanilida (TTC) , essência de tiamina, eugenol, farnesol, monolaurato de glicerina, monocaprinato de diglicerina, amida de ácido saliciclico de N-alquila como amida de ácido saliciclico de n-octila ou amida de ácido saliciclico de n-decila, derivados de xileno halogenado e cresol, como p-cloro-meta-cresol ou p-clorometa-xileno, extratos de Allium sativum, Calendula officinalis, Chamomilla recutita, Echinacea Purpura, Hyssopus Officinalis, Melaleuca alternifolia ou óleo de pé de chá, essência de cravo, mentol e essência de menta, dentre outros.
Da mesma forma, em outra modalidade particular, o agente de inibição de NO sintase é selecionado, por exemplo e não restrito a, a partir do grupo formado por extratos das plantas Vítís vínífera, Olea europaea ou Gíngko bíloba, dentre outros.
Em uma modalidade particular, o agente de descamação e/ou agente queratolitico e/ou agente de esfoliação é selecionado, por exemplo e não restrito a, a partir do grupo formado por hidroxi ácidos e derivados dos mesmos, α-hidroxiácidos, em particular, ácido saliciclico e derivados dos mesmos, ou ácido gentisico; β-hidroxiácidos e seus sais, como ácido glicólico, glicolato de amônio, ácido lático, ácido 2-hidroxioctanoico, ácido α-hidroxicaprílico, ácido mandélico, ácido cítrico, ácido málico ou ácido tartárico; α e ácidos β-hidroxibutirico; polihidróxi ácidos como ácido gluconico, ácido glucurônico ou ácido sacárico; cetoácidos como ácido pirúvico, ácido glioxilico; ácido pirrolidinecarboxilico; ácido cisteico e derivados; ácidos
39/67 aldobiônicos; ácido azelaico e derivados dos mesmos como diglicinato de azeloila; ácido ascórbico e derivados dos mesmos como ácido 6-O-palmitoilascórbico, ascorbil glicosídeo, ácido dipalmitoilascórbico, sal de magnésio de ácido-2-fosfato ascórbico (MAP), sal de sódio de ácido-2fosfato ascórbico (NAP), ascorbil tetraisopalmitato (VCIP); ácido nicotínico, seus ésteres e nicotinamida (também denominado vitamina B3 ou vitamina PP) ; ácido nordiidroguaiarético; ureia; oligofucoses; ácido cinâmico; derivados de ácido jasmônico; hidroxi estilbenos como resveratrol; extrato de Saccarum officinarum; enzimas envolvidas na descamação ou degradação das corneodesmosomes, como glicosidases, enzima quimotríptica de camada córnea (SCCE) ou outras proteases como tripsina, quimotripsina, sutilaína, papaína ou bromelaína; agentes quelantes como ácido etilenodiaminatetracético (EDTA) e seus sais, compostos aminossulfônicos como ácido 4-(2-hidroxietil)piperazina-1etanossulfônico (HEPES) ou diacetato de metilglicina sódio (TRILON® M comercializado por BASE); derivados de ácido 2oxotiazolidina-4-carboxílico (procisteína); derivados de açúcares como O-octanoil-6-D-maltose e N-acetilglucosamina; extrato de pinhão (Castanea satíva) como aquele comercializado por SILAB sob o nome Recoverine® [INC1: água (Aqua), Extrato de Semente de Castanea sativa]; extrato de opuntia (Opuntia ficus-indica) como aquele comercializado por SILAB como Exfolactive® [INC1: Extrato de Flor de Opuntia Ficus Indica Hidrolisado]; ou Phytosphingosine SLC® [INCI: Saliciloil Fitosfingosina] comercializado por Degussa/Evonik, Peel-Moist [INCI: Glicerina, Papaína, Pantotenato de Cálcio, Goma xantana, Caprilil Glicol, Ureia, Lactato de Magnésio, Etilhexilglicerina, Lactato de Potássio, Serina, Alanina, Prolina, Cloreto de Magnésio, Citrato de Sódio]; extrato ou combinação de extratos de Saphora japonica, mamão, abacaxi,
40/67 abóbora ou batata doce, e/ou misturas dos mesmos.
Em outra modalidade particular, o agente antiinflamatório e/ou agente analgésico é selecionado, por exemplo e não restrito a, a partir do grupo formado por extrato de madecassosideo, extrato de echinacea, óleo de semente de amarante, óleo de sândalo, extrato de folha de pessegueiro, extrato de Aloe vera, Arnica montana, Artemisia vulgaris, Asarum maximum, Calendula officinalis, Capsicum, Centipeda cunninghamii, Chamomilla recutita, Crinum asiaticum, Hamamelis virginiana, Harpagophytum procumbens, Hypericum perforatum, Lilium candidum, Malva sylvestris, Melaleuca alternifolia, Origanum majorana, Origanum vulgare, Prunus laurocerasus, Rosmarinus officialis, Salix alba, Silybum marianum, Tanacetum parthenium, Thymus vulgaris, Uncaria guianensis ou Vaccinum myrtillus, furoato de mometasona, prednisolona, anti-inflamatórios não esteroidais incluindo inibidores de ciclooxigenase ou lipoxigenase, benzidamina, ácido acetilsalicíclico, ácido rosmarinico, ácido ursólico, derivados de glicirrizinato, α-bisabolol, azuleno e análogos, sericosideo, ruscogenina, escina, escolina, rutina e análogos, hidrocortisona, clobetasol, dexametasona, prednisona, paracetamol, amoxiprina, benorilato, salicilato de colina, faislamina, salicilato de metila, salicilato de megnésio, salsalato, diclofenac, aceclofenac, acemetacina, bromfenac, etodolac, indometacina, oxametacina, proglumetacina, sulindac, tolmetina, ibuprofeno, dexibuprofeno, carprofeno, fenbufeno, fenoprofeno, flurbiprofeno, cetoprofeno, dexcetoprofeno, cetorolac, loxoprofeno, naproxen, miroprofeno, oxaprozina, pranoprofeno, ácido tiaprofênico, suprofeno, ácido mefenâmico, meclofenamato, ácido meclofenâmico, ácido flufenâmico, ácido tolfenâmico, nabumetona, fenilbutazona, azapropazona, clofezona, cebuzona, metamizol, mofebutazona, oxifenbutazona,
41/67 fenazona, sulfinpirazona, piroxicam, lornoxicam, meloxicam, tenoxicam, celecoxib, etoricoxib, lumiracoxib, parecoxib, rofecoxib, valdecoxib, nimesulida, naproxcinod, fluproquazona ou licofelona, ácidos graxos de ômega-3 e ômega-6, morfina, codeina, oxicodona, hidrocodona, diamorfina, petidina, tramadol, bupenorfina, benzocaina, lidocaina, cloroprocaina, tetracaina, procaina, amitriptilina, carbamazepina, gabapentina, pregabalina, bisabolol, Neutrazen™ [INCI: Água, Butileno Glicol, Dextrano, Palmitoil Tripeptideo-8] comercializado por Atrium Innovations/Unipex Group, Meliprene® [INCI: Dextrano, Acetil Heptapeptideo-1] comercializado por Institut Europeen de Biologie Cellulaire/Unipex Group, Skinaserisyl™ [INCI: Acetil Tetrapeptideo-15] ou Anasensyl™ [INCI: Manitol, Amônio Glicirrizato, Cafeína, Extrato de Hippocastanum (Castanha da índia)] comercializado por Laboratoires Serobiologiques/Cognis, Calmosensine™ [INCI: Acetil Dipeptideo-1] comercializado por Sederma, coenzima Q10 ou éteres de alquilglicerinas.
Além disso, em outra modalidade particular, o agente de branqueamento ou despigmentação de pele é selecionado, por exemplo e não restrito a, a partir do grupo formado por extratos de Achillea millefolium, Aloe vera, Aradirachta indica, Asmuna japonica, Autocarpus incisus, Bidens pilosa, Broussonetia papyri fera, Chlorella vulgaris, Cimicifuga racemosa, Emblica officinalis, Glycyrrhiza glabra, Glycyrrhiza uralensis, Ilex purpureia, Ligusticum lucidum, Ligusticum wallichii, Ligusticum wallichii, Morinda citrifolia, Morus alba, Morus bombycis, Naringi crenulata, Prunus domesticus, Pseudostellariae radix, Rumex crispus, Rumex occidentalis, Sapindus mukurossi, Saxifragia sarmentosa, Scutellaria Galericulate, Sedum sarmentosum Bunge, Stellaria medica, Triticum Vulgare, Uva ursi ou
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Whitania somnifera, flavonoides, extrato de soja, extrato de limão, extrato de laranja, extrato de ginkgo, extrato de pepino, extrato de gerânio, extrato de gaiúba, extrato de alfarroba, extrato de canela, extrato de manjerona, extrato de alecrim, extrato de cravo da índio, extrato de alcaçuz solúvel ou extrato de folha de amora silvestre, Lipocroman-6 [INCI: Dimetilmetoxi Cromanol] ou Chromabright™ [INCI: Dimetilmetoxi Cromanil Palmitato] comercializado por Lipotec, Actiwhite™ LS9808 [INCI: Água, Glicerina, Dilaurato de Sacarose, Polisorbate 20, extrato de Pisum sativum (Ervilha)] ou Dermawhite® NF LS9410 [INCI: Manitol, Arginina HCI, Fenilalanina, EDTA Dissódico, Citrato de Sódio, Ácido Kójico, Ácido Cítrico, Extrato de Levedura] comercializado por Laboratoires Serobiologiques/Cognis, Lumiskin™ [INCI: Triglicerídeo Caprílico/Cáprico, Diacetil-Boldina], Melaclear™ [INCI: Glicerina, Água, Ditiaoctanodiol, ácido Glucônico, Sutilaínas, Beta-caroteno] , O.D.A.white™ [INCI: ácido octadecendioico] ou Etioline™ [INCI: Glicerina, Butileno Glicol, Extrato de folha de Arctostaphylos uva ursi, Extrato de Mitracarpus scaber] comercializado por Sederma, Sepiwhite™ MSH [INCI: Undecilenoil Fenilalanina] comercializado por Seppic, Achromaxyl [INCI: Água, Extrato de Brassica napus] comercializado por Vincience, Gigawhite™ [INCI: Água, Glicerina, Extrato de Malva sylvestris (Malva), Extrato de Folha de Mentha piperita, Extrato de Primula veris, Extrato de Alchemilla vulgaris, Extrato de Veronica officinalis, Extrato de Folha de Melissa officinalis, Extrato de Achillea millefolium], Melawhite® [INCI: Extrato de Leucócito, AHA] ou Melfade®-J [INCI: Água, Extrato de Folha de Arctostaphylos uva-ursi, Glicerina, Ascorbil Fosfato de Magnésio] comercializado por Pentapharm, Albatin® [INCI: Ácido Aminoetilfosfórico, Butileno Glicol, Agua] comercializado por Exsymol, Tyrostat™-! 1 [INCI: Água,
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Glicerina, Extrato de Rumex occidentalis] ou Melanostatine®-5 [INCI: Dextrano, Nonapeptídeo-1] comercializado por Atrium Innovations, arbutina e seus isômeros, ácido kójico e derivados dos mesmos, ácido ascórbico e derivados dos mesmos como ácido 6-O-palmitoilascórbico, ascorbil glicosídeo, ácido dipalmitoilascórbico, sal de magnésio de ácido-2-fosfato ascórbico (MAR), sal de sódio de ácido-2-fosfato ascórbico (NAP), ascorbil glicosídeo ou ascorbil tetraisopalmitato (VCIP); retinol e derivados dos mesmos incluindo tretinoína e isotretinoína, idebenona, ácido hidroxibenzoico e derivados dos mesmos, niacinamida, liquiritina, resorcinol e derivados dos mesmos, hidroquinona, a-tocoferol, β-tocoferol, ácido azelaico, diglicinato de azeloila, resveratrol, ácido linoleico, ácido α-lipoico, ácido diidrolipoico, ácidos ahidróxi, ácidos β-hidróxi, ácido elágico, ácido ferúlico, ácido cinâmico, ácido oleanólico, aloesina e seus derivados e/ou inibidores de serina protease, por exemplo e não restrito a, inibidores de triptase, tripsina ou PAR-2, dentre outros.
Em outra modalidade particular, o agente que estimula a síntese de melanina, o agente pró-pigmentação, o agente de autobronzeamento e/ou o agente de estímulo de proliferação de melanócito é selecionado, por exemplo e não restrito a, a partir do grupo formado por extratos de Citrus Aurantium Dulcis Fruit, Coleus forskohlii, Coleus Esquirolii, Coleus Scutellariodes, Coleus Xanthanthus, Ballota nigra, Ballota lanata, Ballota suavelens, Marrubium cylleneum, Cistus creticus, Amphiachyris amoena, Aster oharai, Otostegia fruticosa, Plectranthus barbatus, Halimium viscosum ou Larix laricema, diidroxiacetona e derivados dos mesmos, açúcares, por exemplo e não restrito a, eritrulose, melanina e derivados dos mesmos incluindo polímeros de melanina e derivados de melanina com um peso molecular baixo que são
44/67 solúveis em água, forscolina e derivados dos mesmos incluindo deacetilforscolina e isoforscolina, tirosina e derivados dos mesmos incluindo acetil tirosina, oleila tirosina , 3-amino tirosina e 3-nitrotirosina, sais de cobre como CuCl2, carotenóides, cantaxantinas, polímeros de ácido diidroxiindol carboxílico, ácido 3,4-diidroxibenzoico, ácido 3-amino-4hidroxibenzoico, aloína, emodina, alizarina, diidroxifenilalanina, ácido 4,5-diidroxinaftalenos-2sulfônico, 3-dimetilaminofenol ou ácido β-aminobenzoico, Melatime™ [INCI: Acetil Tripeptídeo-40 ] comercializado por Lipotec, Heliostatine IS™ [INCI: Extrato de Pisum Sativum] comercializado por Vincience/ISP, Vegetan [INCI: Diidroxiacetona] ou Vegetan Premium [INCI: Diidroxiacetona, Melanin] comercializado por Soliance, MelanoBronze [INCI: Extrato de Vitex Agnus Castus, Acetil Tirosina] comercializado por Mibelle Biochemistry, Melitane® [INCI: Acetil Hexapeptídeo-1] comercializado por Institut Europeen de Biologie Cellulaire/Unipex Innovations, Actibronze® [INCI: Proteína de Trigo Hidrolisada, Acetil Tirosina, Gluconato de Cobre] ou Instabronze® [INCI: Diidroxiacetona, Tirosina] comercializado por Alban Muller, Thalitan [INCI: Algina Hidrolisada, Sulfato de Magnésio, Sulfato de Manganês] comercializado por CODIF, Tyrosilane® [INCI: Metilsilanol Acetiltirosina] comercializado por Exsymol, Tyr-Excel™ [INCI: Oleoil Tirosina, Óleo de Semente de Luffa Cylindrica, Ácido Oleico] ou Tyr-OI [INCI: Oleoil Tirosina, Butileno glicol, Ácido Oleico] comercializado por Sederma/Croda, Bronzing S.F.
[INCI proposto: Butiril Pentapeptídeo] comercializado por Infinitec Activos ou Biotanning® [INCI: Extrato de Citrus Aurantium Dulcis Fruit Hidrolisado] comercializado por Silab, dentre outros.
Em uma modalidade particular, o agente antirruga e/ou antienvelhecimento é selecionado, por exemplo e não
45/67 restrito a, a partir do grupo formado por extratos de Vitis vinifera, Rosa canina, Curcuma longa, Iris pallida, Theobroma cacao, Ginkgo biloba, Leontopodium Alpinum ou Dunaliella salina, Matrixyl® [INCI: Palmitoil Pentapeptideo-4], Matrixil 3000® [INCI: Palmitoil Tetrapeptideo-7, Palmitoil Oligopeptídeo], Essenskin™ [INCI: hidroximetionina cálcica], Renovage [INCI: teprenona] ou Dermaxyl® [INCI: Palmitoil Oligopeptídeo] comercializado por Sederma, Vialox® [INCI: Pentapeptídeo-3], Syn®-Ake® [INCI: Dipeptídeo Diaminobutiroil Benzilamida Diacetato], Syn®-Coll [INCI: Palmitoil Tripeptídeo-5], Fitaluronato [INCI: Goma de Algorrobo (Ceratonia Siliqua)] ou Preregen® [INCI: Proteína de Soja (Feijão-soja) Glicina, Óxido Reductases] comercializado por Pentapharm/DSM, Myoxinol™ [INCI: Extrato de Hibiscus Esculentus Hidrolisado], Syniorage™[INCI: Acetil Tetrapeptídeo-11], Dermican™ [INCI: Acetil Tetrapeptídeo-9] ou DN-AGE™ LS [INCI: Extrato de folha de Cassia Alata] comercializado por Laboratoires Serobiologiques/Cognis, Algisum C® [INCI: Metilsilanol Manuronato] ou Hidroxiprolisilane CN® [INCI: Metilsilanol Hidroxiprolina Aspartato] comercializado por Exsymol, Argireline® [INCI: Acetil Hexapeptídeo-8], SNAP-7 [INCI: Acetil Heptapeptídeo4], SNAP-8 [INCI: Acetil Octapeptídeo-3], Leuphasyl® [INCI: Pentapeptídeo-18], Aldenine® [INCI: Proteína de Trigo Hidrolisada, proteína de soja hidrolisada, Tripeptídeo-1], Preventhelia® [INCI: Diaminopropionoil Tripeptídeo-33], Decorinyl™ [INCI: Tripeptídeo-10 Citrulina], Trylagen® [INCI: Extrato de Fermento de Pseudoalteromonas, Proteína de Trigo Hidrolisada, Proteína de Soja Hidrolisada, Tripeptídeo-10 Citrulina, Tripeptídeo-1], Eyeseryl® [INCI: Acetil Tetrapeptídeo-5] , Peptídeo AC29 [INCI: Acetil Tripeptídeo-30 Citrulina], Lipocroman-6 [INCI: Dimetilmetoxi Cromanol], Chromabright™ [INCI: Dimetilmetoxi Cromanil Palmitato],
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Antarcticine® [INCI: Extrato de Fermento de Pseudoalteromonas], Vilastene™ [INCI: Lisina HCI, Lecitina, Tripeptideo-10 Citrulina], dGlyage™ [INCI: Lisina HCI, Lecitina, Tripeptideo-9 Citrulina], Relistase™ [INCI: Acetilarginiltriptofil Difenilglicina] ou Inyline™ [INCI: Acetil Hexapeptideo-30] comercializado por Lipotec, Kollaren® [INCI: Tripeptideo-1, Dextrano] comercializado por Institut Europeen de Biologie Cellulaire, Collaxyl® IS [INCI: Hexapeptideo-9], Laminixyl IS™ [INCI: Heptapeptideo], Orsirtine™ GL [INCI: Extrato de Oryza Sativa (Arroz)], D'Orientine™ IS [INCI: Extrato de Semente de Phoenix Dactylifera (Tâmara)], Phytoquintescine™ [INCI: Extrato de Einkorn (Triticum Monococcum)] ou Quintescine™ IS [INCI: Dipeptideo-4] comercializado por Vincience/ISP, BONT-LPeptideo [INCI: Palmitoil Hexapeptideo-19] comercializado por Infinitec Activos, Deepaline™ PVB [INCI: Palmitoil Proteína de trigo hidrolisada] ou Sepilift® DPHP [INCI: Dipalmitoil Hidroxiprolina] comercializado por Seppic, Gatuline® Expression [INCI: Extrato de Acmella oleracea], Gatuline® InTense [INCI: Extrato de Flor de Spilanthes Acmella] ou Gatuline® Age Defense 2 [INCI: Extrato de Semente de Juglans Regia (Noz)] comercializado por Gattefosse, Thalassine™ [INCI: Extrato de Alga] comercializado por Biotechmarine, ChroNOIine™ [INCI: Caprooil Tetrapeptideo-3] ou Timulen-4 [INCI: Acetil Tetrapeptideo-2] comercializado por Atrium Innovations/Unipex Group, EquiStat [INCI: Extrato de Fruto de Pyrus Malus, Extrato de Semente de Soja Glicina] ou Juvenesce [INCI: Etoxidiglicol e Triglicerideo Caprilico, Retinol, Ácido Ursólico, Fitonadiona, llomastat] comercializado por Coletica, Ameliox [INCI: Carnosina, Tocoferol, Extrato de Silybum Marianum Fruit] ou PhytoCellTec Malus Domestica [INCI: Cultura Celular de Malus Domestica Fruit] comercializado por ibelle Biochemistry, Bioxilift [INCI:
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Extrato de Pimpinella Anisum] ou SMS Anti-Wrinkle® [INCI: Extrato de Semente de Annona Squamosa] comercializado por Silab, bloqueadores de canal de Ca2+, por exemplo e não restrito a, sais de alverina, manganês ou magnésio, certas aminas secundárias ou terciárias, retinol e derivados dos mesmos, resveratrol, idebenona, coenzima Q10 e derivados dos mesmos, ácido boswélico e derivados dos mesmos, GHK e derivados dos mesmos e/ou sais, carnosina e derivados dos mesmos, enzimas de reparo de DNA, por exemplo e não restrito a, fotoliase ou T4 endonuclease V, ou bloqueadores de canal de cloreto, dentre outros.
Em uma modalidade particular, o agente lipolítico ou agente que estimula lipólise, agente venotônico e/ou agente anticelulite é selecionado, por exemplo e não restrito a, a partir do grupo formado por extratos de Bupleurum Chinensis, Cecropia Obtusifolia, Celosia Cristata, Centella Asiatica, Chenopodium Quinoa, Chrysanthellum Indicum, Citrus Aurantium Amara, Coffea Arabica, Coleus Forskohlii, Commiphora Myrrha, Crithmum Maritimum, Eugenia Caryophyllus, Ginkgo Biloba, Hedera Helix (extrato de hera), Hibiscus Sabdariffa, Ilex Paraguariensis, Laminaria Digitata, Nelumbium Speciosum, Paullinia Cupana, Peumus Boldus, Phyllacantha Fibrosa, Prunella Vulgaris, Prunus Amygdalus Dulcis, Ruscus Aculeatus (extrato de Butcherbroom) , Sambucus Nigra, Spirulina Platensis Algae, Uncaria Tomentosa ou Verbena Officinalis, diidromiricetina, coenzima A, lipase, glaucina, esculina, visnadina, Regu®-Shape [INCI: Ácido Linoleico Isomerizado, Lecitina, Glicerina, Polissorbato 80] comercializado por Pentapharm/DSM, UCPeptide™V [INCI: Pentapeptídeo] ou AT Peptide™ IS [INCI: Tripeptideo-3] comercializado por Vincience/ISP, Liporeductyl® [INCI: Cafeína, Extrato de Raiz de Butcherbroom (Ruscus Aculeatus), TEA-Hidroiodo, Carnitina, Extrato de Hera (Hedera Helix),
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Escina, Tripeptideo-1] comercializado por Lipotec, Adiposlim [INCI: Laurato de Sorbitano, Lauroil Prolina] comercializado por SEPPIC, cafeína, carnitina, escina e/ou iodeto de trietanolamina, dentre outros.
Em uma modalidade particular, o agente de estímulo de síntese de proteína por choque térmico é selecionado, por exemplo e não restrito a, a partir do grupo formado por extratos de Opuntia fícus indica, Salix alba, Luplnus spp. , Secale cereale, extratos de alga vermelha do gênero Porphyra, extratos de crustáceos do gênero Artemia, óleo de semente de jojoba, extratos de semente de uva, extratos de chá verde, geranilgeranilacetona, celastrol, zinco e seus sais, 2ciclopenten-l-ona, inibidores de proteasome, por exemplo e não restrito a, bortezomib; prostaglandinas e derivados dos mesmos, hidroxilamina e derivados dos mesmos, por exemplo e não restrito a, bimoclomol; calcona e derivados dos mesmos, agentes hiperosmóticos, por exemplo e não restrito a, sorbitol e derivados dos mesmos, manitol e derivados dos mesmos ou glicerol e derivados dos mesmos, isosorbeto, ureia ou ácido salicíclico e derivados dos mesmos, dentre outros, Thermostressine™ [INCI: Acetil Tetrapeptídeo-22], ou misturas dos mesmos.
Em outra modalidade particular, o agente de indução de crescimento de cabelo, o agente que atua na circulação capilar e/ou microcirculação, ou o agente retardante de perda de cabelo é selecionado, por exemplo e não restrito a, a partir do grupo formado pelos extratos de Tussllago farfara ou Achillea millefolium, ésteres de ácido nicotínico como nicotinatos de alquila C3-C6 como nicotinato de metila ou hexila, nicotinato de benzila, ou nicotinato de tocoferila; biotina, agentes de inibição de 5a redutase, agentes antiinflamatórios, retinóides, por exemplo e não restrito a, ácido all-trans-retinoico ou tretinoína, isotretinoína,
49/67 retinol ou vitamina A, e derivados dos mesmos, como sal de zinco de acetato, palmitato, propionato, motretinida, etretinato e trans-retinoato; agentes antibactericidas, bloqueadores de canal de cálcio, por exemplo e não restrito a, cinarizina e diltiazem; hormônios, por exemplo e não restrito a, estriol, seus análogos ou tiroxina, seus análogos e/ou sais; agentes antiandrogênicos, por exemplo e não restrito a, oxendolona, espironolactona ou dietilstilbestrol; agentes antirradical, oligossacarideos esterifiçados, por exemplo e não restrito a, aqueles descritos nos documentos EP 0211610 e EP 0064012; derivados de ácidos hexossacárico, por exemplo e não restrito a, ácido glucosacárico ou aqueles descritos no documento EP 0375388; inibidores de glucosidase, por exemplo e não restrito a, D-glucaro-1,5-lactam ou aqueles descritos no documento EP 0334586; inibidores de glicosaminoglicanoase e proteoglicanase, por exemplo e não restrito a L-galactono-1,4-lactona ou aqueles descritos no documento EP 0277428; inibidores de tirosina quinase, por exemplo e não restrito a, 1-amido-l-ciano(3,4diidroxifenil)etileno ou aqueles descritos no documento EP 0403238, diazóxidos, por exemplo e não restrito a, 7(acetiltio)-4',5'-diidrospiro[androst-4-eno-17,2 ' - (3H)furan]-
3-ona, 1,1-dióxido de 3-metil-7-cloro[2H]-1,2,4benzotiadiazina ou espirooxazina; fosfolipídeos, por exemplo e não restrito a, lecitina; ácido salicíclico e derivados dos mesmos, hidroxicarboxílico ou ácidos ceto carboxílicos e ésteres dos mesmos, lactonas e seus sais; antralina, ácidos eicosa-5,8,11-trienoico e ésteres dos mesmos ou amidas dentre outros, minoxidila e derivados ou misturas dos mesmos.
Em outra modalidade particular, o agente retardante ou de inibição de crescimento de pelo é selecionado, por exemplo e não restrito a, a partir do grupo formado por activina ou agonistas de activina, flavonoides como
50/67 quercetina, curcumina, galangina, fisetina, miricetina, apigenina; propil gaiato, ácido nordiidroguaiaretico, ácido cafeico, inibidores de tirosina quinase como lavendustina, erbstatina, tirfostinas, benzoquinona-ansamicina herbimicina A, tiazolidinadionas, fenazocina, ácidos 2,3-diidro-2-tioxolH-indol-3-alcanoicos, derivados de fenotiazina como tioridazina; esfingosina e derivados dos mesmos, estaurosporina e derivados dos mesmos, ácido glicirretínico, brometo de lauril isoquinolínio, Decelerine™ [INCI: Brometo de Lauril Isoquinolínio, Extrato de Fermento de Pseudoalteromonas] comercializado por Lipotec ou inibidores de serina protease, tripsina e/ou misturas dos mesmos.
Em uma modalidade particular, o agente cosmético e/ou absorvente e/ou desodorante de mascaramento de odor corpóreo e/ou antitranspirante, substância de perfume e/ou óleo perfumado é selecionado, por exemplo e não restrito a, a partir do grupo formado pelo sal de zinco complexo de ácido ricinoleico, Styrax, derivados de ácido abiótico, essência de salva, essência de camomila, essência de cravo, essência de cidreira, essência de menta, essência de folha de canela, essência de flor de lima, essência de junípero, essência de vetiver, essência de olíbano, essência de gálbano, essência de labdânio, essência de lavanda, essência de hortelã, laranja bergamota, diidromircenol, lilial, liral, citronelol, essência de limão, essência de mandarina, essência de laranja, essência de lavanda, moscatel, essência de geranium bourbon, semente de anis, coentro, cominho, junípero, extratos de flor-de-lis, lilás, rosas, jasmim, flor de limeira; acetato de benzila, acetato de p-tertbutilciclohexila, acetato de linalila, acetato de feniletila, glicinato de etilmetilfenila, benzoato de linalila, formato de benzila, ciclohexil propionato de alila, propionato de estiralila, salicilato de benzila, etil éter de benzila,
51/67 alcanos lineares com 8 a 18 átomos de carbono, citral, ácido ricinoleico, citronelal, citronelil oxiacetaldeido, ciclamen aldeido, hidroxicitronelal, bourgeonal, iononas, metil cedril cetona, anetol, eugenol, isoeugenol, geraniol, linalool, terpineol, álcool feniletilico, a-hexilcinamaldeido, geraniol, benzilacetona, ciclamen aldeido, ambroxan, indol, hediona, sandelice, ciclovertal, /3-damascona, alii amil glicolato, diidromircenol, fenoxietil isobutirato, ciclohexil salicilato, ácido fenilacético, acetato de geranila, romilat, irotila, floramato, produtos adstringentes ativos como cloreto de alumínio, cloridrato de alumínio, dicloridrato de alumínio, sesquicloridrato de alumínio, hidroxialantoínato de alumínio, clorotartrato de alumínio, tricloridrato de alumínio e zircônio, tetracloridrato de alumínio e zircônio, pentacloridrato de alumínio e zircônio e/ou misturas dos mesmos.
Em uma modalidade particular, o antioxidante é selecionado, por exemplo e não restrito a, a partir do grupo formado por butilhidroxitolueno (BHT), butilhidroxianisol (BHA), tert-butilhidroquinona (TBHQ) , 2,6,-di-tert-butil-4metilfenol, ésteres de ácido gálico como propil gaiato, probucol, polifenóis, ácido ascórbico e seus sais, enzimas como catalase, superóxido dismutase e peroxidases; ácido cítrico, citratos, monoglicerídeo ésteres, metabissulfato de cálcio, ácido lático, ácido málico, ácido succínico, ácido tartárico, vitamina A ou β-caroteno, vitaminas E e C, tocoferóis como acetato de vitamina E, ésteres de ácido ascórbico como palmitato de ascorbila e acetato de ascorbila, zinco, cobre, manitol, glutationa reduzida, carotenóides como criptoxantina, astaxantina e licopeno; cisteína, ácido úrico, carnitina, taurina, tirosina, luteína, zeaxantina, N-acetilcisteína, carnosina, α-glutamilcisteína, quercetina, lactoferrina, ácido diidrolipoico, catequinas de chá,
52/67 palmitato de retinila e derivados dos mesmos, bissulfato, metabissulfeto e sulfeto de sódio, cromanos, cromenos e seus análogos, Lipocroman-6 [INCI: Dimetilmetoxi Cromanol], agentes quelantes de metais como EDTA, sorbitol, ácido fosfórico ou dGlyage™ [INCI: Lisina HCI, Lecitina, Tripeptideo-9 Citrulina]; extrato de Ginkgo Biloba, extratos vegetais como salva, pomegranate, alecrim, orégano, gengibre, manjerona, amora, uva, tomate, chá verde ou chá preto; extrato de oleoresina, extrato de plantas que contêm fenóis como vanilina, ácido elágico e resveratrol; butilhidroquinona terciária ou misturas dos mesmos, sais de metal com uma valência de 2 como selênio, cádmio, vanádio ou zinco; ácido a-lipoico, coenzima Q, idebenona ou derivados dos mesmos.
Em uma modalidade particular, o agente que inibe enzimas de degradação de suor é selecionado, por exemplo e não restrito a, a partir do grupo formado por citratos de trialquila como citrato de trimetila, citrato de tripropila, citrato de triisopropila, citrato de tributila ou citrato de trietila; sulfato ou fosfato de lanosterina, colesterina, campesterina, estigmasterina e sitosterina; ácidos dicarboxilicos e seus ésteres, como ácido glutárico, glutarato de monoetila, glutarato de dietila, ácido adípico, adipato de monoetila, adipato de dietila; ácido malônico e malonato de dietila, ácidos hidroxicarboxilicos e seus ésteres como ácido málico, ácido tartárico ou tartrato de dietila, glicinato de zinco e/ou misturas dos mesmos.
Em outra modalidade particular, o agente que tem a capacidade de filtrar raios UV é selecionado, por exemplo e não restrito a, a partir do grupo formado por agentes fotoprotetores orgânicos ou minerais ativos contra raios ultravioleta A e/ou B como benzotriazóis substituídos, difenilacrilatos substituídos, complexos de níquel orgânico, umbeliferona, ácido urocânico, derivados de bifenila,
53/67 estilbeno, 3-benzilideno cânfora, e derivados dos mesmos como
3- (4-metilbenzilideno)cânfora; derivados de ácido 4aminobenzoico, 4-(dimetilamino)benzoato de 2-etilhexila, 4(dimetilamino)benzoato de 2-octila e 4-(dimetilamino)benzoato de amila; ésteres de ácido cinâmico, como 4-metoxicinamato de 2-etilhexil ou benzoato de dietilamino hidroxibenzoil hexila,
4- metoxicinamato de propila, 4-metoxicinamato de isoamila, cinamato de 2-etilhexila (octocrilenos) 2-ciano-3,3-fenila; ésteres de ácido salicíclico, como salicilato de 2etilhexila, salicilato de 4-isopropilbenzila, salicilato de homomentila; derivados de benzofenona, como 2-hidróxi-4metoxibenzofenona, 2-hidróxi-4-metoxi-4'-metilbenzofenona, 2,2'-diidroxi-4-metoxibenzofenona; ésteres de ácido benzalmalonico, como 4-metoxibenzalmalonato de di-2etilhexila; derivados de triazina, como 2,4,6-trianilino, βcarbo-2 '-etil-1'-hexiloxi-1 ,3,5-triazina, octil triazona ou dioctil butamido triazonas; propano-1 ,3-dionas, como 1—(4— tert-butilfenil)-3-(4'-metoxifenil)propano-1 ,3-diona; derivados de cetotriciclo(5.2.1.0)decano; ácido 2fenilbenzimidazol-5-sulfônico; derivados de ácido benzofenona sulfônico, como ácido 2-hidróxi-4-metoxibenzofenona-5sulfônico e seus sais; ácido 4-(2-oxo-3bornylidenemetil)benzenosulfônico, derivados de benzoil metano, como ácido benzoil metano 2-metil-5-(2-oxo-3bornilideno)sulfônico, como 1-(4'-tert-butilfenil)-3-(4'metoxifenil)propano-1,3-diono, 4-tert-butil-4' metoxidibenzoilmetano, l-fenil-3-(4'-isopropilfenil)-propano1 ,3-diona, compostos de enamina, antranilatos, silícios, derivados de benzimidazol, imidazolinas, derivados de benzoíla, Chromabright™ [INCI: Dimetilmetoxi Cromanil Palmitato] ou Preventhelia® [INCI: Diaminopropionoil Tripeptideo-33] ambos comercializados por Lipotec, óxidos de metal como óxido de zinco, titânio, ferro, zircônio, silício,
54/67 manganês, alumínio e cério; silicatos, talco, sulfato de bário, estearato de zinco, nanotubos de carbono e/ou misturas dos mesmos.
Além disso, em outra modalidade particular, o agente que estimula ou regula a diferenciação de queratinócito é selecionado, por exemplo e não restrito a, a partir do grupo formado por minerais como cálcio, retinóides como retinol ou tretinoína, análogos de vitamina D3 como calcitriol, calcipotriol ou tacalcitol, lupina (Lupinus albus) extrato como aquele comercializado por SILAB sob o nome Structurin® [INCI: Proteína de Lupina Hidrolisada], sulfato de /^-sitosterol, como aquele comercializado por Vincience/ISP sob o nome Phytocohesine PSP® [INCI: Sulfato de Beta-sitosterol Sódio], mais (Zea Mays) extrato como aquele comercializado por Solabia sob o nome Phytovityl C® [INCI: água (Agua), Extrato de Milho Verde (Zea Mays)], glicoconjugados de Helix Aspersa Muller e/ou misturas dos mesmos.
Da mesma forma, em outra modalidade particular, the relaxante muscular, o agente que inibe a concentração muscular, o agente que inibe o agrupamento de receptor de acetilcolina e/ou o agente anticolinárgico é selecionado, por exemplo e não restrito a, a partir do grupo formado por extratos de Atropa belladonna, Hyoscyamus niger, Mandragora officinaruin, Chondodendron tomentosum, plantas do gênero Brugmansía, ou do gênero Datura, toxina de Clostridium botulinum, peptídeos derivados da proteína SNAP-25 ou Inyline™ [INCI: Acetil Hexapeptídeo-30] comercializado por Lipotec, baclofeno, carbidopa, levodopa, bromocriptina, clorphenesina, clorzoxazona, donepezil, mefenoxalona, reserpina, tetrabenazina, dantrolena, tiocolquicosida, tizanidina, clonidina, prociclidina, glicopirrolato, atropina, hiosciamina, benztropina, escopolamina,
55/67 prometazina, difenhidramina, dimenhidrinato, diciclomina, ciclobenzaprina, orfenadrina, flavoxato, ciclopentolato, ipratrópio, oxibutinina, pirenzepina, tiotrópio, trihexifenidila, tolterodina, tropicamida, solifenacina, darifenacina, mebeverina, trimetafana atracúrio, cisatracúrio, doxacúrio, fazadinio, metocurina, mivacúrio, pancurônio, pipecurônio, rapacurônio, tubocuranina, dimetil tubocuranina, rocurônio, vecurônio, suxametônio, 18metoxicoronaridina, carisoprodol, febarbamato, meprobamato, metocarbamol, fenprobamato, tibamato, agentes anticonvulsantes como levetiracetam, estiripentol, fenobarbital, metilfenobarbital, pentobarbital, metarbital, barbexaclona, pirimidona, carbamazepina, oxcarbazepina, benzodiazepinas, por exemplo e não restrito a, clonazepam, cloxazolam, clorazepato, diazepam, flutoprazepam, lorazepam, midazolam, nitrazepam, nimetazepam, fenazepam, temazepam, tetrazepam ou clobazam, dentre outros.
Em outra modalidade particular, as nanocápsulas da presente invenção compreendem outros ingredientes ativos e/ou adjuvantes farmacêuticos de qualquer natureza, hidrófobos, hidrófilos ou anfifilos, que podem ser encontrados dentro das nanocápsulas em solução ou em suspensão na matriz lipídica, ou na fase aquosa da microemulsão. Em particular, os ingredientes ativos e/ou adjuvantes farmacêuticos são selecionados, por exemplo e não restrito a, a partir do grupo formado por antiácidos, agentes contra úlceras pépticas e doença do refluxo gastroesofágico, antiespasmódicos, analgésicos, fármacos anticolinérgicos, fármacos propulsivos, antieméticos, fármacos antináusea, agentes para terapia biliar, agentes para terapia hepática, lipotrópicos, laxantes, antidiarreicos, adsorbentes intestinais, antipropulsivos, fármacos anti-inflamatórios, ingredientes ativos contra obesidade, enzimas, fármacos hipoglicêmicos,
56/67 insulina e análogos, vitaminas, proteínas, minerais, esteroides anabólicos, agentes antitrombóticos, antifibrinolíticos, agentes hemostáticos, agentes antiarrítmicos, estimulantes cardíacos, glicosídeos cardíacos, vasodilatadores, agentes antiadrenérgicos, fármacos anti-hipertensivos, diuréticos, agentes de economia de potássio, anti-hemorroidais, agentes de terapia antivarizes, agentes de estabilização capilar, agentes que atuam no sistema de renina-angiotensina, betabloqueadores, bloqueadores de canal de cálcio seletivo, bloqueadores do canal de cálcio não seletivo, inibidores de ACE, inibidores de angiotensina II, agentes de modificação de lipídeos, antifúngicos, agentes de cicatrização, antipruríticos, antihistaminas, anestésicos, antipsoriáticos, fármacos quimioterápicos, corticosteroides, antisépticos, desinfetantes, agentes antiacne, produtos para uso ginecológico, oxitocicos, anticonceptivos, androgênio, estrogênio, progestagênio, estimulantes de ovulação, gonadotropinas, antiandrogênios, produtos para uso urológicos, antiespasmódicos, fármacos usados em hipertrofia prostática benigna, hormônios, antagonistas de hormônio, antibióticos, tetraciclinas, anfenicóis, antibacterianos beta-lactam, penicilina, sulfonamidas, trimetoprim, macrolídeos, lincosamidas, estreptograminas, aminoglicosídeos antibacterianos, quinolonas antibacterianas, antivirals, soro imune, imunoglobulinas, agentes antineoplásticos, agentes imunomodulatórios, agentes de alquilação, antimetabólitos, alcalóides vegetais e outros produtos naturais, antibióticos citotóxicos, agentes imunossupressores, fármacos para transtornos do sistema músculo esquelético, antirreumáticos, agentes relaxantes musculares, agentes que afetam a estrutura óssea e mineralização, fármacos que atuam no sistema nervoso, anestésicos gerais, anestésicos locais, opioides, agentes
57/67 antimigraina, anticonvulsivos, agentes colinérgicos, agentes dopaminérgicos, antipsicóticos, ansioliticos, hipnóticos, sedativos, antidepressivos, psicoestimulantes, fármacos antidemência, parassimpatomiméticos, fármacos usados em transtornos aditivos, agentes antivarizes, agentes antiparasitários, inseticidas, repelentes contra insetos, descongestionantes nasais, agentes mucolíticos, supressores de tosse, ingredientes ativos oftálmicos, ingredientes ativos otólogicos, fármacos antiglaucoma, mióticos, midriáticos, cicloplégicos e/ou misturas dos mesmos.
Em outra modalidade particular, as nanocápsulas da presente invenção que contêm ingredientes ativos e/ou adjuvantes cosméticos e/ou farmacêuticos podem ser incorporados a fibras naturais ou sintéticas de materiais têxteis antes ou após sua fabricação. Nessa invenção, compreende-se que os materiais têxteis são tecidos de tecido, tecidos de não tecido, trajes e dispositivos médicos. Esses materiais têxteis, em contato direto com a pele do corpo, liberam os ingredientes ativos incorporados ao sistema de entrega da presente invenção por biodegradação do sistema de ligação para o tecido de tecido, tecido de não tecido ou dispositivo médico ou devido ao atrito entre os mesmos e o corpo, devido à umidade corpórea, ao pH da pele ou à temperatura corpórea. Exemplos de tecidos de tecido, tecidos de não tecido, trajes, dispositivos médicos e meios para imobilização de sistemas de entrega podem ser encontrados na técnica anterior (J. Cont. Release 2004, 97, 313 a 320) . Meios para imobilização de sistemas de entrega em materiais têxteis preferenciais são a aplicação por meio de um foulard, banho de exaustão ou aspersão. As fibras naturais e/ou sintéticas podem ser lã, algodão, seda, fibras de náilon, celulose, poliamida ou poliéster dentre outras. Dentre os materiais têxteis, os tecidos de tecido, tecidos de não
58/67 tecido, trajes e dispositivos médicos preferenciais são bandagens, gazes, camisas, meias, calças apertadas, roupas íntimas, espartilhos, luvas, fraldas, absorventes, vestidos, lençóis, lenços, hidrogéis, emplastros adesivos, emplastros não adesivos, emplastros microelétricos e/ou máscaras faciais.
De acordo com outro aspecto, essa invenção se refere a uma composição cosmética, farmacêutica e/ou alimentícia que compreende as nanocápsulas da presente invenção.
As nanocápsulas da presente invenção podem também ser adsorvidas nos polímeros orgânicos sólidos ou suportes minerais sólidos, por exemplo, e não restrito a, talco, bentonita, silica, amido ou maltodextrina dentre outros.
As nanocápsulas da presente invenção podem ser incorporadas em qualquer forma de alimento funcional ou alimento enriquecido ou em cosméticos orais ou nutricosméticos e formuladas com os excipientes e adjuvantes usuais para composições orais ou suplementos alimentares, por exemplo, e não restrito a, componentes graxos, componentes aquosos, umectantes, conservantes, agentes texturizantes, flavorizantes, aromas, antioxidantes e corantes alimentícios comumente usados na indústria alimentícia.
As composições cosméticas, farmacêuticas e/ou alimentares que compreendem as nanocápsulas da presente invenção podem ser preparadas através dos métodos convencionais conhecidos pelos versados na técnica. As composições cosméticas, farmacêuticas e/ou alimentares que incorporam as nanocápsulas da presente invenção podem ser uma composição final, disponível para aplicação sem ter que executar qualquer tipo de procedimento de concentração, solução, diluição, dispersão, pulverização, aspersão ou qualquer outro procedimento similar conhecido pelo versado na
59/67 técnica, ou uma composição intermediária para a qual um ou inúmeros dos procedimentos anteriores serão executados ou qualquer outro procedimento conhecido pelo versado na técnica com a finalidade de obter uma composição final.
As composições cosméticas, farmacêuticas e/ou alimentares que compreendem as nanocápsulas da presente invenção podem ser administradas por administração tópica ou transdérmica, oralmente, ou por qualquer outro tipo de rota adequada, por exemplo, parenteral, e os excipientes cosmética e/ou farmaceuticamente aceitáveis necessários para a formulação do método de administração desejado serão incluídos. No contexto da presente invenção, o termo parenteral inclui rotas nasais, auriculares, oftálmicas, retais, uretrais e vaginais, injeções subcutâneas, intradérmicas, intravasculares, como intravenosas, intramusculares, intraoculares, intravítreas, intracorneais, intraespinhais, intramedulares, intracraniais, intracervicais, intracerebrais, intrameníngea, intraarticular, intrahepática, intratorácica, intratraqueal, intratecal e intraperitoneal, bem como quaisquer outras técnicas de infusão ou injeção similares.
As composições cosméticas e/ou farmacêuticas que compreendem as nanocápsulas da presente invenção podem ser usadas em diferentes tipos de composições de aplicação tópica e transdérmica que, opcionalmente, irão incluir os excipientes cosmética e/ou farmaceuticamente aceitáveis necessários para a formulação do método de administração desejado. As composições de aplicação tópica ou transdérmica podem ser apresentadas em qualquer formulação sólida, líquida ou semissólida, por exemplo, e não restrito a, cremes, múltiplas emulsões, por exemplo, e não restrito a, óleo e/ou silicone em emulsões de água, emulsões de água em óleo e/ou silicone, emulsões do tipo água/óleo/água ou
60/67 água/silicone/água, e emulsões do tipo óleo/água/óleo ou silicone/água/silicone, composições anidro, dispersões aquosas, óleos, leites, bálsamos, espumas, loções, géis, géis creme, soluções hidroalcoólicas, soluções hidroglicólicas, hidrogéis, linimentos, soros, sabões, xampus, condicionadores, soros, filmes de polissacarideo, unguentos, mousses, pomadas, pós, barras, lápis e aspersores ou aerossóis, incluindo formulações com ou sem enxágue. Essas formulações de aplicação tópica e transdérmica podem ser incorporadas por técnicas conhecidas pelos versados na técnica em diferentes tipos de acessórios sólidos, por exemplo, e não restrito a, bandagens, gazes, camisas, meias, meias-calças, roupas intimas, cintas, luvas, fraldas, absorventes higiênicos, curativos, colchas, lenços, remendos adesivos, remendos não adesivos, remendos microelétricos ou máscaras faciais, ou podem ser incorporados em diferentes produtos de maquiagem como base de maquiagem, por exemplo, bases fluidas e bases compactas, loções de remoção de maquiagem, leites de remoção de maquiagem, corretivos para os olhos, sombras, batons, protetores labiais, batons brilhosos e pós, dentre outros. As composições cosméticas ou dermofarmacêuticas da presente invenção podem também ser incorporadas em produtos para o tratamento e/ou cuidado de unhas e cutículas como vernizes de unha, loções para remover verniz de unha e loções para remover verniz de unha, dentre outros.
As composições cosméticas, farmacêuticas e/ou alimentares que compreendem as nanocápsulas da presente invenção podem ser usadas em diferentes tipos de formulações para administração oral, de preferência, sob a forma de cosméticos ou fármacos orais, por exemplo, e não restrito a, cápsulas, incluindo cápsulas de gelatina, cápsulas macias, cápsulas rígidas, tabletes, incluindo tabletes de açúcar
61/67 revestidos, pós, grânulos, goma de mascar, soluções, suspensões, emulsões, xaropes, filmes de polissacarideo, geleias ou gelatinas e qualquer outra forma conhecida pelo versado na técnica.
Em outra modalidade particular, as composições que compreendem as nanocápsulas da presente invenção podem ser usadas para o tratamento de materiais têxteis e podem ser encontradas em agentes de lavagem em forma liquida, bem como detergentes, na fabricação de emulsões, auxiliadores de enxágue, agentes de enxágue, amaciantes de tecido, aspersores, sabões líquidos ou géis ou também em forma sólida, como produtos em pós, grânulos ou compactos. Adicionalmente, essas composições contêm outros componentes, por exemplo, e não restrito a, tensoativos, agentes que aumentam a absorção percutânea, agentes para o pré-tratamento de materiais têxteis, agentes para o tratamento de marcas, abrasivos, amaciantes de água, amaciantes de tecidos, solventes ou agentes solubilizantes, agentes para a variação de toque e acabamento, agentes repelentes de sujeira, agentes antiestáticos, enzimas, agentes que auxiliam na passagem de rupas, agentes clareadores de cor e/ou corante, agentes de brilho, agentes clareadores ópticos, inibidores de acinzentamento ou compostos para o desprendimento de sujeiras, inibidores de transferência de cor, agentes de fobização e impregnação, agentes de intumescência ou espessantes, agentes de geração de consistência, agentes de silício, agentes que aumentam a absorção percutânea de microcápsulas, agentes branqueadores e ativadores de alvejamento de material têxtil, agentes de hidrofilização e/ou misturas dos mesmos.
Outro aspecto da presente invenção se refere ao uso de composições cosméticas, farmacêuticas e/ou alimentares que compreendem as nanocápsulas da presente invenção para o
62/67 tratamento e/ou cuidado da pele, couro cabeludo, cabelo e unhas. De preferência, o tratamento e/ou cuidado da pele, cabelo, couro cabeludo e/ou unhas é selecionado do grupo formado por tratamento e/ou prevenção do envelhecimento da pele, cicatrização da pele e/ou couro cabeludo, tratamento dermatológico de doenças da pele, tratamento e/ou prevenção de celulite, bronzeamento da pele, clareamento da pele ou branqueamento e tratamento e/ou prevenção da perda de cabelo. No contexto da presente invenção, o termo envelhecimento se refere às alterações vivenciadas pela pele com a idade (cronoenvelhecimento) ou devido à exposição ao sol (fotoenvelhecimento) ou a agentes ambientais como fumaça de cigarro, condições climáticas extremas de frio ou vento, poluentes guímicos ou poluição, e inclui todas as alterações visíveis externas, bem como aquelas notáveis pelo toque, por exemplo, e não restrito a, o desenvolvimento de descontinuidades na pele como rugas, linhas de expressão finas, sulcos, irregularidades ou aspereza, aumento no tamanho de poros, perda de elasticidade, perda de firmeza, perda de maciez, perda da capacidade de recuperação da deformação, flacidez da pele como bochechas flácidas, a aparência de bolsas sob os olhos ou a aparência de um queixo duplo, dentre outras, alterações na cor da pele como marcas, avermelhamento, bolsas sob os olhos, aparência de áreas hiperpigmentadas como manchas na pele ou sardas, dentre outras, diferenciação anômala, hiperqueratinização, elastose, queratose, perda de cabelo, pele casca de laranja, perda de estrutura de colágeno e outras alterações histológicas da camada córnea, da derme, epiderme, sistema vascular (por exemplo, a aparência de veias da aranha ou telangiectasias) ou de tecidos próximos à pele, dentre outras.
Outro aspecto da presente invenção se refere ao uso de composições cosméticas, farmacêuticas e/ou alimentares que
63/67 contêm as nanocápsulas da presente invenção para o tratamento de materiais têxteis.
Os exemplos específicos a seguir aqui fornecidos servem para ilustrar a natureza da presente invenção. Esses exemplos estão incluídos somente para fins ilustrativos e não devem ser interpretados como limitações na invenção aqui reivindicada.
EXEMPLOS
METODOLOGIA GERAL
Todos os reagentes e solventes são de qualidade de síntese e são usados sem qualquer tratamento adicional.
As homogeneizações de alta pressão foram executadas em um microfluidizador modelo Ml 10-Y da Microfluidics. O misturador Ultraturrax para a formação de microemulsões é o modelo D-8 da Miccra RT.
Os peptídeos termolábeis hidrofílicos sob a forma de microemulsão foram nanoencapsulados por meio de coacervação complexa. A matriz lipídica das nanocápsulas continha apenas lipidios ou óleos líquidos, assim, não foi necessário aplicar calor durante todo o processo e a degradação dos peptídeos foi evitada.
EXEMPLO 1
Preparação de microemulsões de peptídeos hidrofílicos para sua encapsulação subsequente em nanocápsulas coacervadas que contêm lipidios líquidos.
Exemplo 1-a. Microemulsão do peptideo H-Dpr-AlaAsn-His-QH
Ducosato [INCI: DIETIL-HEXIL SULFOSUCCINATO DE SÓDIO] e ácido isoesteárico [INCI: ÁCIDO ISOSTEÁRICO] (fase A) foram juntamente misturados em um recipiente adequado. Em outro recipiente, o peptideo H-Dpr-Ala-Asn-His-OH foi dissolvido em etanol [INCI: ÁLCOOL]. Uma vez dissolvido, água foi adicionada (fase B).
64/67 agitação.
A fase B foi adicionada à fase A lentamente sob
INGREDIENTE (Nomenclatura INCI) | % EM PESO |
A DIETIL-HEXIL SULFOSUCCINATO DE SÓDIO/ | 89, 75 |
ÁCIDO ISOSTEÁRICO (15/85) | |
B H-Dpr-Ala-Asn-His-OH | 0,25 |
B Água (AQUA) | 7, 00 |
B ÁLCOOL | 3, 00 |
Exemplo 1-b. Microemulsão do peptídeo Ac-Arg-AsnHls-Clt-NH2
Ducosato [INCI: DIETIL-HEXYL SULFOSUCCINATO DE SÓDIO] e ácido isoesteárico [INCI: ÁCIDO ISOSTEÁRICO] (fase A) foram juntamente misturados em um recipiente adequado.
Em outro recipiente, o peptídeo Ac-Arg-Asn-His-CitNH2 foi dissolvido em água. Uma vez dissolvido, etanol [INCI: ÁLCOOL] (fase B) foi adicionado.
A fase B foi adicionada à fase A lentamente sob agitação.
INGREDIENTE (Nomenclatura INCI) | % EM PESO |
A DIETIL-HEXIL SULFOSUCCINATO DE SÓDIO/ | 89, 84 |
ÁCIDO ISOESTEÁRICO (15/85) | |
B Ac-Arg-Asn-His-Cit-NH2 | 0,16 |
B Água (AQUA) | 4, 00 |
B ÁLCOOL | 6, 00 |
EXEMPLO 2
Preparação de | nanocápsulas | coacervadas | com | |
peptideos | microemulsificados hidrofilicos | contendo | apenas | |
lipidios | líquidos. Em um recipiente | adequado, os | seguintes | foram |
adicionados nessa ordem: | água, Amigei [INCI: | GOMA |
ESCLERÓTICA], ácido hialurônico [INCI: HIALURONATO DE SÓDIO],
Zemea [INCI: PROPANODIOL] e fenoxietanol [INCI: FENOXIETANOL]
65/67 (ingredientes A), e a mistura foi agitada até a homogeneidade ser alcançada.
Em outro recipiente, a microemulsão do peptídeo correspondente preparado de acordo com o exemplo 1, óleo de feijão-soja [INCI: ÓLEO DE SOJA (FEIJÃO-SOJA) DE GLICINA] , Arlacel 83 [INCI: SESQUIOLEATO DE SORBITANO] e Arlamol HD [INCI: ISOHEXADECANO] (ingredientes B) foram misturados.
Depois, a mistura de ingredientes B foi adicionada à mistura de ingredientes A, sob agitação com a turbina até que a emulsão fosse formada.
Finalmente, a mistura foi homogeneizada sob pressão em um microf luidizador por 3 ciclos com uma pressão de entrada de 80 bar e pressão na saída de 15.000 psi. Durante todo o processo, a amostra foi mantida a 25°C por meio de um circuito refrigerado de água/glicol.
Depois, uma suspensão de Quat Soy LDMA 25 [INCI: PROTEÍNA DE SOJA HIDROLISADA DE LAURILDIMÔNIO HIDROXIPROPIL] (ingredientes C) em água foi adicionada por gotejamento sob agitação.
Para o peptídeo H-Dpr-Ala-Asn-His-OH, a microemulsão preparada de acordo com o exemplo 1-a foi usada.
INGREDIENTE (Nomenclatura INCI) | % EM PESO |
A Água (AQUA) | QSP100 |
A GOMA ESCLERÓTICA | 0,50 |
A PROPANODIOL | 5, 00 |
A FENOXIETANOL | 2, 6 |
A HIALURONATO DE SÓDIO | 0, 01 |
B H-Dpr-Ala-Asn-His-OH, DIETIL-HEXIL | |
SULFOSUCCINATO DE SÓDIO/ÁCIDO | |
ISOSTEÁRICO (15/85), | 8, 00 |
Água (AQUA), ÁLCOOL | |
B ÓLEO DE SOJA (FEIJÃO-SOJA) DE GLICINA | 12,00 |
66/67
B SESQUIOLEATO DE SORBITANO | 4,30 |
B ISOHEXADECANO | 5, 50 |
C Água (AQUA) | 2,00 |
C PROTEÍNA DE SOJA HIDROLISADA | |
DE LAURILDIMÔNIO HIDROXIPROPIL | 0,20 |
tamanho médio das cápsulas em suspensão obtidas, contendo o peptídeo H-Dpr-Ala-Asn-His-OH e determinadas por Espalhamento de Luz a Laser Dinâmico, foi de 235 nm.
Para o peptídeo Ac-Arg-Asn-His-Cit-NH2, a microemulsão preparada de acordo com o exemplo 1-b foi usada.
INGREDIENTE (Nomenclatura INCI) | % EM PESO |
A Água (AQUA) | QSP100 |
A GOMA ESCLERÓTICA | 0,50 |
A PROPANODIOL | 5, 00 |
A FENOXIETANOL | 2, 6 |
A HIALURONATO DE SÓDIO | 0, 01 |
B Ac-Arg-Asn-His-Cit-NH2, DIETIL-HEXIL | |
SULFOSUCCINATO DE SÓDIO/ ÁCIDO | 10, 00 |
ISOSTEÁRICO (15/85), Água (AQUA), ÁLCOOL | |
B ÓLEO DE SOJA (FEIJÃO-SOJA) DE GLICINA | 10, 00 |
B SESQUIOLEATO DE SORBITANO | 6, 50 |
B ISOHEXADECANO | 3, 00 |
C Água (AQUA) | 2,00 |
C PROTEÍNA DE SOJA HIDROLISADA | 0,20 |
LAURILDIMÔNIO HIDROXIPROPIL |
tamanho médio das cápsulas em suspensão obtidas, contendo o peptídeo Ac-Arg-Asn-His-Cit-NH2 e determinadas por Espalhamento de Luz a Laser Dinâmico, foi de 303 nm.
Na encapsulação de peptídeos, a separação do 10 ingrediente ativo encapsulado e não encapsulado foi executada pela técnica de centrifugação de cesto [David W. Fry et al. Analytical Biochemistry 90: 809 a 815 (1978)] . Uma vez que ambas as frações são tenham sido separadas, a patê não
67/67 encapsulada foi analisada por HPLC. Em nenhum caso foi detectada a presença de peptídeo na fase aquosa da dispersão, portanto, a eficiência de encapsulação foi de quase 100%.
Claims (5)
- REIVINDICAÇÕES1. NANOCÁPSULAS POLIMERICAMENTE REVESTIDAS, caracterizadas pelo fato de que contêm microemulsões de água em lipídios líquidos e que compreendem pelo menos um5 ingrediente hidrofilicamente ativo dissolvido na fase aquosa interna e em que o revestimento polimérico é um coacervato complexo.
- 2. NANOCÁPSULAS, de acordo com a reivindicação 1, caracterizadas em que os lipídios líquidos são selecionados •10 do grupo formado por óleos vegetais, óleo de feijão-soja, óleo de girassol, óleo de milho, óleo de oliva, óleo de palma, óleo de semente de algodão, óleo de colza, óleo de amendoim, óleo de coco, óleo de rícino, óleo de linho, óleo de borragem, óleo de prímula da noite, óleos marinhos, óleos 15 de peixe, óleos de alga, óleos derivados de petróleo, óleo . mineral, parafina líquida, vaselina, álcoois graxos de cadeia curta, álcoois graxos ramificados alifáticos de cadeia média, ésteres de ácidos graxos com álcoois de cadeia curta, miristato isopropílico, palmitato isopropílico, estereato20 isopropílico, adipato isobutílico, triglicerídeos de cadeia média, triglicerídeos cápricos e caprílicos, octanoatos Ci2Ci6, éteres de álcool graxo, éter de dioctila e/ou misturas dos mesmos.• 3. NANOCÁPSULAS, de acordo com a reivindicação 1,25 caracterizadas em que o polímero do revestimento é selecionado do grupo formado por proteínas, polissacarídeos, poliésteres, poliacrilatos, policianoacrilatos, copolímeros e/ou misturas dos mesmos.4. NANOCÁPSULAS, de acordo com a reivindicação 3,30 caracterizadas em que o polímero do revestimento é selecionado do grupo formado por gelatina, albumina, proteína de soja, proteína de ervilha, proteína de fava, proteína de batata, proteína de trigo, proteína de soro de leite, β2/8 lactoglobulina, caseinatos, zeina, alginatos, carragenanas, pectinas, goma arábica, goma xantana, goma guar, quitosano, poli(L-lisina), dextrano sulfato de sódio, carboximetil galactomanano, carboximetil celulose, nitrato de celulose, 5 ftalato acetato de celulose, ftalato de metil hidroxipropil celulose, acetato succinato de hidroxipropil metil celulose, ftalato de polivinil acetato e misturas dos mesmos.5. NANOCÁPSULAS, de acordo com a reivindicação 1, caracterizadas em que o polímero do______revestimento é um •10 polímero catiônico.6. NANOCÁPSULAS, de acordo com a reivindicação 5, caracterizadas em que o polímero catiônico é selecionado do grupo formado por derivados catiônicos de celulose, hidroxietil celulose quaternizada, amidos catiônicos,15 copolímeros de sal de acrilamida e amônio dialila; polímeros de vinilpirrolidona/vinilimidazol quaternizados, produtos de condensação de poliglicóis e aminas, polímeros e copolímeros de poliquartênio, polímeros denominados Merquat de poliquartênio-6, poliquartênio-7, poliquartênio-16,20 poliquartênio-10, poliquartênio-4 copolímeros, dicocoiletilhidroxietilamônio, copolímeros de enxerto com um esqueleto de celulose e grupos amônio quaternário; polipeptídeos de colágeno quaternizado, colágeno hidrolisado de laurildimônio hidroxipropila, polipeptídeos de trigo 25 quaternizado, polietilenimina, polímeros de silicone catiônico, amidometicona—de—qua.têrnio-_22 silicone, ácido adípico e copolímeros de dimetilamino hidroxipropil dietilenotriamina, copolímeros de ácido acrílico com cloreto de dimetildialilamônio, derivados de quitina catiônica,30 quitosano e seus derivados, produtos de condensação de alquileno dihalógeno catiônico, produtos de condensação de dibromobutano com bisdialquilaminas, bis-dimetilamino-1,3 propano, derivados de goma guar catiônica, guar3/8 hidroxipropiltrimônio, polímeros de sal de amônio quaternário, polímeros de polissacarídeo quaternizado de derivados naturais como azarose, proteínas catiônicas de gelatina, proteínas catiônicas de goma arábica, polímeros 5 catiônicos de poliamidas, polímeros catiônicos de policianoacrilatos, polímeros catiônicos de poliláticos, polímeros catiônicos de poliglicólicos, polímeros catiônicos de polianilina, polímeros catiônicos de polipirrol, polímeros catiônicos de polivinilpirrolidona, polímeros catiônicos de •10 amino silicone polímeros e copolimeros, polímeros catiônicos de poliestireno, polímeros catiônicos de álcool polivinílico, polímeros catiônicos de poliestireno e copolimeros anidridos de ácido maleico, polímeros catiônicos de éter metil vinílico, polímeros catiônicos de resinas epóxi, polímeros 15 catiônicos de estireno e copolimeros de metil metacrilato, metacrilato, poliacrilatos e polimetacrilatos de dimetilamino catiônico, derivados de poliamina opcionalmente substituídos por derivados de polietileno glicol, ácidos de poliamino sob condições de pH em que os mesmos são catiônicos, 20 polietilenoimina; derivados de polivinilpirrolidona quaternizada (PVP) e polímeros de uretano hidrofílico, bem como qualquer mistura dos grupos catiônicos mencionados acima.7. NANOCÁPSULAS, de acordo com a reivindicação 1,25 caracterizadas em que o ingrediente hidrofilicamente ativo é selecionado do grupo formado por—aminoácidos, peptídeos, proteínas, proteínas hidrolisadas, enzimas, hormônios, vitaminas, sais minerais, açúcares, nucleotídeos, ácidos nucleicos, moléculas e extratos de origem biológica e30 biotecnológica, vacinas, moléculas hidrofílicas sintéticas ou parcialmente sintéticas e/ou misturas dos mesmos.8. NANOCÁPSULAS, de acordo com a reivindicação 1, caracterizadas em que compreendem outros ingredientes ativos4/8 e/ou adjuvantes cosméticos, farmacêuticos e/ou alimentícios . 9. NANOCÁPSULAS, de acordo com a reivindicação 8, caracterizadas em que os ingredientes ativos e/ou adjuvantes selecionados do grupo ou substâncias que retêm agentes que estimulam a de cura coadjuvantes, agentes que estimulam agentes de reepitelização coadjuvante, sintetizam macromoléculas dérmicas ou redensificação e/ou cosméticos e/ou alimentícios são formado por tensoativos, umectantes umidade, hidratantes ou emolientes, cura, agentes reepitelização, agentes - que epidérmicas, agentes de firmeza restruturação, fatores de crescimento de citocina, agentes que atuam na circulação capilar e/ou microcirculação, agentes antiglicação, sequestrantes de radical livre e/ou agentes de poluição antiatmosférica, sequestrantes de espécies de carbonila ativa, agentes de inibição de 5a redutase, agentes de inibição de lisil e/ou prolil redutase, agentes de estímulo de síntese de defensina, agentes bactericidas e/ou agentes bacteriostáticos e/ou agentes antimicrobianos e/ou agentes germicidas e/ou agentes fungicidas e/ou agentes e/ou agentes de inibição de germe, agentes agentes antiparasitários, agentes antiAgentes de inibição de NO sintase, agentes de ou agentes querotolíticos e/ou agentes agentes comedolíticos, agentes antipsoriase, agentes anticaspas, agentes anti-inflamatórios e/ou analgésicos,- agentes anestésicos;- agentes- antirrugas -e/ouantienvelhecimento, fungistáticos antivirais, histamínicos, descamação esfoliantes, desodorantes para mascaramento de odor absorvente, agentes perfumar e/ou óleos isolados, cosmético substâncias para compostos aromáticos isolados, agentes inibem permeabilidade vascular, , agentes de branqueamento ou inibem enzimas de corpóreo e/ou antirrespirantes, perfumados e/ou antioxidação, agentes que enzimas epidérmicas hidrolíticas despigmentação de pele, agentes que5/8 degradação de suor, agentes que têm a capacidade de filtrar Raios UV, agentes que estimulam ou regulam diferenciação de queratinócito, agentes anticoceira, agentes que estimulam ou inibem a síntese de melanina, agentes pró-pigmentação, 5 agentes de autobronzeamento, agente de estímulo de proliferação de melanócito, propelentes líquidos, vitaminas, aminoácidos, proteínas, biopolímeros, polímeros gelificantes, agentes de relaxamento de pele, agentes que têm a capacidade de reduzir ou tratar bolsas sobre os olhos, agentes para o *10 tratamento e/ou cuidado de pele sensível, agentes adstringentes, agentes que regulam produção de sebo, agentes antiestrias, agentes lipolíticos ou agentes que estimulam lipólise, agentes venotônicos, agentes anticelulite, agentes calmantes, agentes que atuam no metabolismo celular, agentes 15 para aperfeiçoar a junção dérmica-epidérmica, agentes que induzem crescimento de cabelo ou retardantes de perda de cabelo, agentes que inibem ou retardam o crescimentode pelos, agentes de estímulo de síntese de proteína por choque térmico, relaxantes musculares, agentes de inibiçãode20 contração muscular, agentes que inibem agrupamentode receptor de acetilcolina, agentes colinérgicos, agentes inibidores de elastase, agentes inibidores de metaloproteinase da matriz, agentes quelantes, extratos “ vegetais, óleos essenciais, extratos marinhos, sais minerais, 25 extratos celulares, agentes emulsificantes, agentes que estimulam a síntese de lipídeos e componentes... da camada córnea, ceramidas, ácidos graxos, agentes obtidos a partir de um processo de biofermentação e/ou misturas dos mesmos.10. NANOCÁPSULAS, de acordo com a reivindicação 9,30 caracterizadas em que os ingredientes ativos e/ou adjuvantes farmacêuticos são selecionados do grupo formado por antiácidos, agentes contra úlceras pépticas e doença do refluxo gastroesofágico, antiespasmódicos, analgésicos, ξ>/3 fármacos anticolinérgicos, fármacos propulsivos, antieméticos, fármacos antináusea, agentes para terapia biliar, agentes para terapia hepática, lipotrópicos, laxantes, antidiarreicos, adsorbentes intestinais,5 antipropulsivos, fármacos anti-inflamatórios, ingredientes ativos contra obesidade, enzimas, fármacos hipoglicêmicos, insulina e análogos, vitaminas, proteínas, minerais, esteroides anabólicos, agentes antitrombóticos, antifibrinolíticos, agentes hemostáticos, agentes •10 antiarrítmicos, estimulantes cardíacos, glicosídeos cardíacos, vasodilatadores, agentes antiadrenérgicos, fármacos anti-hipertensivos, diuréticos, agentes de economia de potássio, anti-hemorroidais, agentes de terapia antivarizes, agentes de estabilizaçao capilar, agentes que 15 atuam no sistema de renina-angiotensina, betabloqueadores, . bloqueadores do canal de cálcio seletivo, bloqueadores do canal de cálcio não seletivo, Inibidores de ACE, inibidores de angiotensina II, agentes de modificação de lipídeos, antifúngicos, agentes de cicatrização, antipruríticos, anti20 histaminas, anestésicos, antipsoriáticos, fármacos quimioterápicos, corticosteroides, antisépticos, desinfetantes, agentes antiacne, produtos para uso ginecológico, oxitocicos, anticonceptivos, androgênio, estrogênio, progestagênio, estimulantes de ovulação,25 gonadotropinas, antiandrogênios, produtos para uso urológicos,-antiespasmódicos, -fármacos usados em-hipe-rtrofia prostática benigna, hormônios, antagonistas de hormônio, antibióticos, tetraciclinas, anfenicóis, antibacterianos beta-lactam, penicilina, sulfonamidas, trimetoprim,
- 3 0 macrolídeos, lincosamidas, estreptograminas, aminoglicosídeos antibacterianos, quinolonas antibacterianas, antivirais, soro imune, imunoglobulinas, agentes antineoplásticos, agentes imunomodulatórios, agentes de alquilação, antimetabólitos,
- 7/8 alcalóides vegetais e outros produtos naturais, antibióticos citotóxicos, agentes imunossupressores, fármacos para transtornos do sistema músculo esquelético, antirreumáticos, agentes relaxantes musculares, agentes que afetam estrutura 5 óssea e mineralização, fármacos que atuam no sistema nervoso, anestésicos gerais, anestésicos locais, opioides, agentes antimigraina, anticonvulsivos, agentes colinérgicos, agentes dopaminérgicos, antipsicóticos, ansiolíticos, hipnóticos, sedativos, antidepressivos, psicoestimulantes, fármacos Ί0 antidemência, parassimpatomiméticos, fármacos usados em transtornos aditivos, agentes antivarizes, agentes antiparasitários, inseticidas, repelentes contra insetos, descongestionantes nasais, agentes mucolíticos, supressores de tosse, ingredientes ativos oftálmicos, ingredientes ativos 15 otólogicos, fármacos antiglaucoma, mióticos, midriáticos, cicloplégicos e/ou misturas dos mesmos.11. PROCESSO PARA A PREPARAÇÃO DE NANOCÁPSULAS definido naPOLIMERICAMENTE REVESTIDAS, conforme reivindicação 1, caracterizado pelo fato de que compreende a) preparação de uma emulsão de água em óleo (w/o) de uma solução aquosa de um ingrediente hidrofilicamente ativo em óleos ou lipídios líquidos, microemulsão complexa da polimérico.12 .ALIMENTÍCIA, e b) encapsulação por coacervação de um revestimento por meioCOSMÉTICA,COMPOSIÇÃO caracterizada_p_e.l_o_. f ato conforme definido emFARMACÊUTICA E/OU de que compreende as nanocápsulas, reivindicações 1, 2, 3, 4, 5, 6, 7, 8, 913. COMPOSIÇÃO, de acordo com caracterizada em que as nanocápsulas são polímero orgânico sólido ou suporte selecionado do grupo formado por talco, bentonita, silica, qualquer uma das ou10 .reivindicação12, adsorvidas em um mineral sólido amido ou maltodextrina.
- 8/814. COMPOSIÇÃO, de acordo com a reivindicação 12, caracterizada em que essa composição é apresentada em uma formulação selecionada do grupo formado por cremes, múltiplas emulsões, composições anidro, dispersões aquosas, óleos, 5 leites, bálsamos, espumas, loções, géis, géis creme, soluções hidroalcoólicas, soluções hidroglicólicas, hidrogéis, linimentos, soros, sabões, xampús, condicionadores, soro, unguentos, mousses, pomadas, pós, barras, lápis, vaporizadores, aerossóis, cápsulas, cápsulas de gelatina, •10 cápsulas macias, cápsulas rígidas, tabletes, tabletes de açúcar revestidos, grânulos, goma de mascar, soluções, suspensões, emulsões, xaropes, filmes de polissacarídeo, geleias e gelatina.15. COMPOSIÇÃO, de acordo com a reivindicação 12,15 caracterizada em que essa composição é incorporada a um . produto selecionado do grupo formado por corretivos sobre os olhos, base de maquiagem, loções de remoção de maquiagem, leites de remoção de maquiagem, sombras para olhos, batons, batom brilhoso, protetores de lábios e pós.20 16. COMPOSIÇÃO, de acordo com a reivindicação 12, caracterizada em que as nanocápsulas sao incorporadas em um tecido de tecido, um tecido de não tecido ou um dispositivo médico.‘ 17. USO DA COMPOSIÇÃO COSMÉTICA, FARMACÊUTICA E/OU25 ALIMENTÍCIA, conforme definido na reivindicação 12, caracterizado pelo fato de .que é para o tratamento e/ou cuidado da pele, escalpo, cabelo e unhas.18. USO DA COMPOSIÇÃO cosmética e/ou farmacêutica, conforme definido na reivindicação 12, caracterizado pelo 30 fato de qué é para o tratamento de materiais têxteis.
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MY166518A (en) | 2018-07-05 |
ES2386177A1 (es) | 2012-08-10 |
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EP2618926A2 (en) | 2013-07-31 |
US10758490B2 (en) | 2020-09-01 |
WO2012038061A2 (en) | 2012-03-29 |
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Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 20/09/2011, OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF, QUE DETERMINA A ALTERACAO DO PRAZO DE CONCESSAO. |
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B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 13A ANUIDADE. |