BR102018013490A2 - chlorhexidine digluconate polymer nanoparticles - Google Patents

chlorhexidine digluconate polymer nanoparticles Download PDF

Info

Publication number
BR102018013490A2
BR102018013490A2 BR102018013490A BR102018013490A BR102018013490A2 BR 102018013490 A2 BR102018013490 A2 BR 102018013490A2 BR 102018013490 A BR102018013490 A BR 102018013490A BR 102018013490 A BR102018013490 A BR 102018013490A BR 102018013490 A2 BR102018013490 A2 BR 102018013490A2
Authority
BR
Brazil
Prior art keywords
chlorhexidine digluconate
nanoparticles
digluconate
polymeric
zein
Prior art date
Application number
BR102018013490A
Other languages
Portuguese (pt)
Other versions
BR102018013490B1 (en
Inventor
Fábio Oliveira De Sousa Francisco
Thayanne Cavalcante Dantas Jennifer
Original Assignee
Fundacao Univ Federal Do Amapa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Fundacao Univ Federal Do Amapa filed Critical Fundacao Univ Federal Do Amapa
Priority to BR102018013490-6A priority Critical patent/BR102018013490B1/en
Publication of BR102018013490A2 publication Critical patent/BR102018013490A2/en
Publication of BR102018013490B1 publication Critical patent/BR102018013490B1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/43—Guanidines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/11—Encapsulated compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
    • A61K8/645—Proteins of vegetable origin; Derivatives or degradation products thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/41—Particular ingredients further characterized by their size
    • A61K2800/413—Nanosized, i.e. having sizes below 100 nm

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

nanopartículas poliméricas de digluconato de clorexidina a presente invenção refere-se à incorporação de digluconato de clorexidina em nanopartículas de zeína em veículo hidroetanólico para uso como agente antimicrobiano. foram testadas diferentes concentrações, sendo as mais promissoras as que continham zeína a 0,0712%, etanol 12,5%-35,1%, e digluconato de clorexidina entre 0,0675 e 0,5% p/v. o uso do nanocarreador polimérico melhorou substancialmente a capacidade bactericida e bacteriostática do digluconato de clorexidina, sendo as referidas concentrações reduzidas pelo menos em 12 e 24 vezes (tabela 1), portanto se poderia reduzir as doses utilizadas sem o comprometimento do efeito antimicrobiano esperado. as referidas formulações mostraram-se ainda estáveis em condições habituais de armazenamento, temperatura ambiente (25°c) e geladeira (4°c), portanto viáveis a serem manufaturadas e utilizadas nas diferentes aplicações nas que o digluconato de clorexidina seja utilizado.polymeric chlorhexidine digluconate nanoparticles the present invention relates to the incorporation of chlorhexidine digluconate into zein nanoparticles in a hydroethanolic vehicle for use as an antimicrobial agent. different concentrations were tested, the most promising being those containing 0.0712% zein, 12.5% -35.1% ethanol, and chlorhexidine digluconate between 0.0675 and 0.5% w / v. the use of the polymeric nanocarrier has substantially improved the bactericidal and bacteriostatic capacity of chlorhexidine digluconate, with the said concentrations being reduced by at least 12 and 24 times (table 1), so one could reduce the doses used without compromising the expected antimicrobial effect. the aforementioned formulations were still stable under usual conditions of storage, room temperature (25 ° c) and refrigerator (4 ° c), therefore feasible to be manufactured and used in the different applications in which chlorhexidine digluconate is used.

Description

RELATÓRIO DESCRITIVODESCRIPTIVE REPORT

NANOPARTÍCULAS POLIMÉRICAS DE DIGLUCONATO DEPOLYMERIC NANOPARTICLES OF DIGLUCONATE OF

CLOREXIDINACHLOREXIDIN

01. A presente invenção refere-se à incorporação de digluconato de clorexidina em nanopartículas poliméricas para uso como agente antimicrobiano.01. The present invention relates to the incorporation of chlorhexidine digluconate in polymeric nanoparticles for use as an antimicrobial agent.

02. O digluconato de clorexidina já possui seu uso consagrado como agente antimicrobiano, seja no âmbito hospitalar como degermante, antisséptico cirúrgico e de feridas, como na área odontológica, como antisséptico em enxaguatórios, na profilaxia da cárie dentária e no tratamento periodontal e endodôntico.02. Chlorhexidine digluconate already has its established use as an antimicrobial agent, whether in the hospital environment as a degenerative, surgical and wound antiseptic, as well as in the dental field, as an antiseptic in mouthwashes, in dental caries prophylaxis and in periodontal and endodontic treatment.

03. Sua efetividade antimicrobiana está relacionada à concentração utilizada, em baixas concentrações sua ação é bacteriostática e em altas concentrações é bactericida.03. Its antimicrobial effectiveness is related to the concentration used, in low concentrations its action is bacteriostatic and in high concentrations it is bactericidal.

04. Na área Odontológica, o digluconato de clorexidina tem demonstrado alguns inconvenientes quando relacionado ao uso prolongado, tais como o enfraquecimento das estruturas ósseas, o escurecimento de tecidos, descamação reversível da mucosa, aumento dos depósitos calcificados supre gengivais, manchas e comprometimento estético.04. In the Dental area, chlorhexidine digluconate has shown some inconveniences when related to prolonged use, such as the weakening of bone structures, the darkening of tissues, reversible peeling of the mucosa, increased calcified deposits supply gingival, stains and aesthetic compromise.

05. A nanotecnologia aplicada ao desenvolvimento farmacêutico visa melhorar questões relacionadas à estabilidade de fármacos, diminuição das doses utilizadas, e consequentemente a diminuição de efeitos adversos decorrentes da utilização dos agentes terapêuticos, tais como o digluconato de clorexidina.05. Nanotechnology applied to pharmaceutical development aims to improve issues related to drug stability, decrease in doses used, and consequently the reduction of adverse effects resulting from the use of therapeutic agents, such as chlorhexidine digluconate.

06. Outro fator importante é garantir que a incorporação do digluconato de clorexidina seja compatível com os constituintes da formulação para que não ocorra redução de sua efetividade, como ocorre quando este é veiculado em dentifrícios, que possuem agentes detergentes, que acarretam na redução da ação antimicrobiana devido a inúmeras incompatibilidades físico-químicas.06. Another important factor is to ensure that the incorporation of chlorhexidine digluconate is compatible with the constituents of the formulation so that there is no reduction in its effectiveness, as occurs when it is carried in dentifrices, which have detergent agents, which reduce the action antimicrobial due to numerous physico-chemical incompatibilities.

Petição 870180161217, de 10/12/2018, pág. 4/8Petition 870180161217, of 10/12/2018, p. 4/8

2/32/3

07. As nanopartículas que constituem a presente invenção apresentaram atividade antimicrobiana in vitro superior, quando comparadas ao fármaco em solução nas mesmas concentrações.07. The nanoparticles that make up the present invention showed superior in vitro antimicrobial activity when compared to the drug in solution at the same concentrations.

08. Estudos microbiológicos in vitro demonstram que o uso das nanopartículas de digluconato de clorexidina apresentam concentrações antibacterianas (MIC concentração inibitória mínima e MBC - concentração bactericida mínima) efetivamente menores do que os agentes antimicrobianos utilizados na prática clínica frente à Streptococcus mutans, conforme a tabela a seguir.08. In vitro microbiological studies demonstrate that the use of chlorhexidine digluconate nanoparticles has antibacterial concentrations (MIC minimum inhibitory concentration and MBC - minimum bactericidal concentration) effectively lower than the antimicrobial agents used in clinical practice against Streptococcus mutans, as shown in the table Next.

09. Tabela 109. Table 1

Teste test MIC (pg/ml) MIC (pg / ml) MBC ( pg/ml) MBC (pg / ml) Referência Reference Nanopartículas de digluconato de clorexidina a 0,25% 0.25% chlorhexidine digluconate nanoparticles 1,62 1.62 3,25 3.25 Digluconato de clorexidina em solução a 0,25% Chlorhexidine digluconate in 0.25% solution 5,96 5.96 10,30 10.30 Digluconato de clorexidina a 0,12% 0.12% chlorhexidine digluconate 40,00 40.00 40,00 40.00 Pinheiro (2012) Pinheiro (2012) Digluconato de clorexidina a 0,2% 0.2% chlorhexidine digluconate 62,50 62.50 83,33 83.33 Ahrari (2015) Ahrari (2015) Triclosano Triclosan 20,80 20.80 20,80 20.80 Mcbain (2004) Mcbain (2004)

Petição 870180161217, de 10/12/2018, pág. 5/8Petition 870180161217, of 10/12/2018, p. 5/8

3/33/3

ReferênciasReferences

AHRARI, F; ESLAMI, N; RAJABI, O; GHAZVINI, K; BARATI, S. The antimicrobial sensitivity of Streptococcus mutans and Streptococcus sangius to colloidal solutions of different nanoparticles applied as mouthwashes. Dental Research Journal. v.12, n.1, p.44-49, 2015.AHRARI, F; ESLAMI, N; RAJABI, O; GHAZVINI, K; BARATI, S. The antimicrobial sensitivity of Streptococcus mutans and Streptococcus sangius to colloidal solutions of different nanoparticles applied as mouthwashes. Dental Research Journal. v.12, n.1, p.44-49, 2015.

MCBAIN, A. J; LEDDER, R. G; SREENIVASAN, P; GILBERT, P. Selection for highlevel resistance by chronic triclosan exposure is not universal. Journal of Antimicrobial Chemotherapy. v.53, p 772-777, 2004.MCBAIN, A. J; LEDDER, R. G; SREENIVASAN, P; GILBERT, P. Selection for highlevel resistance by chronic triclosan exposure is not universal. Journal of Antimicrobial Chemotherapy. v.53, p 772-777, 2004.

PINHEIRO, M. A. Efeito antimicrobiano de tinturas de produtos naturais sobre bactérias da cárie dentária. Revista Brasileira em Promoção Saúde. v.25, n.2, p.197201, 2012.PINHEIRO, M. A. Antimicrobial effect of tinctures of natural products on dental caries bacteria. Brazilian Journal of Health Promotion. V.25, n.2, p.197201, 2012.

10. As nanopartículas são compostas de veículo hidroetanólico, do polímero biodegradável zeína e do digluconato de clorexidina. Em buscas em bases de patentes, não foram identificadas patentes que descrevam tecnologia similar.10. The nanoparticles are composed of a hydroethanolic vehicle, the biodegradable polymer zein and the chlorhexidine digluconate. In searches on patent bases, no patents were identified that describe similar technology.

11. As nanopartículas foram obtidas através de solvatação iônica, sendo as mais promissoras obtidas com a concentração de zeína de a 0,0712 %p/v e etanol a 12,5% v/v, compatíveis com diferentes aplicações.11. The nanoparticles were obtained through ionic solvation, the most promising ones being obtained with a zein concentration of 0.0712% w / v and ethanol 12.5% v / v, compatible with different applications.

12. Com a nanopartícula polimérica formada, foi testada a incorporação de digluconato de clorexidina em diferentes concentrações (0,0675% - 0,5% p/v), sendo as mais promissoras sob o ponto de vista da estabilidade às que continham concentrações menores que 0,25% p/v do fármaco, ainda que as demais tenham mostraram-se efetivas.12. With the polymeric nanoparticle formed, the incorporation of chlorhexidine digluconate in different concentrations (0.0675% - 0.5% w / v) was tested, being the most promising from the point of view of stability to those containing lower concentrations that 0.25% w / v of the drug, even though the others have been effective.

13. A tecnologia apresentou tamanho de partícula, potencial zeta e índice de polidispersão favoráveis, homogeneidade, e estabilidade quando mantida em condições de armazenamento usuais (temperatura ambiente: 25°C e geladeira: 4°C).13. The technology presented favorable particle size, zeta potential and polydispersity index, homogeneity, and stability when maintained under usual storage conditions (room temperature: 25 ° C and refrigerator: 4 ° C).

Claims (5)

NANOPARTÍCULAS POLIMÉRICAS DE DIGLUCONATO DE CLOREXIDINAPOLYMERIC NANOPARTICLES OF CHLOREXIDINE DIGLUCONATE 01. Composição de nanopartículas políméricas caracterizada pelo uso do digluconato de clorexidina em sua composição01. Composition of polymeric nanoparticles characterized by the use of chlorhexidine digluconate in its composition 02. Nanopartículas de acordo com a reivindicação 1 caracterizadas pelo uso do polímero biodegradável zeína dispersas em etanol/agua.02. Nanoparticles according to claim 1 characterized by the use of the biodegradable polymer zein dispersed in ethanol / water. 03. Nanopartículas, de acordo com as reivindicações 1 e 2, caracterizadas pelo uso de zeína a 0,0712% dispersa em etanol 12,5%-35,1% e digluconato de clorexidina entre 0,0675 e 0,5% p/v na sua composição.03. Nanoparticles according to claims 1 and 2, characterized by the use of 0.0712% zein dispersed in 12.5% -35.1% ethanol and chlorhexidine digluconate between 0.0675 and 0.5% w / v in its composition. 04. Uso das nanopartículas de acordo com a reivindicações 1 e 2 caracterizado por sua aplicação como agente bactericida e antisséptico.04. Use of nanoparticles according to claims 1 and 2 characterized by their application as a bactericidal and antiseptic agent. 05. Uso das nanopartículas de acordo com a reivindicação 4 caracterizado por inibir o crescimento de bactérias típicas da cavidade oral, pele e mucosas, tecidos moles e duros, e todos os demais usos nos quais os microrganismos envolvidos apresentem sensibilidade a este agente.05. Use of nanoparticles according to claim 4 characterized by inhibiting the growth of bacteria typical of the oral cavity, skin and mucous membranes, soft and hard tissues, and all other uses in which the microorganisms involved are sensitive to this agent.
BR102018013490-6A 2018-06-29 2018-06-29 CHLOREXIDINE DIGLUCONATE POLYMER NANOPARTICLES BR102018013490B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
BR102018013490-6A BR102018013490B1 (en) 2018-06-29 2018-06-29 CHLOREXIDINE DIGLUCONATE POLYMER NANOPARTICLES

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
BR102018013490-6A BR102018013490B1 (en) 2018-06-29 2018-06-29 CHLOREXIDINE DIGLUCONATE POLYMER NANOPARTICLES

Publications (2)

Publication Number Publication Date
BR102018013490A2 true BR102018013490A2 (en) 2019-12-31
BR102018013490B1 BR102018013490B1 (en) 2023-10-03

Family

ID=69055588

Family Applications (1)

Application Number Title Priority Date Filing Date
BR102018013490-6A BR102018013490B1 (en) 2018-06-29 2018-06-29 CHLOREXIDINE DIGLUCONATE POLYMER NANOPARTICLES

Country Status (1)

Country Link
BR (1) BR102018013490B1 (en)

Also Published As

Publication number Publication date
BR102018013490B1 (en) 2023-10-03

Similar Documents

Publication Publication Date Title
ES2534843T3 (en) Antimicrobial and anti-acne formulations
ES2846854T3 (en) Antiseptic compositions comprising silver and menthol ions and uses thereof
JP5740393B2 (en) Composition suitable for topical treatment of fungal infections of the skin and nails
JPH03128316A (en) Liquid polymer composition and use thereof
BRPI0608690A2 (en) use of an antimicrobial composition
US20140234455A1 (en) Antimicrobial composition, method for its preparation and its use
BR112017012806B1 (en) soluble zinc polyphosphate complex and zinc polyphosphate production method
WO2016176749A1 (en) Method for obtaining a product for preventing and stopping caries lesions and remineralising teeth, and thus obtained product
BR112020010787A2 (en) use of dianhydroexitol in oral and dental care to reduce the development of bacterial strains
Soundarajan et al. Antibacterial and anti-inflammatory effects of a novel herb-mediated nanocomposite mouthwash in plaque-induced gingivitis: a randomized controlled trial
ES2711128T3 (en) Compositions and pharmaceutical formulations for topical application with astringent and antimicrobial effect
SE1650162A1 (en) Antimicrobial and cleansing composition comprising a polymeric biguanide, EDTA, and surfactants.
BR112017012807B1 (en) COMPOSITION FOR ORAL HYGIENE AND USE OF A SOLUBLE ZINC POLYPHOSPHATE COMPLEX IN THE PREPARATION OF THE SAME
BR102018013490A2 (en) chlorhexidine digluconate polymer nanoparticles
ES2601902T3 (en) Antibacterial or anti-acne formulations containing nicnic acid or a usnate and a metal salt
BR112017013014B1 (en) personal hygiene composition, and method for depositing zinc on an individual's skin and / or hair
ES2715281T3 (en) Treatment of microbial infections
Yu et al. Metronidazole and Ketoprofen-Loaded Mesoporous Magnesium Carbonate for Rapid Treatment of Acute Periodontitis In Vitro
BR112021013471A2 (en) COMPOSITIONS THAT GENERATE ELECTROCHEMICAL GAS TRANSMITTER AND BIMETAL CELLS FOR THE GENERATION OF GAS TRANSMITTERS
PT1642568E (en) Mouthwash
EP4076412B1 (en) Gold- and graphene-based mixture and compositions and use thereof
BR102021011811A2 (en) NANOTECHNOLOGY APPLIED TO TRICRESOL FORMALIN FOR DENTAL USE
BR102020002662A2 (en) ANACARDIC ACID NANOPARTICLES AND THEIR USE AS AN ANTISEPTIC AGENT IN ENDODONTIC DRESSING
BR102017011935A2 (en) anacardic acid nanoparticles extracted from cashew and its use as a bactericidal and larvicidal agent
JP2023165258A (en) Oral composition

Legal Events

Date Code Title Description
B03A Publication of a patent application or of a certificate of addition of invention [chapter 3.1 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 29/06/2018, OBSERVADAS AS CONDICOES LEGAIS