WO2023012616A1 - Composition pour la prévention et/ou le traitement de l'acné - Google Patents
Composition pour la prévention et/ou le traitement de l'acné Download PDFInfo
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- WO2023012616A1 WO2023012616A1 PCT/IB2022/057011 IB2022057011W WO2023012616A1 WO 2023012616 A1 WO2023012616 A1 WO 2023012616A1 IB 2022057011 W IB2022057011 W IB 2022057011W WO 2023012616 A1 WO2023012616 A1 WO 2023012616A1
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Classifications
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- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/40—Transferrins, e.g. lactoferrins, ovotransferrins
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/075—Ethers or acetals
- A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
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- A—HUMAN NECESSITIES
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- A61K31/6615—Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
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- 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
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/345—Alcohols containing more than one hydroxy group
-
- 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
- A61K8/60—Sugars; Derivatives thereof
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/008—Preparations for oily skin
Definitions
- the present invention relates to a composition for the prevention and/or treatment of acne. More particularly, the present invention relates to a composition for the prevention and/or treatment of acne, which comprises: lactoferricin; glycerophosphoinositol (GPI) or a salt thereof with an amino acid; and chlorphenesin or chlorphenesin carbamate; and its use in the therapeutic or cosmetic field .
- GPI glycerophosphoinositol
- Acne is a multi-factorial skin disease that causes acne lesions to form predominantly on the face and upper trunk. Acne is believed to develop due to the concomitant action of several factors, the main ones being: excessive sebum production (seborrhea) ; obstruction of the follicle with sebum and kerat inocytes (with the formation of comedones) ; colonization of follicles by Cutibacterium acnes (also known as Propionibacterium acnes) , a common human anaerobic bacterium; release of inflammatory mediators.
- Acne can be classified as non-inf lammatory , characterized only by comedones, or inflammatory, that is characterized by papules, pustules, nodules and/or cysts.
- comedones are colonized by bacteria, which transform the sebum into free fatty acids that irritate follicular epithelium and cause an inflammatory response to neutrophils and then to lymphocytes, which additional break down of the epithelium.
- the rupture of the inflamed follicle in the dermis causes an additional local inflammatory reaction with production of papules.
- the prevention and/or treatment of acne can be carried out topically or systemically (for example through oral administration of specific antibiotics) .
- the topical route involves local application of products that are able to reduce seborrhea, bacterial proliferation and/or follicular inflammation. These products need to be applied consistently and for a long time in order to obtain satisfactory and long-lasting results, so they must be characterized by high tolerability and ease of application.
- the Applicant therefore has faced the problem of finding a composition for topical application that performs a purifying, toning, soothing and sebumregulating action on the skin, particularly suitable for impure and acne-prone skin.
- compositions particularly suitable for topical application, which includes, as active principles, lactof erricin, glycerophosphoinositol (GPI) , or a salt thereof with an amino acid, and chlorphenesine or chlorphenesin carbamate, which perform in combination a strong sebum-regulating and anti-inflammatory action, with a significant synergistic effect, such as to make the composition particularly suitable for the prevention and/or treatment of acne, in particular acne vulgaris .
- active principles lactof erricin, glycerophosphoinositol (GPI) , or a salt thereof with an amino acid, and chlorphenesine or chlorphenesin carbamate, which perform in combination a strong sebum-regulating and anti-inflammatory action, with a significant synergistic effect, such as to make the composition particularly suitable for the prevention and/or treatment of acne, in particular acne vulgaris .
- the present invention therefore relates to a composition for topical application, which comprises: lactoferricin; glycerophosphoinositol (GPI) or a salt thereof with an amino acid; chlorphenesin or chlorphenesin carbamate.
- GPI glycerophosphoinositol
- the present invention relates to a composition for topical application, which comprises: lactoferricin; glycerophosphoinositol (GPI) or a salt thereof with an amino acid; chlorphenesin or chlorphenesin carbamate, for topical use in the prevention and/or treatment of acne.
- GPI glycerophosphoinositol
- the present invention relates to the cosmetic use of a composition as defined above by topical application on subjects affected by acne .
- lactoferricin it is meant peptides, also known as lactoferrin hydrolysates, which are obtained by digesting a lactoferrin with a proteolytic enzyme, generally pepsin.
- Lactoferrin is a glycoprotein with antimicrobial and iron-carrying action, naturally present in various biological fluids of mammals, in particular in milk, and in neutrophil granulocytes, which are immune cells with defense functions against bacterial and fungal infections.
- Lactoferrin can be of natural or synthetic origin, and can include different forms, both monomeric and oligomeric, possibly already bound to iron (ololactoferrin) or not bound to iron (apolactoferrin) .
- Bovine lactoferrin is generally used.
- lactoferrin hydrolyzates and their preparation are reported for example in the following articles: Wakabayashi H. , et al, Current Pharm. Design, 9 (16) (2003) , 1277-87; Theolier J. , et al, Dairy Science & Technology, 94 (2) (2013) , 181-193; Eliassen L.T. , et al, Anticancer Res. , 22 (5) (2002 Sep-Oct) , 2703-10.
- the peptides resulting from the proteolysis of lactoferrin generally have a number of amino acid units from 5 to 30, preferably from 5 to 15.
- lact of erricin has a molecular weight much lower than that of the starting protein, it contains the lactoferrin N-terminal sequence and maintains its biological activity, which is enhanced thanks to its greater bioavailability compared to the complete protein .
- lactof erricin is present in the composition according to the present invention in an amount from 0.05% to 5.0% by weight, preferably from 0.1% to 3.0% by weight, with respect to the total weight of the composition.
- glycerophosphoinositol (CAS Registry No. 129830-95-1) has the following formula:
- GPI and its salts are ubiquitous molecules that can be detected both within cells and in the extracellular space. They are able to modulate and regulate inactivation of phospholipase enzyme (cytosolic A2 - CPLA2) involved in initiation of the inflammatory cascade.
- phospholipase enzyme cytosolic A2 - CPLA2
- the GPI choline or lysine salt is a product of plant origin that inhibits release of arachidonic acid induced by activation of phospholipase, effectively regulating the inflammatory cascade.
- the level at which the effect of GPI is expressed, in terms of mechanism of action, is "upstream" with respect to inhibition of cyclooxygenase and lipoxygenase, activity typically exercised by nonsteroidal anti-inflammatory drugs (NSAIDs) .
- NSAIDs nonsteroidal anti-inflammatory drugs
- GPI is able to counteract pro-inflammatory and pro-thrombotic responses induced by a bacterial lipopolysaccharide in human blood monocytes, thus leading to a decrease in production of inflammatory promoters, effectively reducing transcription of inflammatory genes and, more generally, limiting the inflammatory process (see M. Vessichelli et al, Journal of Biological Chemistry, Volume 292 Issue 31, 12828-12841 (March 2017) ) .
- the GPI or its salt with amino acid is present in the composition according to the present invention in an amount from 0.05% to 4.0% by weight, preferably from 0.1% to 2.0% by weight, compared to the total weight of the composition.
- the weight ratio between lactof erricin and GPI is from 0.1 to 5, preferably from 0.5 to 3.
- Chlorphenesin (CAS Registry No. 104-29-0) and chlorphenesin carbamate (CAS Registry No. 886-74-8) are active principles known in the pharmacological field (muscle relaxants) which also perform a cosmetic function as preservatives and biocides with antimicrobial and antifungal activities.
- chlorphenesin or chlorphenesin carbamate is present in the composition according to the present invention in an amount from 0.05% to 4.0% by weight, more preferably from 0.1% to 2.0% by weight, with respect to the total weight of the composition.
- the composition for topical application according to the present invention further comprises antarticin, i.e. a glycoprotein obtained by fermentation of marine bacteria Pseudoal teromonas . It is an active principle used in cosmetics, with regenerating, restructuring and protective properties. It also prevents skin dryness, thanks to adhesive capacities that reduce cellular water loss through evapotranspiration, keeping the skin hydrated. Antarcticine also stimulates the production of collagen and elastin.
- antarticin is present in the composition according to the present invention in an amount from 0.05% to 6.0% by weight, preferably from 0.1% to 3.0% by weight, with respect to the total weight of the composition.
- the composition for topical application according to the present invention further comprises a Lilac (Syringa vulgaris) extract, which is rich in phenylpropanoid glycosides (PPGs) , which are water-soluble derivatives of phenylpropanoids (PP) , a large group of natural polyphenols widely distributed in the plant kingdom.
- PPGs phenylpropanoid glycosides
- PP phenylpropanoids
- Verbascoside also known as acteoside, is its main constituent. It is a hydrophilic molecule having various pharmacological activities, including antioxidant, antimicrobial, antiinflammatory and neuroprotect ive .
- the anti-inflammatory effects of verbascoside are mainly exerted by inhibiting release of histamine and arachidonic acid from mast cells.
- the inhibitory activity depends on the presence of Ca 2+ ions and correlates with the inhibition of phospholipase Az.
- verbascoside mainly inhibits nitric oxide (NO) , tumor necrosis factor (TNF- a) and interleukin 12 (IL-12) production.
- the Lilac (Syringa vulgaris) extract is present in the composition according to the present invention in an amount from 0.01% to 4.0% by weight, preferably from 0.02% to 2.0% by weight, with respect to the overall weight of the composition.
- the composition for topical application according to the present invention further comprises lactobionic acid (CAS Registry No. 96-82-2) , which performs a purifying action, exerting a delicate exfoliating action, which helps to eliminate dead cells from the stratum corneum, promoting cell renewal and improving skin firmness.
- lactobionic acid is present in the composition according to the present invention in an amount from 0.05% to 4.0% by weight, preferably from 0.1% to 2.0% by weight, with respect to the total weight of the composition.
- the composition for topical application according to the present invention further comprises at least one amino acid selected from proline, alanine, glycine and serine. These are amino acids naturally present in the skin, useful for maintaining both optimal levels of elastin and natural protective barrier function for the epidermal stratum corneum .
- said at least one amino acid is present in the composition according to the present invention in an amount from 0.01% to 2.0% by weight, preferably from 0.02% to 1.0% by weight, with respect to the total weight of the composition.
- composition for topical application according to the present invention further comprises ethylhexylglycerin, which has a preservative, antibacterial and emollient action.
- ethylhexylglycerin is present in the composition according to the present invention in an amount from 0.01% to 1.5% by weight, preferably from 0.05% to 1.0% by weight, with respect to the total weight of the composition.
- composition for topical application comprises, in addition to the aforementioned active principles, at least one physiologically acceptable excipient. This in order to obtain a product suitable for skin application, in particular in the form of gel, emulsion, lotion, cream, paste .
- composition according to the present invention can comprise ingredients commonly used in the cosmetic or dermatological field, such as for example: abrasive agents in particle form, viscosity regulators, water, water-soluble solvents (for example glycerol) , gelling agents, preservatives, emulsifiers, humectants, emollients, stabilizers, pH regulators, sun filters, etc.
- abrasive agents in particle form such as for example: abrasive agents in particle form, viscosity regulators, water, water-soluble solvents (for example glycerol) , gelling agents, preservatives, emulsifiers, humectants, emollients, stabilizers, pH regulators, sun filters, etc.
- abrasive agents in particle form such as for example: abrasive agents in particle form, viscosity regulators, water, water-soluble solvents (for example glycerol) , gelling agents, preservative
- lactof erricin Example 1
- GPI Example 2
- chlorphenesin Example 3
- the test was conducted on human sebocytes Pci- SEB, using good practices for cell cultivation.
- the cells were thawed, propagated in a specific basal medium and incubated under standard culture conditions (37°C, 5% CO2) with the addition of the relevant active principle ( lactof erricin, GPI, chlorphenesin, or a mixture of the three) or in the absence of active principles (control) .
- the relevant active principle lactof erricin, GPI, chlorphenesin, or a mixture of the three
- control control
- the cells When the cells reached a desired confluence, they were subjected to trypsinization and counted for seeding and for experiment setup. After 3-4 days, specific supplements were added to the growth medium to favor sebocyte maturation and lipid accumulation.
- fat-soluble Oil Red dye was used, which penetrates by diffusion into the cells and reaches the lipid drops, coloring them.
- the cells were washed twice with phosphate buffered saline (PBS) and fixed by two passes in a 10% formaldehyde solution.
- the cells fixed in monolayer were then washed twice with a 60% isopropanol solution, and the monolayers were left in the air until complete evaporation of the solvent.
- the cells were then stained with an Oil Red solution (2 mg/ml) , excess dye was removed and the cells washed several times with water. Isopropanol was then added to each well, which is able to break up drops by solubilizing the contained lipids.
- the clear solution thus obtained was inserted into a spectrophotometer to measure absorbance at 540 nm.
- the evaluation of lipid accumulation and therefore of active principle efficacy is based on comparison between absorbance of the treated sample and absorbance of the control not treated with the active principle (set equal to 100) .
- the absorbance measured at 450 nm is directly proportional to the amount of lipids present in the cells. The values are expressed as the arithmetic mean over three samples.
- Example 1 lactof erricin, obtained by hydrolysis of bovine lactoferrin with pepsin (aqueous solution at 0.1% by weight ) ;
- Example 2 GPI lysine salt (0.1% by weight aqueous solution) ;
- Example 3 chlorphenesin (aqueous solution at 0.1% by weight) .
- GPI lysine salt 0.017% by weight
- chlorphenesin 0.017% by weight
- with an overall concentration of 0.1% by weight Example 4 .
- lact of erricin (Example 1) and GPI (Example 2) have a sebum-regulating effect per se, while for chlorphenesin (Example 3) this effect is insignificant.
- the value of the % variation measured on the combination of the three active principles is -24.38%, i.e. more than double the expected value based on the activity of the individual components. This is an evident synergistic effect.
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Abstract
L'invention concerne une composition, en particulier appropriée pour une application topique, qui comprend, en tant que principes actifs, de la lactoferrine, du glycérophosphoinositol (OPT), ou un sel de celui-ci avec un acide aminé, et de la chlorphénésine ou du carbamate de chlorphénésine, qui mettent en oeuvre en combinaison une action marquée de régulation de sébum et anti-inflammatoire, avec un effet synergique significatif. La composition est particulièrement appropriée pour la prévention et/ou le traitement de l'acné, en particulier de l'acné simple.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP22758270.7A EP4380599A1 (fr) | 2021-08-03 | 2022-07-28 | Composition pour la prévention et/ou le traitement de l'acné |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT102021000020975 | 2021-08-03 | ||
| IT102021000020975A IT202100020975A1 (it) | 2021-08-03 | 2021-08-03 | Composizione per la prevenzione e/o il trattamento dell'acne. |
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| Publication Number | Publication Date |
|---|---|
| WO2023012616A1 true WO2023012616A1 (fr) | 2023-02-09 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/IB2022/057011 WO2023012616A1 (fr) | 2021-08-03 | 2022-07-28 | Composition pour la prévention et/ou le traitement de l'acné |
Country Status (3)
| Country | Link |
|---|---|
| EP (1) | EP4380599A1 (fr) |
| IT (1) | IT202100020975A1 (fr) |
| WO (1) | WO2023012616A1 (fr) |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107049890A (zh) * | 2017-06-27 | 2017-08-18 | 广东芭薇生物科技股份有限公司 | 一种具有舒缓抗粉刺功效的护肤品 |
| US20170304409A1 (en) * | 2014-09-24 | 2017-10-26 | ISTITUTO PROFILATTICO E FARMACEUTICO CANDIOLI & C. SPA in abbreviated form CANDIOLI FARMACEUTICI | Compositions useful for the prevention and/or treatment of infections and inflammations |
| US20190099340A1 (en) * | 2017-09-29 | 2019-04-04 | Rodan & Fields, Llc | Retinaldehyde containing compositions and methods of use |
| US20200375870A1 (en) * | 2016-02-12 | 2020-12-03 | Rodan & Fields, Llc | Moisturizing compositions and uses thereof |
| CN112587446A (zh) * | 2020-12-31 | 2021-04-02 | 广州膜束生物科技有限公司 | 一种治疗痤疮的组合物及其制备方法和应用 |
-
2021
- 2021-08-03 IT IT102021000020975A patent/IT202100020975A1/it unknown
-
2022
- 2022-07-28 EP EP22758270.7A patent/EP4380599A1/fr active Pending
- 2022-07-28 WO PCT/IB2022/057011 patent/WO2023012616A1/fr unknown
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170304409A1 (en) * | 2014-09-24 | 2017-10-26 | ISTITUTO PROFILATTICO E FARMACEUTICO CANDIOLI & C. SPA in abbreviated form CANDIOLI FARMACEUTICI | Compositions useful for the prevention and/or treatment of infections and inflammations |
| US20200375870A1 (en) * | 2016-02-12 | 2020-12-03 | Rodan & Fields, Llc | Moisturizing compositions and uses thereof |
| CN107049890A (zh) * | 2017-06-27 | 2017-08-18 | 广东芭薇生物科技股份有限公司 | 一种具有舒缓抗粉刺功效的护肤品 |
| US20190099340A1 (en) * | 2017-09-29 | 2019-04-04 | Rodan & Fields, Llc | Retinaldehyde containing compositions and methods of use |
| CN112587446A (zh) * | 2020-12-31 | 2021-04-02 | 广州膜束生物科技有限公司 | 一种治疗痤疮的组合物及其制备方法和应用 |
Non-Patent Citations (3)
| Title |
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| "Ultra Protection Anti-Aging Moisturizer SPF 15 PA++", GNPD, 1 October 2010 (2010-10-01), XP002754290 * |
| DATABASE GNPD [online] MINTEL; 13 May 2020 (2020-05-13), ANONYMOUS: "Repair Cream", XP055905319, retrieved from https://www.gnpd.com/sinatra/recordpage/7445307/ Database accession no. 7445307 * |
| DATABASE GNPD [online] MINTEL; 20 July 2021 (2021-07-20), ANONYMOUS: "Alpha-Arbutin Brightening Micro Essence Emulsion", XP055905323, retrieved from https://www.gnpd.com/sinatra/recordpage/8827993/ Database accession no. 8827993 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP4380599A1 (fr) | 2024-06-12 |
| IT202100020975A1 (it) | 2023-02-03 |
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