WO2018000060A1

WO2018000060A1 - Anti-acne sunscreen composition

Info

Publication number: WO2018000060A1
Application number: PCT/BR2016/050152
Authority: WO
Inventors: Marina Castello ESPÓSITO; Tássia HANASHIRO
Original assignee: LOreal SA
Current assignee: LOreal SA
Priority date: 2016-06-30
Filing date: 2016-06-30
Publication date: 2018-01-04
Anticipated expiration: 2018-12-30
Also published as: BR112018077287A2; BR112018077287B1

Abstract

The present invention relates to an anti-acne sunscreen composition comprising a specific combination of components, namely a mixture of drometrizole trisiloxane and terephthalylidene dicamphor sulfonic acid as sunscreens, a mixture of salicylic acid and lipohydro acid as keratolytic agents, niacinamide as anti-inflammatory agent and a mixtrue of phyto-active substances comprising Cinnamomum cassia bart extract, Zingiber officinale (ginger) root extract and Sanguisorba officinalis root extrat as a sebum regulator, and its uses.

Description

ANTI-ACNE SUNSCREEN COMPOSITION

FIELD OF THE INVENTION

The present invention is directed to a sunscreen composition with antiacne effect comprising a specific combination of components and its uses.

BACKGROUND OF THE INVENTION

The photoprotection of keratinous substrates, including both skin and hair, is considered by many to be necessary in order to facilitate protection from sun- damage, sunburn, photo-aging, as well as to decrease the chances of skin cancer development caused by exposure to ultraviolet ("UV") radiation. There are typically two types of UV-A/UV-B sunscreen compositions used to accomplish photoprotection, namely, inorganic UV filters and organic UV filters.

Inorganic UV filters such as titanium dioxide and zinc oxide are typically employed in large quantities in order to ensure proper coverage/maximum protection over the surface onto which they are applied. As a result, inorganic UV filters have a tendency to cause skin to which they are applied to feel dry, and further impart an undesirable color onto the treated surface (naturally white, but sometimes colored for aesthetic purposes with varying degrees of aesthetic success).

Further, UV filters may either protect against UV-A radiation (longwave), UV-B radiation (shortwave), or both. In the past, it was commonly held that protection against UV-B radiation was the primary or even sole consideration in sun- protection. However, more recent research has revealed that exposure to UV-A radiation may also be dangerous and lead to undesirable effects. As such, the current trend in sun-protection endeavors is typically to protect against both UV-A and UV-B in a single composition, and to increase both the SPF and the UV-A ratings of the composition.

Sunscreens are treated as over-the-counter ("OTC") products in many jurisdictions, including in the United States of America ("US"). As a result of the classification of sunscreens as OTC products, in the US, sunscreen is regulated by the U.S. Food and Drug Administration ("FDA"), which, due to regulatory issues and safety concerns, has limited the active ingredients of sunscreen compositions, such as UV filters, substantially. Thus, there are limited UV filters available to achieve high efficacy with respect to both SPF and UV-A protection. Most commonly, these UV filters are regarded to include avobenzone, oxybenzone, octisalate, octocrylene, and homosalate. With regard to oxybenzone, there is currently a growing consumer preference to reduce or eliminate this UV filter from sun-protectant compositions since there is some evidence, largely arising from correlational studies and in-vitro experiments that it may cause safety concerns for example being linked to increased risks of malignant melanoma, a rarer but more deadly form of skin cancer. However, it is very challenging to achieve both high SPF and high UV-A protection in a worldwide composition in the absence of oxybenzone.

US Patent No. 9,050,475 B2 (the '475 Patent) discloses methods and compositions for the protection of an object from UV light, which includes multiple photostabilizers but which is essentially free of oxybenzone and oxtinoxate. The '475 Patent claims to enhance the SPF by adding antioxidants, photostabilizers and/or film forms. However, the '475 Patent does not claim any defined level of UV-A protection. In particular, the '475 Patent describes the photostabilization of avobenzone, which is a UV-A filter and which is not itself photostable, however it is not believed that the stabilization of avobenzone, by itself, is capable of enabling a sufficiently high UV-A protection in a composition for current consumer and health requirements and desires.

Therefore, it is desired a sunscreen composition capable of not only of a defined high SPF rating, but also providing a defined high UV-A rating, which has eliminated oxybenzone content and, additionally, it is desired that this composition presents oil control and anti-acne effect, for the following reasons.

It is known that the main determinant factor of skin oiliness is the amount of secretion of the sebaceous glands. The sebaceous glands are formed by cells of pyknotic nucleus and located in the dermis. Said cells discharge its lipid content in the hair follicles on the skin surface. This content is referred to as "sebum" or tallow, which is therefore a holocrine secretion, comprising 92-100% of lipids (EBLING & ROOK, 1979).

The sebaceous secretion is composed of several types of fats: triglycerides, free fatty acids, esterified waxes, squalene and cholesterol.

There is a greater number of glands in some areas of the skin, which are more voluminous. These areas are the "T-zone" (which includes the forehead, nose and chin), back, chest, ears, armpits, genitals and scalp.

Oily skin is shiny, thick, having dilated infundibulum of the pilo- sebaceous follicle (pore), especially in seborrheic regions, and tendency to acne development (CUNLIFFE & COTTERILL, 1975). This clinical aspect is aesthetically unpleasant and this implies the need to develop specific products for oily skin.

Acne is a very common dermatological problem that affects a portion of the world population, mainly in the age group 1 1 -25 years. It is characterized by comedones, papules, pustules, cysts or scars, located mainly in "seborrheic areas" - body regions with the highest amount of sebaceous glands - facial central area, back and chest (VIGLIOGLIA & RUBIN, 1991 ).

In the physiopathology it is observed as important elements the increase of the sebaceous secretion of the gland, follicular hyperkeratosis with consequent obstruction, causing accumulation of keratin and sebum in the follicle and bacterial colonization besides inflammation (SAMPAIO & RIVITTI, 2000).

The origin is not completely known, however it is known that genetic aspects and emotional, immunological, hormonal, environmental factors, besides the modification of the local flora, with increased bacterial population, specially Propioniumbacterium acne, are involved in the genesis, or worsening of the condition.

Products for oily skin should have the purpose of regulating sebaceous secretion without deeply degrease it, since it unleashes the rebound effect, with increased fat production. They may also act by reducing the bacterial flora and hyperkeratosis (CLAR, 1994). The most suitable carriers are oil-water emulsions and gels, which should not contain comedogenic or acnegenic ingredients.

Therefore, it is desired a sunscreen composition with oil control and anti-acne effect.

The inventors succeeded to overcome the problems of the prior art and surprisingly reveal a sunscreen composition with anti-acne effect also presenting oil control.

SUMMARY OF THE INVENTION

The present invention relates to a sunscreen composition with anti-acne effect comprising a specific combination of components such as sunscreens, keratolytic, anti-inflammatory agents and a sebum regulator and its uses.

The composition of the invention presents a dry touch, effective oil control without overdrying, mattifying effect, UV-protection and anti-acne effect.

DETAILED DESCRIPTION OF THE INVENTION

The anti-acne sunscreen composition of the present invention comprises: (a) a mixture of drometrizole trisiloxane and terephthalylidene dicamphor sulfonic acid as sunscreen agents;

(b) a mixture of salycilic acid and lipohydroxy acid (LHA) as kerato lytic agents;

(c) Niacinamide as anti-inflammatory agent; and

(d) a mixture of phyto-active substances comprising Cinnamomum cassia bark extract, Zingiber officinale (ginger) root extract and Sanguisorba officinalis root extract as a sebum regulator.

As a preferred embodiment, the LHA of the invention may be the capryloyl salicylic acid.

According to the invention, the concentration of the mixture of sunscreen agents may be between 2% and 8%, preferably between 3% and 7% by weight with respect to the total weight of the composition.

The keratolytic agents may be present at a concentration of 0.1 % to 2%, preferably of 0.5% to 1 .2% by weight with respect to the total weight of the composition.

The anti-inflammatory agent may be present at a concentration of 0.1 % to 3%, preferably of 0.5% to 2.5% by weight with respect to the total weight of the composition.

The sebum regulator may be present at a concentration of 0.05% to

2.5%, preferably of 0.1 % to 2% by weight with respect to the total weight of the composition.

The composition of the invention may further comprise any usual cosmetically acceptable ingredient, which may be chosen especially from such as additional sunscreens, perfume/fragrance, polymers, preserving agents, solvents, actives, surfactants, fat materials, vitamins and mixtures thereof.

The optional additional ingredients may represent from 84.5% to 97.75%, preferably, from 87.3% to 95.9% by weight with respect to the total weight of the composition.

The actives drometrizole trisiloxane and terephthalylidene dicamphor sulfonic acid are preferably those known as Mexoryl™ XL and Mexoryl™ SX, respectively.

The mixture of phyto-active substances present in the composition of the invention is preferably the one known as Sebustop^® up. Needless to say, a person skilled in the art will take care to select the optional additional ingredients and/or the amount thereof such that the advantageous properties of the composition according to the invention are not, or are not substantially, adversely affected by the envisaged addition.

Non-limiting examples of additional sunscreen agents which can be used in accordance with the invention include ethylhexyl triazone, octocrylene, butyl methoxydibenzoylmethane, silica, titanium dioxide, bis-ethylhexyloxyphenol methoxyphenyl triazine, methylene bis-benzotriazolyl tetramethylbutylphenol, polyglyceryl-10 laurate and mixtures thereof.

Exemplary polymers include, but are not limited to, xanthan gum, Zea mays (corn) starch, ammonium polyacryloyldimethyl taurate, poly C10-30 alkyl acrylate and mixtures thereof.

Non-limiting examples of preserving agents which can be used in accordance with the invention include salicylic acid, phenoxyethanol and mixtures thereof.

Suitable solvents include, but are not limited to water, C12-C15 alkyl benzoate, alcohols, caprylyl glycol and mixtures thereof.

Suitable additional actives include, but are not limited to, disodium EDTA, triethanolamine, capryloyl salicylic acid, sodium hyaluronate and mixtures thereof.

Non-limiting examples of surfactants suitable for the composition of the present invention are behenyl alcohol, glyceryl stearate, disodium ethylene dicocamide PEG-15 disulfate, glyceryl stearate citrate and mixtures thereof.

Exemplary fat materials include, but are not limited to, isopropyl lauroyl sarcosinate, diisopropyl sebacate, cetyl alcohol and mixtures thereof.

The pH of the anti-acne sunscreen composition of the invention is preferably within the range of 5 to 6, more preferably, of 5.5.

The density of the anti-acne sunscreen composition of the invention is preferably within the range of 0.8 g/cm³ to 1 .2 g/cm³, more preferably, of 1 .02 g/cm³.

Furthermore, the anti-acne sunscreen composition of the present invention may preferably present a Sun Factor Protection 30 and a flash point range between 50-60 ^QC. Also, the composition of the invention is not a rinse-off composition. The anti-acne sunscreen composition of the invention is for topical application on human skin, preferably the face. Also, the composition of the invention presents a mattifying effect.

The anti-acne sunscreen composition of the invention is in the form of a cream.

According to a preferred embodiment, the composition of the invention is hypoallergenic. "Hypoallergenic" as used herein, refers to a composition with reduced allergenic potential.

The anti-acne sunscreen composition of the invention can be used as a daily product for the skin (including for the skin of acne patients). Therefore, the composition of the invention may be used as sunscreen and anti-acne.

The anti-acne sunscreen composition of the present invention is a non- comedogenic composition.

In a preferred embodiment, the composition of the invention is for the manufacture of a medicament for preventing or treating acne.

The anti-acne sunscreen composition of the invention is particularly suitable in the prevention or treatment of other forms of acne, such as acne vulgaris, acne conglobata, acne medicamentosa, acne necrotica, acne neonatorum, polymorphous acne, nodulocystic acne, acne keloid, premenstrual acne, occupational acne, acne rosacea, senile acne and solar acne.

By way of non-limiting illustration, the invention will now be described with reference to the following examples.

EXAMPLES

Examples 1 and 2

A suitable composition of the invention is as follows

Example 1 Example 2

INCI US Name Type

Concentration Concentration et ylhexyl triazone sunscreen 2 2

fragrance perfume 0.5 -- octocrylene sunscreen 4 2.5 xanthan gum polymer 0.25 0.25 preserving

salycilic acid agent/keratolytic 0.5 0.5

agent

Zingiber officinale (ginger) root extract plant extract/sebum 0.15 2 Example 1 Example 2

INCI US Name Type

Concentration Concentration

(and) Sanguisorba officinalis root regulator

extract (and) Cinnamomum cassia

bark extract

drometrizole trisiloxane sunscreen 1 0.5

water solvent 1 1 disodium EDTA active 0.1 0.1 behenyl alcohol (and) glyceryl stearate

(and) disodium ethylene dicocamide

surfactant 3 3 PEG-15 disulfate (and) glyceryl

stearate citrate

isopropyl lauroyl sarcosinate fat material 2.5 2.5

diisopropyl sebacate fat material 5 5 triethanolamine active 1 .2 1 .2 butyl methoxydibenzoylmethane sunscreen 3.5 3

C12-C15 alkyl benzoate solvent 2.5 2.5

Silica (and) titanium dioxide sunscreen 6.0 6.0 terephthalylidene dicamphor sulfonic

sunscreen 3.0 3.0 acid

Vitamin/ anti¬

Niacinamide 2.0 2.0

inflammatory agent

capryloyl salicylic acid keratolytic agent 0.3 0.3

cetyl alcohol fat material 0.5 0.5 alcohol solvent 5.0 5.0 phenoxyethanol Preserving agent 0.6 0.6 caprylyl glycol solvent 0.4 0.4

Zea mays (corn) starch polymer 2.0 2.0 bis-ethylhexyloxyphenol

sunscreen 0.5 -- methoxyphenyl triazine

sodium hyaluronate active 0.04 0.04 methylene bis-benzotriazolyl

tetramethyl butylphenol (and) sunscreen 2.0 2.0

polyglyceryl-10 laurate

ammonium polyacryloyldimethyl

polymer 0.7 0.7 taurate Example 1 Example 2

INCI US Name Type

Concentration Concentration water solvent 47.76 49.41 poly C_{1 0}-3o alkyl acrylate polymer 2.0 2.0

Total weight % 100 100

Example 3

A study was conducted to evaluate the Sun Protection Factor (SPF) of the composition of Example 1 , applied in standardized quantity on defined zones, on healthy adult subject's back, followed by exposure to UV according to the ISO/EN 24444 Cosmetics Sun protection test methods - In vivo determination of the Sun Protection Factor (SPF) (2010).

^*Confidence Interval.

The composition of Example 1 has an average SPF of 37.3.

Example 4

A test was conducted in order to evaluate the cutaneous acceptability and efficacy of the composition of Example 1 on adult subjects with sensitive skin and assess its cosmetic qualities, after application for 28 consecutive days under the normal conditions of use.

The composition was applied on face 15 minutes before sun exposure and re-applied every 2 hours until no sun exposure.

The study was carried out on the composition of the invention which safety have been assured by a toxicologist, with the aim to further confirm its safety which will be used by a large number of consumers under normal and reasonably foreseeable use conditions.

The majority of the subjects appreciated the composition of the invention (example 1 ), and it is possible to conclude that the composition of the present invention is well tolerated on cutaneous level after 28 days of multiple application, daily used by 54 adult subjects. It is listed below the results related to the time of measure:

I Timmediate-Efficacy

The skin is with a mattifying effect. The skin looks less shiny and oily. The skin complexion looks more radiant, feels purified, healthier and looks smoother.

T1 week Efficacy

The skin is with a mattifying effect. The skin is with a mattifying effect even in hot and humid climates. The skin looks less shiny and oily. The pores are less visible. The skin complexion looks more radiant and skin is soothed. The skin feels purified and healthier, looks smoother and better.

T4 week Cosmeticity

The skin is with a mattifying effect. The skin is with a mattifying effect even in hot and humid climates. The skin looks less shiny and oily. Imperfections looks reduced day by day. The pimples looks reduced and pores are less visible.

The skin complexion looks more radiant. The skin is soothed, feels purified and healthier. The skin looks smoother and the quality of the skin looks better. The texture of the product is light and is not oily when touching. The product provides a velvety touch, quickly absorbed, provides a dry touch and doesn't leave the white residue and doesn't leave noodles.

T4 week Acceptability

The product is gentle for the skin, doesn't leave the skin sticky, shiny, and is suitable for the subject's skin type.

Globally, 97.34% subjects found the product to be pleasant. 86.79% subject would like to continue using the product.

Claims

WO 2018/000060 -j _Q PCT/BR2016/050152

SET OF CLAIMS

1 . Anti-acne sunscreen composition comprising:

(a) a mixture of drometrizole trisiloxane and terephthalylidene dicamphor sulfonic acid as sunscreen agents;

(c) Niacinamide as anti-inflammatory agent; and

2. Composition, according to claim 1 , wherein the LHA is capryloyl salicylic acid.

3. Composition, according to one of the preceding claims, wherein the amount of the mixture of sunscreen agents is from 2% to 8% by weight of the total composition.

4. Composition, according to one of the preceding claims, wherein the amount of the mixture of keratolytic agents is from 0.1 % to 2% by weight of the total composition.

5. Composition, according to one of the preceding claims, wherein the amount of Niacinamide is from 0.1 % to 3% by weight of the total composition.

6. Composition, according to one of the preceding claims, wherein the amount of the mixture of phyto-active substances is from 0.05% to 2.5% by weight of the total composition.

7. Composition, according to one of the preceding claims, wherein it further comprises cosmetically acceptable ingredients selected from additional sunscreens, perfume/fragrance, polymers, preserving agents, solvents, actives, surfactants, fat materials, vitamins and mixtures thereof.

8. Composition, according to claim 7, wherein the cosmetically acceptable ingredients represent from 84.5% to 97.75% by weight with respect to the total weight of the composition.

9. Composition, according to one of the preceding claims, wherein it presents a Sun Factor Protection 30.

10. Composition, according to one of the preceding claims, wherein it is in the form of a cream. wherein it is as sunscreen and anti-acne.

12. Use, according to claim 1 1 , wherein it is for the manufacture of a medicament for preventing or treating acne.

13. Use, according to one of claims 1 1 to 12, wherein the composition is in the form of a cream.

14. Use, according to one of claims 1 1 to 1 3, wherein the composition is a non-comedogenic composition.

15. Use, according to one of claims 1 1 to 14, wherein the composition presents mattifying effect, effective oil control and anti-acne effect.