Cosmetic anti-blemish composition, use of the composition and method for anti-blemish treatment

Abstract

The present invention relates to cosmetic anti-blemish compositions, in the form of a serum, which are particularly useful in treatments for restoring facial firmness and elasticity (loss of tone).

Claims

1. An anti-aging cosmetic composition, wherein the composition is a serum comprising: a) at least one antioxidant selected from the group consisting of butylated hydroxytoluene (BHT), tocopherol acetate, natural plant extracts, and mixtures thereof; b) at least one humectant selected from the group consisting of glycerol, glycols, sorbitol, mannitol, and mixtures thereof; c) a combination of Hymenaea courbaril extract and a mixture of unfermented Paeonia albiflora root extract/phenoxyethanol/ethylhexylglycerin; d) at least one emulsifier selected from the group consisting of polyethylene glycol (PEG)-40 hydrogenated castor oil, glyceryl citrate, potassium cetyl phosphate, PEG-100, acrylates, xanthan gum, cetearyl alcohol, mixture of glyceryl stearate/PEG-100, and mixtures thereof; and e) cosmetically acceptable carriers.

2. The composition of claim 1, wherein the at least one antioxidant is butylated hydroxytoluene (BHT).

3. The composition of claim 1, wherein the at least one humectant is glycerol.

4. The composition of claim 1, wherein the at least one emulsifier is PEG-40 hydrogenated castor oil.

5. The composition of claim 1, further comprising a viscosity donor selected from xanthan gum, carbopol, a mixture of hydroethylacrylate/sodium acryloyldimethyltaurate copolymer/squalane/polysorbate 60, and mixtures thereof.

6. The composition of claim 5, wherein the viscosity donor is xanthan gum.

Description

BRIEF DESCRIPTION OF THE FIGURES

(1) The graph of FIG. 1 shows the mean values of the Ur/Ue parameter obtained throughout the study (Mean±SD, n=26).

(2) The graph of FIG. 2 shows the mean values of the Ur/Uf parameter obtained throughout the study (Mean±SD, n=26).

(3) The graph of FIG. 3 shows mean values of collagen intensity, I340/I295 versus time. Mean±standard deviation, n=20.

DESCRIPTION OF THE INVENTION

(4) The present invention relates to anti-aging cosmetic compositions in the form of a serum, which are particularly useful in a treatment to restore facial firmness and elasticity (sagging).

(5) Surprisingly, the compositions according to the present invention exhibit effective results: Immediately: immediate lifting effect; After 7 days: they enhance collagen production by up to 8×2 and restore the facial contour; After 15 days: they smooth wrinkles, revitalize and lighten the skin; After 30 days: they restore firmness.

(6) “Serum”, in the context of the present invention, means compositions having a distinct texture, characterized by lightness during application, fluid appearance and by comprising higher concentrations of active ingredients than common cosmetic treatments, forming a polymeric film on the skin surface, which when dried promotes an immediate tensor effect facilitating permeation of active ingredients and an interaction with the skin to stimulate and protect its main mechanisms, cells and fibers that guarantee skin support, firmness and elasticity.

(7) The anti-aging cosmetic compositions according to the present invention are provided in the form of a serum comprising:

(8) a) at least one antioxidant;

(9) b) at least one humectant;

(10) c) at least one active ingredient;

(11) d) at least one emulsifier; and

(12) e) cosmetically acceptable carriers.

(13) The antioxidant is selected from the group consisting of butylated hydroxytoluene (BHT), tocopherol acetate or natural plant extracts, or mixtures thereof, particularly butylated hydroxytoluene (BHT);

(14) The humectant is selected from the group consisting of glycerol, glycols, sorbitol, mannitol or mixtures thereof, particularly glycerol;

(15) The active ingredient is selected from the group consisting of a mixture of Paeonia albiflora root extract/phenoxyethanol/ethyl hexylglycerine, a mixture of Secale Cereale extract/penethylene glycol, Avena Sativa extract, Hymenaea courbaril extract, Schinus terebinthifolius extract, a mixture of Casearia sylvestris/silica, acetyl tetrapeptide-2, a mixture of sodium cocoyl amino acids/sarcosine/potassium aspartate/magnesium aspartate/propylene glycol, Cichorium intybus extract, or mixtures thereof, particularly the mixture of Paeonia albiflora root extract/phenoxyethanol/ethylhexylglycerin, mixture of Secale Cereale extract/penethylene glycol, Avena Sativa extract, Hymenaea courbaril extract, Schinus terebinthifolius extract, a mixture of Casearia sylvestris/silica, or mixtures thereof;

(16) The emulsifier is selected from the group consisting of PEG-40 hydrogenated castor oil, glyceryl citrate, potassium cetyl phosphate, PEG-100, acrylates, xanthan gum, cetearyl alcohol, mixture of glyceryl stearate/PEG-100, or mixtures thereof, particularly PEG-40 hydrogenated castor oil.

(17) Cosmetically acceptable carriers may be selected from compounds known in the art.

(18) Exemplary carriers are: solvents, preservatives (such as phenoxyethanol and iodopropynyl butylcarbamate), perfumes/fragrances (such as pataqueira essential oil), polymer neutralizers, chelating agents (such as disodium EDTA), pH adjusting agents, among others.

(19) The compositions according to the present invention may further comprise a viscosity donor selected from xanthan gum, carbopol, a mixture of hydroethylacrylate/sodium acryloyldimethyltaurate copolymer/squalane/polysorbate 60, or mixtures thereof. In particular, the viscosity donor is xanthan gum.

(20) The cosmetic compositions according to the present invention act on 11 major mechanisms responsible for restoring skin firmness and elasticity, acting on 11 mechanisms:

(21) 1. Increase in collagen production by up to 8×*;

(22) 2. Formation of a tensor film on the surface of the skin;

(23) 3. Reinforcement of the skin supporting tissue;

(24) 4. Restores natural hydration;

(25) 5. Elastin stimulation;

(26) 6. Hyaluronic acid stimulation;

(27) 7. Cell renewal;

(28) 8. Elastin protection;

(29) 9. Collagen protection;

(30) 10. Tensor effect on the deeper layers of the skin; and

(31) 11. Protection of the supporting fibers.

(32) Another object of the present invention consists of the use of the cosmetic compositions in an anti-aging treatment, particularly to restore firmness and elasticity of facial skin.

(33) Still another object of the present invention is an anti-aging treatment method as well as a method for restoring firmness and elasticity of facial skin, which comprises applying a cosmetically effective amount of the composition according to the present invention at least once a day.

(34) The following examples, without any limitation, illustrate the anti-aging cosmetic compositions according to the present invention, which surprisingly provide an immediate and prolonged effect, as explained herein.

EXAMPLES

Example 1. Composition According to the Present Invention

(35) The following table illustrates the cosmetic compositions according to the present invention.

(36) TABLE-US-00001 TABLE 1 Anti-aging cosmetic compositions Ingredient Example A Example B Water/Paeonia albiflora 2.00 1.50 extract/phenoxyethanol/ethylhexyl glycerin Water/Secale Cereale Extract/Penthylene 4.00 6.00 Glycol aqua 80.63 82.11 Avena Sativa Extract/Water 4.00 2.00 Butylated Hydroxytoluene (BHT) 0.05 0.05 Disodium EDTA 0.10 0.10 Fragrance 0.20 0.20 Glycerin (glycerol) 5.00 4.00 Hymenaea courbaril Extract 0.50 0.70 Iodopropynyl Butylcarbamate 0.09 0.08 Pataqueira essential oil 0.001 0.001 PEG-40 Hydrogenated Castor Oil 1.00 1.50 Phenoxyethanol 0.80 0.70 Schinus terebinthifolius Extract 0.03 0.01 Water/Casearia sylvestris Extract/Silica 0.10 0.05 Xanthan gum (Keltrol SFT) 1.50 1.00 TOTAL 100.00 100.00

Example 2. Evaluation of the Increase in Skin Firmness and Elasticity by Cutometry

(37) 26 survey participants have completed the study and their average age was: 51±8 years.) There were no reports or evidence of adverse reaction during the study.

(38) The product was applied twice a day, once in the morning and once at night, on the forearm identified with a satin ribbon, by massaging it until completely absorbed.

(39) The methodology consisted of evaluating the increase in skin firmness and elasticity through cutometry measurements (Cutometer® MPA-580 and Multiprobe Adapter MPA-580, CKeletronics, Germany) performed in the beginning of the study, after 30 minutes from the first application and after 28 and 56 days of home use of the product under investigation. Cutometry measurements were performed on the forearm region. The increase in skin firmness has been evaluated using the Ur/Ue parameter (R5) and the increase in skin elasticity was evaluated using the Ur/Uf parameter (R7).

(40) Skin firmness has been assessed using the Ur/Ue parameter. Ur/Ue parameter is the ratio between immediate retraction and immediate skin deformation and corresponds to the biological elasticity.

(41) Increased skin firmness is evidenced by an increase in the Ur/Ue parameter that reflects an improvement of properties of the elastic fibers and collagen.

(42) Skin elasticity was evaluated using the Ur/Uf parameter, which consists of the ratio between immediate retraction and total skin deformation, including the viscous part of skin deformation, and corresponds to biological elasticity.

(43) Increased skin elasticity is evidenced by the increase in the Ur/Uf parameter that reflects an improvement of the elastic fiber properties.

(44) Based on the mean values of the Ur/Ue parameter, the percent increase in skin firmness (% AF) is calculated according to equation 1. % AFti=100*(Ur/Ueti−Ur/Uet0)/Ur/Uet0 (Equation 1) wherein: % AFti=percent increase in firmness; Ur/Ueti=mean Ur/Ue parameter values obtained after i days of study (i=30 minutes, 28 and 56 days); Ur/Urt0=mean Ur/Ue parameter values obtained in the beginning of the study (baseline).

(45) Based on the mean values of the Ur/Uf parameter, the percent increase in skin elasticity (% AE) is calculated according to equation 2. % AEti=100*(Ur/Uf ti−Ur/Uf t0)/Ur/Uf t0 (Equation 2) wherein: % AEti=percent increase in elasticity; Ur/Ufti=mean Ur/Uf parameter values obtained after i days of study (i=30 minutes, 28 and 56 days); Ur/Uft0=mean Ur/Uf parameter values obtained in the beginning of the study (baseline).

(46) The significance of the increase in skin firmness is assessed by applying a bimodal, paired Student's t-test method based on a 95% confidence interval to the basal mean values of the Ur/Ue parameter in relation to the values obtained after i days of use; i=30 minutes, 28 and 56 days. The proper result is achieved when Ur/Ueti is significantly higher than Ur/Uet0 (P<0.05) indicating an increase in skin firmness.

(47) The significance of increased skin elasticity is assessed by applying the bimodal, paired Student's t-test method, based on a 95% confidence interval, to the basal mean values of the Ur/Uf parameter in relation to values obtained after i days of use; i=30 minutes, 28 and 56 days. The proper result is achieved when Ur/Ufti is significantly higher than Ur/Uf t0 (P<0.05) indicating an increase in skin elasticity.

(48) According to the results, it was verified that there was a significant increase in firmness and elasticity of the forearm skin after 28 and 56 days of home use of the product under investigation.

(49) The percent values of increase in forearm skin firmness were: 4.0% after 28 days and 9.1% after 56 days of home use.

(50) 75.0% of the survey participants exhibited increased forearm skin firmness after 28 days and 80.0% after 56 days of home use of the product being investigated.

(51) The percent values obtained of increase in forearm skin elasticity were: 3.4% after 28 days and 6.2% after 56 days of home use.

(52) 76.9% of the survey participants exhibited increased forearm skin elasticity after 28 days and 84.6% after 56 days of home use of the product being investigated.

BRIEF DESCRIPTION OF THE FIGURES

(53) The graph of FIG. 1 shows the mean values of the Ur/Ue parameter obtained in the beginning of the study, 30 minutes after the first application, after 28 and 56 days of home use of the product being investigated.

(54) The graph of FIG. 2 shows the mean values of the Ur/Uf parameter obtained in the beginning of the study, 30 minutes after the first application, after 28 and 56 days of home use of the product being investigated.

Example 3. In Vivo Evaluation of the Increase in the Synthesis of Collagen by DRS

(55) 20 survey participants have completed the study. Average Age: 46±12 years.) There were no reports or evidence of adverse reaction during the study.

(56) Upon enrollment of the participants in the study, they were instructed to discontinue the use of any topical products on the face for up to 72 hours prior to the beginning of the study. On the first day of the study, the survey participants who attended the laboratory were given clarifications by the main investigator on the study procedures, ethical and legal aspects, risks and benefits of the study procedure, medical support, reimbursement of participation costs and were asked to sign two copies of the TCLE. After staying for 15 minutes in an acclimatized room (22±2° C. and 50±5% RH), the baseline measurement (spectrum acquisition prior to the application of the product) was performed at the outer corner of the eye and the measurements were made randomly on the right and left sides of the survey participant. Spectra were obtained in the range of from 260 to 360 nm with emission at 380 nm using a 6-mm diameter optical-bifurcated probe coupled to Fluorolog—Jobin Yvan Horibe, Model FL3-12 with a xenon lamp. After the baseline measurement, the participants received the investigational product and instructions for using and completing the use log. The survey participants returned to the laboratory after 28, 56 and 90 days of use of the investigational product to repeat the measurement procedure, as performed on the first day of the study.

(57) The composition according to the present invention was applied twice a day, once in the morning and once in the evening on clean and dry skin by massaging the product on the face until being completely absorbed.

(58) According to the obtained results, it was possible to conclude that after 28, 56 and 90 days of continuous use of the investigational product a significant increase in collagen intensity was observed relative to the baseline skin condition. The product under investigation caused an increase in collagen intensity over the baseline skin condition of 3.1% after 28 days, 24.1% after 56 days and 26.1% after 90 days of continuous use.

(59) The graph of FIG. 3 shows the mean values of the signal intensity referring to collagen, I340/I295 versus the time of study.

Example 4. Evaluation of the Efficacy of a Cosmetic Product Through the Efficacy Perceived by the Survey Participant and the Evaluation of Dermatological Clinical Efficacy Under Normal Use Conditions

(60) The survey participants were evaluated by a dermatologist in the beginning of the study (D0) to verify the inclusion and exclusion criteria and were also evaluated in the end of the study to verify possible reactions or discomforts experienced while using the product.

(61) The included participants were clinically evaluated by the dermatologist for the initial state of the face skin and were later instructed to answer a self-assessment questionnaire on the initial state of the face skin (D0).

(62) After inclusion and application of the initial questionnaire, the product was applied under supervision to all participants.

(63) After the first application of the product, evaluations of perceived and clinical efficacy were performed through questionnaires 10 minutes after applying the product in the Institute (Immediate) and after 7, 14, 28 and 56 days (+/−2 days) of use of the product.

(64) Participants were instructed to use the product at home according to the provided instructions for 56 days (+/−2 days).

(65) 70 female participants aged 40 to 70 years (average of 56 years) presenting wrinkles of grades II to V and apparent flaccidity of grades I to IV were included in the study.

(66) Assessment of Perceived Efficacy: An improvement in wrinkles (deep lines), expression lines/signs (fine lines), signs of aging, firmness, general appearance and facial harmony was observed in D14 and D56 as compared to D7; An improvement in wrinkles (deep lines), expression lines/signs (fine lines), signs of aging, general appearance and facial harmony was observed in d28 as compared to D7; An improvement in wrinkles (deep lines), expression lines/signs (fine lines), signs of aging, firmness and facial harmony was observed in D56 as compared to D14; An improvement in expression lines/signs (fine lines), signs of aging, firmness, general appearance and facial harmony was observed in D56 as compared to D28.

(67) Immediate: 72.4% of the participants perceived a tensor effect; 82.8% of participants reported improved overall appearance; 39.7% of the participants reported an improvement in the appearance of wrinkles/expression lines.

(68) D7: 62% of the participants reported a reduction in wrinkles (deep lines); 66% of the participants reported a reduction in expression lines/signs (fine lines); 66% of the participants reported a reduction in the signs of aging (weather marks, spots, wrinkles/expression lines and sagging); 78% of the participants reported improved firmness; 91% of the participants reported an improvement in the overall appearance (bright, revitalized, rebalanced, healthy looking skin); 71% of the participants reported an improvement in facial harmony (improved facial contour).

(69) D14: 71% of the participants reported a reduction in wrinkles (deep lines); 83% of the participants reported a reduction in expression lines/signs (fine lines); 83% of the participants reported a reduction in the signs of aging (weather marks, spots, wrinkles/expression lines and sagging); 91% of the participants reported an increase in skin firmness; 98% of the participants reported an improvement in the overall appearance (bright, revitalized, rebalanced, healthy looking skin); 86% of the participants reported an improvement in facial harmony (improved facial contour).

(70) D28: 86% of the participants reported a reduction in wrinkles (deep lines); 88% of the participants reported a reduction in expression lines/signs (fine lines); 86% of the participants reported a reduction in the signs of aging (weather marks, spots, wrinkles/expression lines and sagging); 90% of the participants reported an increase in skin firmness; 98% of the participants reported an improvement in the overall appearance (bright, revitalized, rebalanced, healthy looking skin); 86% of the participants reported an improvement in facial harmony (improved facial contour).

(71) D56: 93% of the participants reported a reduction in wrinkles (deep lines); 93% of the participants reported a reduction in expression lines/signs (fine lines); 90% of the participants reported a reduction in the signs of aging (weather marks, spots, wrinkles/expression lines and sagging); 91% of the participants reported an increase in skin firmness; 100% of the participants reported an improvement in the overall appearance (bright, revitalized, rebalanced, healthy looking skin); 91% of the participants reported an improvement in facial harmony (improved facial contour).
Assessment of Clinical Efficacy

(72) Comparison with D0: An improvement in firmness, facial harmony, overall appearance and healthy appearance was observed in times Immediate and D7 over D0; An improvement in expression lines on the face, signs of aging, firmness, facial harmony, overall appearance and healthy appearance was observed at D14 as compared to D0; An improvement in the degree of periorbital wrinkles, facial expression lines, signs of aging, degree of sagging, firmness, facial harmony, overall appearance and healthy appearance was observed at D28 and D56 as compared to D0.

(73) Comparison with Immediate: An improvement in facial harmony was observed at D7 as compared with

(74) Immediate; An improvement in the signs of aging, firmness, facial harmony, overall appearance and healthy appearance was observed at D14 as compared to Immediate; An improvement in the degree of (periorbital) wrinkles, signs of aging, degree of sagging, firmness, facial harmony, overall appearance and healthy appearance was observed at D28 as compared to Immediate: An improvement in the degree of (periorbital) wrinkles, facial expression lines, signs of aging, degree of sagging, firmness, facial harmony, overall appearance and healthy appearance was observed at D56 as compared to Immediate.

(75) Comparison with D7: An improvement in the signs of aging, firmness, facial harmony, overall appearance and healthy appearance was observed at D14 as compared to D7; An improvement in the degree periorbital wrinkles, signs of aging, degree of sagging, firmness, facial harmony, overall appearance and healthy appearance was observed at D28 as compared to D7: An improvement in the degree of periorbital wrinkles, facial expression lines, signs of aging, degree of sagging, firmness, facial harmony, overall appearance and healthy appearance was observed at D56 as compared to D7.

(76) Comparison with D14: An improvement in firmness, facial harmony, overall appearance and healthy appearance was observed in D28 as compared to D14; An improvement in the degree of periorbital wrinkles, facial expression lines, signs of aging, degree of sagging, firmness, facial harmony, overall appearance and healthy appearance was observed at D56 as compared to D14.

(77) Comparison with D28: An improvement in the degree of periorbital wrinkles, facial expression lines, signs of aging, firmness, facial harmony, overall appearance and healthy appearance was observed at D56 as compared to D28.

Example 5. Evaluation of the Efficacy of a Cosmetic Product Through Instrumental Measurements Under Normal Use Conditions

(78) The survey participants were evaluated by a dermatologist in the beginning of the study (TO) to verify the inclusion and exclusion criteria and were also evaluated in the end of the study to verify possible reactions or discomforts experienced while using the product.

(79) After the initial medical evaluation images of the periorbital, nasogenian, and frontal regions were obtained using Optical 3D Skin Measuring Device PRIMOS Compact 5.075. The obtained images of the periorbital and nasogenian regions were performed randomly.

(80) After acquisition of the initial images the product was applied under supervision to all participants.

(81) New images using Optical 3D Skin Measuring Device PRI MOS Compact 5.075 were performed 15 minutes after application of the product (Immediate) and after 7, 14, 28 and 56 days (+1-2 days) of use of the product.

(82) Participants were instructed to use the product at home according to the provided instructions for 56 days (+1-2 days).

(83) The participants were allowed to rest in a temperature- and relative humidity-controlled room (20° C.±2° C. and 50%±5 RH) for 30 minutes prior to the initial measurements and while performing the measurements.

(84) 29 female participants aged 32 to 69 years (average of 58 years) presenting wrinkles of grades II to V and apparent flaccidity of grades II to IV were included in the study.

(85) Assessment of Cutaneous Relief—Primos

(86) Periorbital Region: The product caused a reduction in wrinkle volume after seven, fourteen, twenty-eight and fifty-six days of use; The product caused a reduction in the average roughness (Ra) and average depth (Rz) of wrinkles after fifty-six days of use; The product caused a reduction in rippling (Wt) of the wrinkles immediately after application of the product and after fifty-six days of use; The product caused a reduction in wrinkle depth after fourteen, twenty-eight and fifty-six days of use; The product caused a reduction in wrinkle texture after fifty-six days of use.

(87) Nasogenian Region: The product caused a reduction in the average roughness, average depth and maximum roughness of wrinkles after seven, fourteen, twenty-eight and fifty-six days of use. The product caused a reduction in rippling of the wrinkles after seven and fourteen days of use; The product caused a reduction in wrinkle texture after fifty-six days of use.

(88) Frontal Region: The product caused a reduction in volume, average roughness, average depth, maximum roughness, rippling and depth of the wrinkles after twenty-eight and fifty-six days of use; and The product caused a reduction in wrinkle texture after seven and fifty-six days of use.

(89) The person skilled in the art, by means of the teachings of the text and examples disclosed herein, will readily appreciate the advantages of the invention and will propose equivalent embodiment variations and alternatives without departing from the scope of the invention as defined in the so appended claims.