The present invention relates to super-concentrated cosmetic anti-sign compositions, in the form of an elixir, particularly useful in the treatment of wrinkles, especially in the area under eyes.
Skin aging is the result of several factors. In addition to each individual's genetic predisposition, there are external factors and factors related to life style and quality, where our organism, including the skin, undergoes alterations and slowing down of several physiological processes.
Wrinkles can appear in people of any age and sex and, as ultimate perception, the skin appearance compromised with deep wrinkles end by imparting a fatigue and aging appearance to those people afflicted thereby.
Cosmetic compositions, even if super-concentrated, provably effective in reducing the amount of wrinkles, particularly in the area under the eyes, while improving firmness of the eyelids are still desirable.
    
    
The present invention relates to super-concentrated cosmetic anti-sign compositions, in the form of an elixir, which are particularly useful in the treatment of wrinkles, specially in the area under eyes, while improving firmness of the eyelids.
By “elixir”, as used herein, it is intended to mean any cosmetic compositions which are super-concentrated in active ingredients targeted to reducing wrinkles and improving firmness of the eyelids. By “super-concentrated” it is intended to mean any cosmetic compositions containing more than about 7% of one or more active compounds, particularly from about 7 to about 15% of one or more active compounds.
The cosmetic anti-sign composition according to the present invention is an elixir comprising:
The emollient is selected from the group consisting of capric/caprylic trigliceride, caprylyl methicone, alkyl benzoate having 12 to 15 carbons, dibutyl adipate, dicaprylyl carbonate, isononyl isononanoate, dicapryl ether, dodecane, ethylhexyl palmitate, ethyl macadamiate, isohexadecane, isoamyl cocoate, ou suas misturas. In a particular embodiment, the emollient is capric/caprylic trigliceride.
The humectant is selected from the group consisting of glycerol, glycols, sorbitol, mannitol, or mixtures thereof. In a particular embodiment, the humectant is glycerol.
The active compound is selected from the group consisting of Hymenaea courbaril extract, Spilanthes Acmella extract, a mixture of silanetriol/hyaluronic acid, a mixture of sodium cocoyl amino acids/sarcosine/potassium aspartate/magnesium aspartate/propylene glycol, acethyl tetrapeptide-2, a mixture of Paeonia albiflora extract/phenoxyethanol/ethylhexylglycerine, extrato de Cichorium intybus, or mixtures thereof. In particular the active compound is Hymenaea courbaril extract, Spilanthes Acmella extract, a mixture of silanetriol/hyaluronic acid, a mixture of sodium cocoyl amino acids/sarcosine/potassium aspartate/magnesium aspartate/propylene glycol, or mixtures thereof.
The emulsifier is selected from the group consisting of a mixture of cetearyl isononanoate/ceteareth-20/cetearyl alcohol/glyceril stearate/glycerine/ceteareth-12/cethyl palmitate, acrylates, xanthan gum, glyceril citrate, potassium cethylphosphate, PEG-100, cetearyl alcohol, a mixture of glyceril stearate/PEG-100, or mixtures thereof. In particular the emulsifier is a mixture of cetearyl isononanoate/ceteareth-20/cetearyl alcohol/glyceril stearate/glycerine/ceteareth-12/cethyl palmitate, acrylates, xanthan gum, or mixtures thereof. Particularly the emulsifier is cyclopentasiloxane.
The sensorial modifier is selected from the group consisting of cyclopentasiloxane, dimethicone, cyclopentasiloxane/dimethicone crospolymers/titanium isopropyl triisostearate, nylon-12, polimethylsilsesquioxane, or mixtures thereof.
The cosmetically acceptable vehicles can be selected from those compounds known in the art.
As examples of vehicles there can be mentioned: solvents, preservatives, perfumes/fragrances, polymer neutralizing agents, chelating agents (such as disodium EDTA), pH adjusting agents, and the like.
The cosmetic compositions according to the present invention act on 11 main mechanisms responsible for wrinkle formation on the area under the eyes and eyelid flaccidity. Those are as follows:
This simultaneous action on 11 mechanisms is possible because of the super-concentrate of synergistically and simultaneously acting active ingredients containing:
The compositions according to the present invention can be provided in the form of a medicine-dropper to facilitate dropwise application directly onto the skin area to be treated, particularly the area under the eyes.
Therefore, the present invention also contemplates an applicator device which is a medicine-dropper containing the composition of the present invention.
In a particular embodiment, the cosmetic compositions according to the present invention act on the expression signs, in addition to protecting, replacing, and stimulating hyaluronic acid, showing improvement in the eyelid firmness.
Another object of the present invention is the use of the cosmetic compositions in anti-sign treatment, particularly in wrinkle treatment, in the area under the eyes.
Still another object of the present invention is a method of anti-sign treatment, as well as method of wrinkle reduction, particularly in the area under the eyes, consisting of applying a cosmetically effective amount of a composition according to the present invention, on the area under the eyes, at least twice daily. In a particular embodiment, the cosmetically effective amount consists of drops.
The following examples, but without any limitation, illustrate the cosmetic anti-sign compositions according to the present invention, which surprisingly act, simultaneously, on 11 main mechanisms responsible for wrinkle formation in the area under the eyes, and eyelid flaccidity.
The following table illustrates cosmetic compositions according to the present invention.
  
    
      
        
        
          
            
          
        
        
          
            
          
          
            
          
        
      
      
        
        
        
        
          
            
            
            
          
          
            
            
            
          
          
            
          
        
      
      
        
        
        
        
          
            
            
            
          
          
            
            
            
          
          
            
            
            
          
          
            
          
          
            
            
            
          
          
            
            
            
          
          
            
            
            
          
          
            
            
            
          
          
            
            
            
          
          
            
          
          
            
          
          
            
          
          
            
          
          
            
            
            
          
          
            
            
            
          
          
            
            
            
          
          
            
            
            
          
          
            
          
          
            
          
          
            
          
          
            
            
            
          
          
            
            
            
          
          
            
            
            
          
          
            
          
        
      
    
  
The methodology consisted of assessing the increase in firmness and elasticity of the skin by using cytometry measurements (Cytometer® MPA-580 and Multiprobe Adapter MPA-580, CKeletronics, Germany) taken at the beginning of the study, 30 minutes after the first application of the test product at the laboratory and after applying the test product at home for 7, 14, 28 and 56 days. Cytometry measurements were taken on the forearm area. The increase in firmness of the skin was assessed by means of the Ur/Ue parameter (R5) and the increase in elasticity of the skin was assessed through the Ur/Uf parameter (R7).
Firmness of the skin was assessed through the Ur/Ue parameter. The Ur/Ue parameter is the ratio between instant retraction and instant deformation of the skin and corresponds to the biological elasticity.
An increase in firmness is evidenced by an increase in the Ur/Ue parameter Ur/Ue parameter that reflects an increase in the properties of the elastic fibers and collagen.
Elasticity of the skin was assessed through the Ur/Uf parameter that is the ratio between instant retraction and total deformation of the skin, including the viscous part of the skin deformation, and corresponds to the biological elasticity.
An increase in elasticity of the skin is evidenced by an increase in the Ur/Uf parameters that reflects an increase in the properties of the elastic fibers.
From the average values of the Ur/Ue parameter the percentage increase in firmness of the skin (% AF) is calculated, according to Equation 1.
  
  % AFti=100*(Ur/Ueti−Ur/Uet0)/Ur/Uet0  (Equation 1)
where: % AFti=percentage increase in firmness; Ur/Ueti=average values of the Ur/Ue parameter obtained after day i of the study (i=30 minutes, 7, 14, 28 and 56 days); Ur/Urt0=average values of the Ur/Ue parameter obtained at the beginning of the study (basal).
From the average values of the Ur/Uf parameter the percentage increase in elasticity of the skin (% AE) is calculated, according to Equation 2.
  
  %AEti=100*(Ur/Uf ti−Ur/Uf t0)/Ur/Uf t0  (Equation 2)
where: % AEti=percentage increase in elasticity; Ur/Ufti=average values of the Ur/Uf parameter obtained after day i of the study (i=30 minutes, 7, 14, 28 and 56 dias); Ur/Uft0=average values of the Ur/Uf parameter obtained at the beginning of the study (basal).
A significância do aumento da firmeza da pele is evaluated by applying the Student's bimodal paired t-test, considering a confidence interval of 95%, to the average basal values of the Ur/Ue parameter as compared to the values obtained after a i-day use; i=30 minutes, 7, 14, 28 and 56 days. A suitable result is reached when Ur/Ueti is significantly greater than Ur/Uet0 (P<0.05), indicating an increase in firmeza da pele.
A significância do aumento da elasticidade da pele is evaluated by applying the Student's bimodal paired t-test, considering a confidence interval of 95%, to the average basal values of the Ur/Uf parameter as compared to the values obtained after a i-day use; i=30 minutes, 7, 14, 28 and 56 dias. A suitable result is reached when Ur/Ufti is significantly greater than Ur/Uf t0 (P<0.05), indicating an increase in elasticidade da pele.
25 participants completed the study; average age: 43±14 years. No adverse reactions were noticed or reported during the study.
The cosmetic composition according to the present invention was applied twice daily, once in the morning and once at night.
1 drop on the forearm area, with movements from inside out until its complete absorption.
According to the results achieved, a significant increase in firmness of the forearm skin could be seen after applying the test product at home for 7, 14, 28 and 56 days.
The percentage values of increase in firmness of the forearm skin were: 3.4% after applying the test product at home for 7 days, 6.4% for 14 days, 9.1% for 28 days and 13.7% for 56, as compared to the initial condition of the skin.
76.0% of the participants showed an increase in firmness of the forearm skin after applying the test product at home for 7 days and 96.0% for 14, 28 and 56 days.
There was a significant increase in elasticity of the forearm skin after applying the test product at home for 7, 14, 28 and 56 days.
The percentage values of increase in elasticity of the forearm skin were: 1.6% after applying the test product at home for 7 days, 3.5% for 14 days, 5.3% for 28 days and 8.8% for 56 days.
76.0% of the participants showed an increase in elasticity of the forearm skin after applying the test product at home for 7 days, 80.0% for 14 days, 92.0% for 28 days and 96.0% for 56 days.
The increase in elasticity of the skin is illustrated on the graph in 
The increase in firmness of the skin is illustrated on the graph in 
The volunteers in the research were evaluated by a dermatologist at the beginning of the study (D0) for the criteria of admission and non-admission and were also evaluated at the end of the study for eventual reactions or discomforts experienced while using the product.
Those volunteers admitted in the research (female individuals, aged 39-70 years—average age 57 years—, having grade II to V wrinkles and I to IV phototype) were clinically evaluated by a dermatologist for the initial condition of the face complexion and subsequently they were advised to fill in a self-evaluation questionnaire also related to the initial condition of the face complexion (D0).
In this step, initial images were also acquired from the periorbital area using the Optical 3D Skin Measuring Device PRIMOS Compact 5.075 equipment. Imaging of the periorbital area was performed at random.
A supervised application of the product was performed on all participants.
Within 30 minutes after the first application of the product, new images were acquired by using the Optical 3D Skin Measuring Device PRIMOS Compact 5.075 equipment. New images were acquired after a 7-, 14-, 28- and 56 day (+/−2 days)-use of the product.
Further assessments of the perceived and clinical efficacy were performed through questionnaires, 10 minutes after the first application of the products (Dimediato) and after a 7-, 14-, 28- and 56 day (+/−2 days)-use of the product.
The participants were advised to apply the product at home for 56 days (+/−2 days), according to the instructions provided.
The participants remained at rest in a room at controlled temperature and relative humidity (20° C.±2° C. and 50%±5 RH) for 30 minutes prior to and while the measurements were taken.
D7:
D14:
D28:
D56:
As compared to time point D0:
As compared to time point Dimediato:
As compared to time point D7:
As compared to time point D14:
As compared to time point D28:
Assessment of cutaneous protuberance—Primos:
The product promoted a reduction in Texture after a seven-, fourteen-, twenty-eight-, and fifty-six-day use.
The volunteers in the research were evaluated by a dermatologist at the beginning of the study (D0) for the criteria of admission and non-admission and were also evaluated at the end of the study for eventual reactions or discomforts experienced while using the product.
Those volunteers admitted in the research (female individuals, aged 39-70 years—average age 57 years—, having grade II to V wrinkles and I to IV phototype) were clinically evaluated by a dermatologist for the initial condition of the face complexion and subsequently they were advised to fill in a self-evaluation questionnaire also related to the initial condition of the face complexion (D0).
In this step, initial images were also acquired from the periorbital area using the Optical 3D Skin Measuring Device PRIMOS Compact 5.075 equipment. Imaging of the periorbital area was performed at random.
A supervised application of the product was performed on all participants.
Within 30 minutes after the first application of the product, new images were acquired by using the Optical 3D Skin Measuring Device PRIMOS Compact 5.075 equipment. New images were acquired after a 7-, 14-, 28- and 56 day (+/−2 days)-use of the product.
Further assessments of the perceived and clinical efficacy were performed through questionnaires, 10 minutes after the first application of the products (Dimediato) and after a 7-, 14-, 28- and 56 day (+/−2 days)-use of the product.
The participants were advised to apply the product at home for 56 days (+/−2 days), according to the instructions provided.
The participants remained at rest in a room at controlled temperature and relative humidity (20° C.±2° C. and 50%±5 RH) for 30 minutes prior to and while the measurements were taken.
Assessment of Perceived Efficacy
Dimediato:
D7:
D14:
D28:
D56:
As compared to time point D0:
As compared to time point Dimediato:
As compared to time point D7:
As compared to time point D14:
As compared to time point D28:
Assessment of cutaneous protuberance—Primos:
Based on the teachings provided in the disclosure of the invention and examples one skilled in the art would be able to appreciate the advantages of the invention and propose variations and alternative equivalent embodiments, without departing from the scope of the invention, as defined in the appended claims.
| Number | Date | Country | Kind | 
|---|---|---|---|
| 102016019120-3 | Aug 2016 | BR | national | 
| Filing Document | Filing Date | Country | Kind | 
|---|---|---|---|
| PCT/BR2017/050129 | 5/24/2017 | WO | 00 |