Gel useful for the delivery of cosmetic active ingredients

Abstract

It is described a gel, for cosmetic use, composed of a mixture of a polymer which forms a gel, a surfactant, and propionyl L-carnitine glycinate hydrochloride, useful for treating disturbances of the skin such as cellulite and wrinkles.

1 . A solid powder which comprises:
 a) a carboxy vinyl polymer which forms a gel;   b) a surfactant; and   c) at least one active ingredient selected from the group comprising:   agents supporting the microcirculation;   agents for the activation of the lipolysis;   anti-inflammatory compounds;   skin whitening compounds;   antioxidants and anti-wrinkling compounds;   agents which improve skin penetration and efficacy of common anticellulite agents;   essential fatty acids (EFAs);   sunscreens; or   salts of L-carnitine or an alkanoyl L-carnitine with amino acids having formula (I):   
     
       
         
         
             
             
         
       
       in which: 
       R is hydrogen or a straight or branched-chain alkanoyl group having 2-5 carbon atoms selected from the group consisting of acetyl, propionyl, butyryl, valeryl and isovaleryl; and 
       Y is the anion of an amino acid occurring in proteins selected from the group consisting of: leucine, isoleucine, vahine, cysteine, arginine, glutamic acid, glutamine, asparagine, glycine, alanine, threonine, serine, proline, hystidine, methionine, phenylalanine and tryptophane; 
       the anion Y −  can optionally be salified at the amino group. 
     
   
   
       2 . A gel which comprises:
 a) a carboxy vinyl polymer;   b) a surfactant; and   c) at least one active ingredient selected from the group comprising:   agents supporting the microcirculation;   agents for the activation of the lipolysis;   anti-inflammatory compounds;   skin whitening compounds;   antioxidants and anti-wrinkling compounds;   agents which improve skin penetration and efficacy of common anticellulite agents;   essential fatty acids (EFAs);—sunscreens; or   salts of an alkanoyl L-carnitine with amino acids having formula (I):   
     
       
         
         
             
             
         
       
     
     in which: R is hydrogen or a straight or branched-chain alkanoyl group having 2-5 carbon atoms selected from the group consisting of acetyl, propionyl, butyryl, valeryl and isovaleryl; and Y is the anion of an amino acid occurring in proteins selected from the group consisting of: leucine, isoleucine, vahine, cysteine, arginine, glutamic acid, glutamine, asparagine, glycine, alanine, threonine, serine, proline, hystidine, methionine, phenylalanine and tryptophane;
 the anion Y −  can optionally be salified at the amino group. 
 
   
   
       3 . The solid powder of  claim 1  or the gel of  claim 2 , in which the carboxy vinyl polymer is Carbopol. 
   
   
       4 . The solid powder of  claim 1  or the gel of  claim 2 , in which the surfactant is selected from the group consisting of sodium dodecyl sulfate; an amino acid based cationic surfactant and an amino acid based nonionic surfactant. 
   
   
       5 . The solid powder of  claim 1 , in which the active ingredient is a compound not stable in water or in solution. 
   
   
       6 . The solid powder of  claim 1  or the gel of  claim 2 , in which the agents supporting the microcirculation is selected from the group consisting of extracts of Gingko biloba, ruscus, melilot, red vine and viburnum. 
   
   
       7 . The solid powder of  claim 1  or the gel of  claim 2 , in which the agents for the activation of the lipolysis is selected from the group consisting of extracts of Ground ivy, root of Angelica, Paulinia; M and xanthic bases such as caffeine, theobromine and theophylline. 
   
   
       8 . The solid powder of  claim 1  or the gel of  claim 2 , in which the anti-inflammatory compounds is selected from the group consisting of rosmarinic acid, glycyrrizinate derivatives, alpha bisabolol, azulene and derivatives thereof, asiaticoside, sericoside, ruscogenin, escin, escolin, quercetin, rutin, betulinic acid and derivatives thereof, catechin and derivatives thereof. 
   
   
       9 . The solid powder of  claim 1  or the gel of  claim 2 , in which the skin whitening compounds is selected from the group consisting of ferulic acid, hydroquinone, arbutine, and kojic acid. 
   
   
       10 . The solid powder of  claim 1  or the gel of  claim 2 , In which the antioxidants and anti-wrinkling compounds is selected from the group consisting of retinol and derivatives thereof, tocopherol and derivatives thereof, salicylates and their derivatives thereof. 
   
   
       11 . The solid powder of  claim 1  or the gel of  claim 2 , in which the agents which improve skin penetration and efficacy of common anticellulite agents is selected from the group consisting of a monocarboxylic acids comprising lactic acid, glycolic acid, mandelic acid and mixtures thereof. 
   
   
       12 . The solid powder of  claim 1  or the gel of  claim 2 , in which the essential fatty acids (EFAs) is selected from the group consisting of linoleic acid, gamma-linolenic acid, homo-gamma-linolenic acid, columbinic acid, eicosa-(n-6,9,13)-trienoic acid, arachidonic acid, timnodonic acid, hexaenoic acid and mixtures thereof. 
   
   
       13 . The solid powder of  claim 1  or the gel of  claim 2 , in which the sunscreens, is selected from the group consisting of PABA and derivatives thereof, cinnamate and benzophenone derivatives such as octyl methoxy-cinnamate and 2-hydroxy-4-methoxy-benzophenone. 
   
   
       14 . The solid powder of  claim 1  or the gel of  claim 2 , in which L-carnitine or the alkanoyl L-carnitine with amino acids having formula (I) is selected from the group consisting of acetyl L-carnitine L-isoleucinate hydrochloride, propionyl L-carnitine L-leucinate hydrochloride, L-carnitine L-valinate phosphate, acetyl L-carnitine L-cysteinate hydrochloride, acetyl L-carnitine L-arginate dihydrochloride, acetyl L-carnitine L-glutamninate hydrochloride, acetyl L-carnitine L-asparaginate hydrochloride, acetyl L-carnitine glycinate hydrochloride, acetyl L-carnitine L-alaninate hydrochloride, acetyl L-carnitine L-threoninate hydrochloride, acetyl L-carnitine L-serinate hydrochloride, propionyl L-carnitine L-prolinate hydrochloride, L-carnitine L-hystidinate hydrochloride, L-carnitine L-methionate hydrochloride, propionyl L-carnitine L-phenylalaninate hydrochloride, and acetyl L-carnitine L-typtophanate hydrochloride or propionyl L-carnitine glycinate hydrochloride. 
   
   
       15 . The solid powder of  claim 1  or the gel of  claim 2 , in which the active ingredient is propionyl L-carnitine glycinate hydrochloride. 
   
   
       16 . Method of preparation of the powder of  claim 1 , which comprises the following steps:
 a) preparation of the gel dissolving in water, or in a solution, the gelling agent, the surfactant and one or more active ingredients for cosmetic use, maintaining the pH from 4.0 to 6.0;   b) the gel so obtained is divided in single doses and put into vials;   c) to obtain a powder the vials of step b) are lyophilized; alternatively the gel of point a) is directly subjected to Spray-drying procedure and the powder so obtained is put, in a suitable amount, into vials.   
   
   
       17 . The method of  claim 16 , in which the pH is controlled using an inorganic or organic acid or base. 
   
   
       18 . The method of  claim 17 , in which the base is selected from the group comprising: sodium hydroxide, potassium hydroxide, or a basic amino acid selected from lysine, arginine, histidine, or ornithine. 
   
   
       19 . Cosmetic composition, comprising the powder or the gel of  claims 1  or  2 , and optionally one or more cosmetically acceptable excipient and/or diluent. 
   
   
       20 . Cosmetic composition comprising as active ingredient propionyl L-carnitine glycinate hydrochloride, and optionally at least a further active ingredient, and/or cosmetically acceptable excipient, and/or diluent. 
   
   
       21 . Cosmetic composition of  claim 20 , in which the excipient and/or diluent is selected from the group consisting of thickener agents; preservatives; silicone polymers; emollients; water; colouring agents; opacifiers; and perfumes. 
   
   
       22 . Cosmetic composition of  claim 20 , in which the further active ingredient is selected from the group consisting of
 agents supporting the microcirculation;   agents for the activation of the lipolysis;   anti-inflammatory compounds;   skin whitening compounds;   antioxidants and anti-wrinkling compounds;   agents which improve skin penetration and efficacy of common anticellulite agents;   essential fatty acids (EFAs); and   sunscreens.   
   
   
       23 - 30 . (canceled) 
   
   
       31 . Kit comprising the powder of  claim 1 , and separately, in the same or in a different container, water or a liquid solution. 
   
   
       32 . Kit comprising the powder of  claim 1 , in which the active ingredient is propionyl L-carnitine glycinate hydrochloride, and separately, in the same or in a different container, water or a liquid solution. 
   
   
       33 . A method of preventing or treating disturbances of the skin, comprising topically administering an effective amount of the cosmetic composition of  claim 20  to an area of the skin requiring such treatment.