Topical composition containing antioxidants
Compositions for topical application that effectively deliver antioxidants across the epidermis, dermis, or a combination thereof into cells and/or the bloodstream while concurrently maintaining chemical activity of the antioxidants. In certain aspects, these formulations include emulsions and balms each having a lipophilic carrier and a lipophilic antioxidant solubilized by the lipophilic carrier. Also disclosed herein are methods for making these compositions for topical application.
1. A topical composition comprising:
30-75 percent by weight water;
3-6 percent by weight surfactant;
1-50 percent by weight lipophilic carrier having a molecular weight between 150 and 600;
0.25-4 percent by weight lipophilic antioxidant having a formula:
wherein:
R 1 represents a C 1 to C 9 linear or branched alkyl group or styrene;
R 2 is optional and represents a C 1 to C 6 linear or branched alkyl group or styrene;
Y 1 represents a C 1 to C 6 linear or branched alkyl group, styrene, —SR 5 , or —(CH 2 ) n COOR 6 ;
n is from 1 to 10;
R 5 represents isoprene, a methyl group, an ethyl group, a propyl, a butyl, a pentyl group, a hexyl group, an isopropyl group, an isobutyl group, a sec-butyl group, a tert-butyl group, a tert-pentyl group, a neo-pentyl group, an isopentyl group, an isohexyl group, a neohexyl group, styrene, or
wherein R 11 , R 12 , and R 13 independently represent OH, a methyl group, ethyl group, a propyl group, a butyl group, an isopropyl group, a tert-butyl group, an isoprene, or a tert-pentyl group;
R 6 represents an alkyl group having C 10 to C 30 ;
and
wherein the formula includes pharmaceutically acceptable salts thereof;
1-10 percent by weight skin penetration enhancer;
9-11 percent by weight paraffinic oil; and
0.5-5 percent by weight of a preservative mixture comprising propylene glycol, diazolidinyl urea, methylparaben, and propylparaben and tetrasodium ethylenediaminetetraacetic acid;
wherein once the topical composition is compounded, the topical composition is a cream emulsion.
2. A topical composition comprising:
30-75 percent by weight water;
3-6 percent by weight surfactant;
1-50 percent by weight lipophilic carrier having a molecular weight between 150 and 600;
0.25-4 percent by weight lipophilic antioxidant having a formula:
wherein:
R 3 and R 4 independently represent a C 1 to C 6 branched alkyl;
Y 2 represents a C 1 to C 6 linear or branched alkyl group, —R 5 , or —(CH 2 ) n COOR 6 ;
R 5 represents isoprene, a methyl group, an ethyl group, a propyl, a butyl, a pentyl group, a hexyl group, an isopropyl group, an isobutyl group, a sec-butyl group, a tert-butyl group, a tert-pentyl group, a neo-pentyl group, an isopentyl group, an isohexyl group, a neohexyl group, styrene, or
wherein R 11 , R 12 , and R 13 independently represent OH, a methyl group, ethyl group, a propyl group, a butyl group, an isopropyl group, a tert-butyl group, an isoprene, or a tert-pentyl group, and
R 6 represents an alkyl group having C 10 to C 30 ;
n is from 1 to 10;
and
wherein the formula includes pharmaceutically acceptable salts thereof;
1-10 percent by weight skin penetration enhancer;
9-11 percent by weight paraffinic oil; and
0.5-5 percent by weight of a preservative mixture comprising propylene glycol, diazolidinyl urea, methylparaben, and propylparaben and tetrasodium ethylenediaminetetraacetic acid;
wherein once the topical composition is compounded, the topical composition is a cream emulsion.
3. A topical composition comprising:
30-75 percent by weight water;
3-6 percent by weight surfactant;
1-50 percent by weight lipophilic carrier having a molecular weight between 150 and 600;
0.25-4 percent by weight lipophilic antioxidant having a formula:
wherein:
R 3 and R 4 independently represent a C 1 to C 6 branched alkyl;
Y 3 represents a linear or branched alkyl group having C 10 to C 30 ;
and
wherein the formula includes pharmaceutically acceptable salts thereof;
1-10 percent by weight skin penetration enhancer;
9-11 percent by weight paraffinic oil; and
0.5-5 percent by weight of a preservative mixture comprising propylene glycol, diazolidinyl urea, methylparaben, and propylparaben and tetrasodium ethylenediaminetetraacetic acid;
wherein once the topical composition is compounded, the topical composition is a cream emulsion.