Compositions and methods for enhancing the efficacy of contraceptive microbicides

Abstract

The present disclosure relates to compositions and methods for contraception that also enhance the efficacy of microbicides. Such compositions serve the dual purpose of preventing pregnancy and lessening the risk of spreading sexually transmitted diseases. More specifically, the compositions and methods relate to syngergistic contraceptive microbicide and antiviral compositions comprising a combination of a contraceptive microbicide and an antiviral agent in an acidic carrier that enhances the efficacy of both the contraceptive microbicide and antiviral agent.

1 .- 7 . (canceled) 
     
     
         8 . A composition comprising:
 a) a matrix-forming compound selected from the group consisting of: alginic acid, chitosan, gellan gum, and poloxamer;   b) a bioadhesive compound that is the same or different from the matrix-forming compound;   c) L-lactic acid; and   d) an aqueous-based pharmaceutically acceptable carrier,   
       wherein the composition has a nonmatrix state when not in contact with ejaculate, and a matrix state when in contact with ejaculate, and wherein the composition is essentially free of D-lactic acid. 
     
     
         9 . The composition of  claim 8 , further comprising a humectant. 
     
     
         10 . The composition of  claim 9 , wherein the humectant is selected from the group consisting of glycerol, polyethylene glycol, polypropylene glycol, sorbitol, and triacetin. 
     
     
         11 . The composition of  claim 10 , further comprising a preservative. 
     
     
         12 . The composition of  claim 11 , wherein the preservative is selected from the group consisting of benzoic acid, sodium benzoate, methylparaben, ethylparaben, butylparaben, propylparaben, benzyalkonium chloride, phenylmercuric nitrate, and chlorhexidine. 
     
     
         13 . The composition of  claim 8 , wherein the matrix-forming compound is alginic acid. 
     
     
         14 . The composition of  claim 13 , wherein the alginic acid has an average molecular weight in the range of about 20,000 to about 300,000 g/mole. 
     
     
         15 . The composition of  claim 8 , wherein the bioadhesive compound is selected from the group consisting of xanthan gum, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, sodium carboxymethyl cellulose, chitosan, polycarbophil, and carbopol. 
     
     
         16 . The composition of  claim 15 , wherein the bioadhesive compound is xanthan gum. 
     
     
         17 . The composition of  claim 8 , wherein the composition in the matrix state is capable of trapping and inactivating sperm. 
     
     
         18 . The composition of  claim 8 , wherein the composition in the matrix state is capable of preventing or inhibiting the growth of and preventing or reducing the infectivity of microbes causing sexually transmitted infections. 
     
     
         19 . The composition of  claim 8 , comprising about 1-10% of the matrix forming compound, about 1-10% of the bioadhesive compound, and 1-10% L-lactic acid. 
     
     
         20 . The composition of  claim 8 , comprising about 3-5% of the matrix forming compound, 2.5-3.5% of the bioadhesive compound, and 1-7% L-lactic acid. 
     
     
         21 . A composition comprising:
 a) alginic acid;   b) xanthan gum;   c) L-lactic acid; and   d) water,   
       wherein the composition has a nonmatrix state when not in contact with ejaculate, and a matrix state when in contact with ejaculate, and wherein the composition is essentially free of D-lactic acid. 
     
     
         22 . The composition of  claim 21 , wherein the alginic acid has an average molecular weight in the range of about 20,000 to about 300,000 g/mole. 
     
     
         23 . The composition of  claim 21 , wherein the composition in the matrix state is capable of trapping and inactivating sperm. 
     
     
         24 . The composition of  claim 21 , wherein the composition in the matrix state is capable of preventing or inhibiting the growth of and preventing or reducing the infectivity of microbes causing sexually transmitted infections. 
     
     
         25 . The composition of  claim 21 , further comprising at least one of citric acid, potassium bitartrate, and benzoic acid. 
     
     
         26 . The composition of  claim 25 , further comprising glycerol.