Self micro-emulsifying drug delivery system with increased bioavailability

Abstract

The invention provides a formulation comprising (a) a drug that is poorly water-soluble, (b) at least one surfactant, and (c) at least one polar lipid, wherein the formulation is substantially free of a polar solvent, as well as methods of preparing the formulation and methods of increasing the bioavailability of a drug using the formulation.

1 . A formulation comprising:
 (a) a drug that is poorly water-soluble,   (b) at least one surfactant, and   (c) at least one polar lipid,   
       wherein the formulation is substantially free of a polar solvent. 
     
     
         2 . The formulation of  claim 1 , wherein the at least one surfactant is selected from the group consisting of nonionic, cationic, and anionic surfactants. 
     
     
         3 . The formulation of  claim 1 , wherein the at least one polar lipid is selected from the group consisting of mono- and di-glycerides, esters of fatty acids, and polysilane esthers. 
     
     
         4 . The formulation of  claim 1 , wherein formulation contains 10-90% surfactants. 
     
     
         5 . The formulation of  claim 1 , wherein the formulation contains 10-90% polar lipids. 
     
     
         6 . The formulation of  claim 5 , wherein the formulation contains two polar lipids. 
     
     
         7 . The formulation of  claim 6 , wherein the at least one surfactant is a polysorbate and the two polar lipids are propylene glycol monocaprylate and propylene glycol dicaprate. 
     
     
         8 . The formulation of  claim 7  comprising 10-30% (w/w) propylene glycol monocaprylate, 20-60% (w/w) propylene glycol dicaprate, and 10-30% (w/w) polysorbate. 
     
     
         9 . The formulation of  claim 7  comprising 15-20% (w/w) propylene glycol monocaprylate, 35-50% (w/w) propylene glycol dicaprate, and 15-20% (w/w) polysorbate. 
     
     
         10 . The formulation of  claim 7  comprising 15-17% (w/w) propylene glycol monocaprylate, 38-42% (w/w) propylene glycol dicaprate, and 15-17% (w/w) polysorbate. 
     
     
         11 . The formulation of  claim 7 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, polysorbate 80, and mixtures thereof. 
     
     
         12 . The formulation of  claim 8 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, polysorbate 80, and mixtures thereof. 
     
     
         13 . The formulation of  claim 9 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, polysorbate 80, and mixtures thereof. 
     
     
         14 . The formulation of  claim 10 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, polysorbate 80, and mixtures thereof. 
     
     
         15 . The formulation of  claim 7 , wherein the polysorbate is polysorbate 80. 
     
     
         16 . The formulation of  claim 8 , wherein the polysorbate is polysorbate 80. 
     
     
         17 . The formulation of  claim 9 , wherein the polysorbate is polysorbate 80. 
     
     
         18 . The formulation of  claim 10 , wherein the polysorbate is polysorbate 80. 
     
     
         19 . A method of increasing the bioavailability of a drug that is poorly water-soluble comprising preparing the formulation of  claim 1 , and administering the formulation to a host. 
     
     
         20 . The method of  claim 19 , wherein the at least one surfactant is a polysorbate, and wherein the formulation contains two polar lipids that are propylene glycol monocaprylate and propylene glycol dicaprate.