Polymerized phosphatidylcholine vesicles as drug carriers.

Abstract

Polymerized ammonium and phosphatidylcholine vesicles have been synthesized via poly(methacrylate) and poly(disulfide) formation. A functionalized polymeric liposome has also been synthesized and effectively conjugated with alpha chymotrypsin. Vesicles derived from 2 have been studied most extensively as potential carriers of drugs. The are extremely stable toward physical perturbation and exposure to organic solvents or detergents, and should be able to maintain their integrity and homogeneity during pharmaceutical manufacturing procedures, including lyophilization. The fact that they retain substantial quantities of lipophilic substances in the presence of detergent concentrations in excess of those found in the upper gastrointestinal tract suggests that they should be able to carry and selectively release lipophilic drugs in the lower reaches of the GI tract. Moreover, the apparent lack of acute toxicity of these vesicles, as indicated by intravenous administration to outbred mice, further suggests that such photopolymerized liposomes may represent a unique and valuable carrier for the controlled delivery of certain types of therapeutic agents, especially by the oral route.