PREPARTION AND IN VITRO ANTIVIRAL ACTIVITY OF LIPOSOMES OF LIPOPHILIC ESTERS OF ACYCLOVIR

The long chain acyclovir such as the acyclovir laurate and acyclovirpalmitate were prepared directly from acyclovir by application of the usual esterification meth-ods with appropriate acyl chlorides. The lipophilic prodrugs were found to be retained easier byliposomes whereas acyclovir escaped readily from liposomes.When assayed in African green mon-key cell cultures against herpes simplex virus type I strain, the acyclovir palmitate liposomesproved to be more active compared with the parent drug and its liposome, suggesting an en-hanced compatibility between the ester and liposomal lipids and an increased uptake ofencapsulated prodrug by infected cells.