Preparation and in vitro antiviral activity of liposomes of lipophilic esters of acyclovir.
The long chain acyclovir such as the acyclovir laurate and acyclovir palmitate were prepared directly from acyclovir by application of the usual esterification methods with appropriate acyl chlorides. The lipophilic prodrugs were found to be retained easier by liposomes whereas acyclovir escaped readily from liposomes. When assayed in African green monkey cell cultures against herpes simplex virus type I strain, the acyclovir palmitate liposomes proved to be more active compared with the parent drug and its liposome, suggesting an enhanced compatibility between the ester and liposomal lipids and an increased uptake of encapsulated prodrug by infected cells.
Tong
P
P
302 Hospital of Infectious Diseases, Beijing.
Hou
X P
XP
Shao
S
S
Zhang
Y M
YM
Zhang
C H
CH
D000212:Acyclovir / Q000494:pharmacology; D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D008081:Liposomes; D011355:Prodrugs; D018139:Simplexvirus / Q000187:drug effects; D014709:Vero Cells
D000998:Antiviral Agents; D008081:Liposomes; D011355:Prodrugs; D000212:Acyclovir