Preparation and invitro evaluation of acyclovir loaded PEGylated liposomes

Abstract

Introduction: Acyclovir is an antiviral drug that its mechanism is to inactivating DNA polymerase and preventing DNA synthesis. Intra venus (IV) infusion is one drug delivery method. Intra venus infusion is an invasive way for drug delivery, and considering its frequency of use; patient compliance is low for this dosage form. Preparing PEGylated liposomes of Acyclovir may prolong its circulatory time and reduce its frequency of use. Liposomes are the first nano-drug delivery systems that have been successfully translated into real-time clinical applications. Stealth technology has been explored in developing a drug delivery system that makes their detection by the mononuclear phagocyte system difficult. Generally, polyethyleneglycol (PEG) is used as a polymer and the process is called PEGylation. PEGylation produces alterations in the physiochemical properties of the active moiety, which further prolongs its circulatory time and reduces dosage frequency. Objective: Preparation and invitro evaluation of acyclovir loaded PEGylated liposomes Methods: Film hydration method was used to prepare modified liposomes with PEG. To partially reduce the size of the resulting liposomes, sonication and extruder were used. Size distribution and zeta potential of the prepared samples was assessed using zetasizer. Next, the amount of drug loading by liposomes was examined. Liposomes were also evaluated for in vitro release. Results: The results of acyclovir loaded PEGylated liposomes showed that the volume size of the prepared formulations was between 122 and 157 nm and the average drug loading in the prepared formulations was over 50%, which is an acceptable amount. Conclusion: After preparing several series of formulations containing acyclovir loaded PEGylated liposomes and evaluating their physicochemical properties, their release kinetics were examined and in most of the prepared formulations, Higuchi model showed the lowest error and Reciprocal Powered Time model showed the highest R^2.