Abstract

Objective: The objective of this study was to formulate and evaluate liposomes loaded with acyclovir.
 Methods: Liposomal formulation of acyclovir was prepared by “thin lipid film method”. Mixture of phosphotidyl choline (soya lecithin), acyclovir and cholesterol of varying weight ratio was used for the preparation of liposomes. Total nine batches were prepared and each batch was prepared in triplicate. All batches were evaluated by drug entrapment and release kinetic studies. Stability study was carried out with F4 batch.
 Results: F2 and F9formulations showed better drug entrapment efficiency compared to the other batches. The drug entrapment efficiency of all batches was found within the range of 51.42 % to 79.0 %. F4 shows highest release of about 79.0% in 4 h. F4 formulation was found to follow significantly zero-order release kinetics. Short term stability study of formulation F4 showed no significant change in release kinetics.
 Conclusion: The F4 batches showed promising results compared to other formulations. No changes were founded during the short-term stability study of F4.

Highlights

  • Liposomes are composed of a lipid bilayer which used as drug delivery vehicles

  • The Drug Entrapment Efficiency (%) values found with various cholesterol proportions are shown in fig. 1

  • From fig. 1 it is evident that % entrapment increases with a decrease in mol % of the cholesterol in the liposome and it became lowest at 39.5 mol% cholesterol (F3), the lowest entrapment efficiency being 51.42%

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Summary

Introduction

Liposomes are composed of a lipid bilayer which used as drug delivery vehicles. The hydrophobic chains of the lipids form the bilayer and the polar head groups of the lipids are towards the extra vesicular solution and inner cavity. Liposomes have polar and non-polar groups on the same molecule. Liposome preparation techniques may be broadly classified into two types– bulk method and film method. In the film method lipid films are deposited on a substrate followed by hydration to get the liposomes. The hydrophilic part of liposomes is mainly phosphoric acid bound to water-soluble molecules. On the other hand hydrophobic part of liposome contains two fatty acid chains with 10 to 24 carbon atoms and each chain contains 0 to 6 double bonds [3]

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