GALACTOSYLATED POLY (D, L-LACTIC-CO-GLYCOLIC ACID) NANOPARTICLES FOR LIVER TARGETED DELIVERY OF ACYCLOVIR

Abstract

Introduction: The present study discusses d-galactose (Gal) –acyclovir- poly (D, L-lactic-co-glycolic acid) nanoparticles (Gal-PLGA-NPs) using galactose as an asialoglycoprotein receptor (ASGPR) ligand for hepatic targeting.

Methods and Materials: The PLGA nanoparticles (PLGA-NPs) were prepared by double emulsification method and galactose was conjugated to the free amine group of amine ended PLGA. Galactosylation of poly (D, L-lactic-co-glycolic acid) was confirmed by FTIR study and zeta potential measurements. The Gal-PLGA-NPs obtained were characterized for their morphology, particle size, polydispersity index and zeta potential.

Results and Discussion: The spherical nanoparticles prepared with Gal-PLGA were in the 198.1 nm size range exhibited a negative electrical charge (-8.5 mV), with 84.1% acyclovir entrapment efficiency and showed lower extent of in vitro drug release (40% over 48 h). The Gal-PLGA nanoparticles were remarkably targeted to the liver, and keep at a high level during the experiment. The accumulation in the liver was 36.71±0.68% at 24 h after administration. The Gal-PLGA nanoparticles were remarkably targeted to the liver, and keep at a high level during the experiment. The accumulation in the liver was 36.71±0.68% at 24 h after administration.

Conclusion: These results suggest that Gal-PLGA-NPs are safe and potentially promising for hepatocyte-selective targeting.

KEYWORDS: Galactosylation, Galactosylated-PLGA-Nanoparticles, Liver-Targeting, asialoglycoprotein, Acyclovir.