Abstract

TARGETED DELIVERY OF ANTIVIRAL DRUG VIA SURFACE ANTIGEN DOCKED VESICULAR CONSTRUCT FOR EFFECTIVE MANAGEMENT OF HEPATITIS

Tushar Sambre*, Tanvi Sambre and Shivprasad Mujumdar

ABSTRACT

The intrinsic liver tropism of liposomes can be augmented by the addition of targeting features such as the incorporation of hepatotropic elements of the hepatitis viruses. Liposome containing acyclovir appended with HBsAg deliver the acyclovir to hepatocytes through specific binding to a receptor present on the surface of hepatocyte. In the present study, we evaluated the functional ability of HBsAg to be employed as a ligand for targeting hepatocyte.Acyclovir (ACV) is an antiviral drug which is given orally and parenterally. One of the most crucial problems which are encountered with oral administration of ACV is the rapid first pass metabolism of the drug resulting in poor bioavailability (upto 30%). In case of plain liposomal formulation drug released found to be 35.3±2.3% after 24 hr. where as in case of HBsAg coated liposomal formulation drug release was found to be 39.8±2.6% after 24 hr. The results strongly suggest that liver uptake of ligand appended liposomes was comparative more than plain liposomal formulation. Immunological response to protein immobilized on the surface of liposome (NS-3DD) was significantly lower as compared to immunological response of plain HBsAg. The body distribution study revealed that 47.2%of the dose recovered in the liver after administration of HBsAg coated liposome while 35.85% and 4.69 % were recovered after plain liposomal and acyclovir respectively. These result indicated that liposome containing acyclovir appended with HBsAg had strong liver targeting property, suggesting that this novel carrier system containing antiviral drug could be used for delivery drug to treat liver diseases.

Keywords: Nanotechnology; liposomes; Acyclovir; Hepatitis B surface antigen (HBsAg); Anti-HBV activity.