Abstract

PREPARATION AND CHARACTERIZATION OF SOFOSBUVIR LOADED CHITOSANTRIPOLYPHOSPHATE MUCOADHESIVE MICROSPHERES

Reenu Patwa^*1, Sandesh Asati¹, Shailendra Lariya¹, Geeta Parkhe²

¹Radhraman College of Pharmacy, Bhopal (M.P.)

²Scan Research laboratories Bhopal (M.P.)

ABSTRACT

Hepatitis C virus (HCV) infection is a major cause of end-stage liver disease and hepatocellular carcinoma. The advent of direct-acting antiviral treatments for chronic hepatitis C infection has dramatically increased rates of cure. The aim of the present study was to develop sofosbuvir loaded chitosan microspheres by the ionic gelation method using sodium tripolyphosphate (Na-TPP) as the crosslinking agent. The use of ionotropic gelation avoids the possibility of the occurrence of the toxic and undesirable effects associated with the use of glutaraldehyde, a chemical crosslinking agent. The prepared microspheres were evaluated for mean particle size and particle size distribution, drug loading, encapsulation efficiency and in-vitro drug release. FT-IR spectroscopic analysis was performed to ascertain drug polymer interaction. The release profiles showed zero-order release behavior up to 12 hours where the highest drug release was 99.78 % of the sofosbuvir loaded in the chitosan microspheres, indicating a strong crosslinking between chitosan and TPP anions. The surface morphology of the prepared microspheres was studied by SEM. With an increase in the crosslinking density the rate of drug release decreased. From the results of the present investigation it may be concluded that drug loaded chitosan microspheres can be prepared by a simple technique which avoids the use of complex apparatus and special precautions.

Keywords: Hepatitis C virus, Sofosbuvir, Microspheres, Chitosan, Sodium tripolyphosphate