Abstract

COMPARATIVE STUDIES OF EXEMESTANE PROLIPOSOMES FOR IMPROVED ORAL DELIVERY

*Rajesh Kumar N.

ABSTRACT

The aim of these studies was to develop proliposomal formulations to enhance the oral bioavailability of exemestane by improving solubility, dissolution. Exemestane is a novel oral steroidal aromatase inactivator, which showed promising antitumor activity in postmenopausal women with hormonal sensitive (estrogen dependent) breast cancer. Proliposomal powder formulations were prepared using different ratios of drug (exemestane), phosphatidylcholine (PC), cholesterol and different grade of polyethylene glycol (PEG) by solvent evaporation method. The effect of phospholipid composition, different grade of polyethylene glycol and drug:lipid ratio on in vitro performance of proliposomes was studied. Proliposomes provided enhanced exemestane dissolution due to incorporation into the phospholipid bilayers, polyethelene glycol and change in the physical state from crystalline to amorphous. The in vitro dissolution studies revealed that the polyethylene glycol 4000 contains the proliposomes were successful in enhancing the permeation of exemestane. These proliposomal formulations of exemestane could provide improved oral bioavailability due to enhanced solubility, permeability and hence absorption.

Keywords: .