Abstract :
The aim of the present study was to develop proliposomal formulations to enhance the oral bioavailability of agomelatin by
improving solubility, dissolution and/or intestinal permeability. Proliposomal powder formulations were prepared using
different ratios of agomelatin, phospholipon 90H and cholesterol by solvent evaporation method. The effect of phospholipid
composition and drug:lipid ratio on in vitro performance of proliposomes was studied. Proliposomes were characterized for
their particle size distribution, zeta potential, micromeritics, and entrapment efficiency. Further, the formulated proliposomes
were subjected to in vitro drug release performance in both simulated gastric and intestinal fluid demonstrate improved
dissolution characteristics compared to pure drug. Multimedia dissolution profiles were carried out to demonstrate enhanced
dissolution characteristics compared to pure drug. Proliposomes provided enhanced agomelatin dissolution due to
incorporation into the phospholipid bilayers and change in the physical state from crystalline to amorphous. These
proliposomal formulations of agomelatin could provide improved oral bioavailability due to enhanced solubility, permeability
and enhanced absorption.
Keywords: Proliposomes, agomelatin, perfusion, bioavailability, Dissolution, Permeability
Keyword :
Proliposomes, agomelatin, perfusion, bioavailability, Dissolution, Permeability