Abstract

FORMULATION AND EVALUATION OF LIPOSPHERES FOR ANTIRETROVIRAL THERAPY

Smita Sachin Pimple*, Khilchandra Ganesh Bhirud, Angira Gaurav Purohit

ABSTRACT

Lipospheres of lopinavir (LPV) and ritonavir (RTV) were prepared by melt dispersion technique using Compritol® 888 ATO as lipid matrix and Poloxamer 407 and Phospholipon 90G as surfactant. Drug entrapped free flowing lipospheres of LPV and RTV were obtained after optimization using 3 2 factorial design and characterized for entrapment efficiency, particle size distribution, differential scanning calorimetry (DSC), X-ray diffraction (XRD), scanning electron microscopy (SEM) and in vitro release and stability studies. Entrapment efficiencies of 81.5 ± 0.21% and 96.93 ± 0.81% were obtained for optimized formulations of LPV lipospheres (LPVL) and RTV lipospheres (RTVL) respectively. Particle size of LPVL and RTVL were found to be 9.926 ± 1.03 μm and 7.756 ± 0.21 μm respectively. DSC and XRD results confirmed the drug entrapment in lipospheres. SEM studies revealed the spherical shape of lipospheres and in vitro release studies showed sustained drug release. Lipospheres drug delivery system proved to be promising for anti-retroviral therapy.

Keywords: Lopinavir, Ritonavir, Lipospheres, Entrapment, Particle size.