Formulation Development and Evaluation of Liposphere of Poor Water Soluble Drug for Hyperlipidemia

Abstract

Lipospheres offer a new approach to improve an aqueous solubility of BCS class-II drugs. Simvastatin is a third generation fibric acid derivative belonging to this class, employed clinically as a hypolipidemic agent to lessen the risk caused by atherosclerosis. An attempt was made to improve aqueous solubility of Simvastatin by aid of stearic acid and Paraffin oil. The factorial batches of the Simvastatin lipospheres were formulated by melt dispersion technique using 32 factorial design with variables X1- concentration of stearic acid and X2- concentration of paraffin oil and responses Y1 - % Drug Entrapment (% DE) and Y2 - % Drug Release (% DR). From the surface response graphs the optimized batch was formulated and evaluated for saturation solubility, in-vitro drug release studies. Significant improvement in the aqueous solubility of the drug in the Simvastatin lipospheres supports the applicability of lipospheres as a tool for improving aqueous solubility of the BCS class-II drugs.
 Keywords: Linospheres; Simvastatin; Drug release; Hyperlipidemic; Drug entrapment.

Lipospheres and Pro-Nanolipospheres: Advancements in Drug Delivery Systems

“…Their internal core contains the drug dissolved or dispersed, and their particle sizes range from 0.01 to 100 µm. (Bekerman et al, 2004;Elgart et al, 2012;Khopade & Jain, 1997) Lipospheres are one of the lipid-based drug delivery systems complying well with the needs of a drug delivery system, as they have high dispersibility in aqueous media, easy in their preparation and scaling up, and their high ability to entrap hydrophobic drugs; enhancing the solubility and permeability characteristics of especially class II and IV drug candidate (Ganesan & Allimalarkodi, 2015;Kumar et al, 2021).…”