Enhancement of solubility and therapeutic potential of poorly soluble lovastatin by SMEDDS formulation adsorbed on directly compressed spray dried magnesium aluminometasilicate liquid loadable tablets: A study in diet induced hyperlipidemic rabbits

Abstract

The aim of present study was to formulate and evaluate a self-microemulsifying drug delivery systems (SMEDDS) containing lovastatin and to further explore the ability of porous Neusilin® US2 tablet as a solid carrier for SMEDDS. SMEDDS formulations of varying proportions of peceol, cremophor RH 40 and transcutol-P were selected and subjected to in-vitro evaluation, including dispersibility studies, droplet size, zeta potential measurement and release studies. The results indicated that the drug release profile of lovastatin from SMEDDS formulations was statistically significantly higher (p-value < 0.05) than the plain lovastatin powder. Thermodynamic stability studies also confirmed the stability of the prepared SMEDDS formulations. The optimized formulation, which consists of 12% of peceol, 44% of cremophor RH 40, and 44% of transcutol-P was loaded into directly compressed liquid loadable tablet of Neusilin® US2 by simple adsorption method. In order to determine the ability of Neusilin® US2 as a suitable carrier pharmacodynamics study were also carried out in healthy diet induced hyperlipidemic rabbits. Animals were administered with both liquid SMEDDS and solid SMEDDS as well. From the results obtained, Neusilin® was found to be a suitable carrier for SMEDDS and was equally effective in reducing the elevated lipid profile. In conclusion, liquid loadable tablet (LLT) is predicted to be a promising technique to deliver a liquid formulation in solid state.

Keywords

• Lovastatin
• Self-microemulsifying drug delivery system (SMEDDS)
• Neusilin® US2
• Liquid loadable tablet
• Solid carrier system
• Pharmacodynamics studies