Improved Intestinal Absorption and Bioavailability Enhancement of Rosuvastatin Calcium via Proliposome Powder

Abstract

The main objective of the present study was to develop proliposomal formulations to enhance the oral bioavailability of rosuvastatin calcium by improving solubility, dissolution and/or intestinal permeability. Proliposomal powder formulations were prepared with drug varying the Phospholipon 90H and cholesterol ratio in the range of 1:0 to 1:1 using pearlitol SD200 as carrier by film deposition method. The prepared proliposomal powder was filled into capsules. The bioavailability enhancement of proliposomes loaded with drug was studied focusing on phospholipid composition and drug:lipid ratio. Prepared proliposomes were characterized for their particle size distribution, zeta potential, entrapment efficiency, in vitro dissolution study and thermal characteristics to understand the phase transition behavior. Further, the formulated proliposomes were subjected to stability behaviour, ex vivo permeation studies using rat intestine followed by in vivo studies. Physicochemical studies help in optimization of formulations. Enhancement in dissolution is due to incorporation of rosuvastatin calcium into the phospholipids and change in the physical state from crystalline to amorphous, thus improving oral bioavailability. Ex vivo studies show significant permeation enhancement across gastrointestinal membrane compared to control. In conclusion, proliposomes provide a powerful and functional way of distribution of inadequately soluble rosuvastatin calcium drug which is proved from in vivo studies based on the enhanced oral delivery.

Keywords: Proliposomes, cholesterol, liposomes, permeability, bioavailability

Cite this Article

Smitha Gandra, S. Sharath C. Reddy, S. Nagasri, V. Vyshnavi, Raju Jukanti. Improved Intestinal Absorption and Bioavailability Enhancement of Rosuvastatin Calcium via Proliposome Powder. Research & Reviews: A Journal of Drug Formulation, Development and Production. 2020; 7(3): 23–40p.