Formulating Self Phospholipids Dispersion of Poorly Water-Soluble Drug to Enhance Oral Bioavailability

Abstract

In present study, self-nano phospholipid dispersion (SNPD) of Simvastatin (SIM) was prepared based on Phosal 53 MCT to improve the oral bioavailability. Ternary phase diagrams were constructed to evaluate the efficient nanoemulsion regions and also for the optimum concentrations of lipid (Phosal 53 MCT) and surfactant (Cremophore RH 40), co-surfactant (Gelucire 50/13) and water in the formulation. The globule size of SNPD batch A was found to be 115.7 nm, while zeta potential of final SNPD batch A was found to be 5.3 mV. Formulations were evaluated using DSC, XRD, SEM as well as in vitro drug release. In vitro dissolution profile of SNPD batch A powder showed 1.3% drug release in 60 min while simvastatin showed 0.7% drug release in min. which suggests that batch A has superior dissolution rather than simvastatin. The in vivo oral absorption of selected formulation was greater in comparison to pure drug powder, as was evaluated in Wistar rats. SIM-SNPD is found to be more bioavailable with greater relative bioavailability as compared with pure drug powder during an in vivo study in rats. These formulations might be new alternative carriers that enhance the oral bioavailability of poorly water-soluble molecules, such as SIM.

Keywords: Bioavailability, nano-dispersion, in vivo evaluation, phospholipid, Simvastatin

Cite this Article

S.K. Kamble, S.S. Shinde. Formulating Self Phospholipids Dispersion of Poorly Water-Soluble Drug to Enhance Oral Bioavailability. Research & Reviews: A Journal of Pharmaceutical Science. 2019; 10(3): 24–33p.