Formulation of lyophilized oily-core poly-Ɛ-caprolactone nanocapsules to improve oral bioavailability of Olmesartan Medoxomil

Authors:
Publisher website
Google Scholar
Abstract
Objective: This study aims to detect the enhancement in oral bioavailability of a poorly water-soluble antihypertensive drug Olmesartan Medoxomil (OM) due to formulation of lyophilized oily-core nanocapsules. Significance: A comparative pharmacokinetics study in rats was conducted for oily-core polymeric nanocapsules (ONC) after formulation and lyophilization against market tablet product to show the significant improvement in oral absorption of OM. Materials and methods: OM loaded ONC were prepared using poly-Ɛ-caprolactone (0.5% w/v) as a polymer and an oily core of Labrafac PG® by applying a well-controlled nanoprecipitation technique in terms of injection rate (80 mL/h) and magnetic stirring rate (300 rpm). The prepared lyophilized ONC were in-vitro characterized after reconstitution and evaluated in-vivo for oral bioavailability after a single OM oral dose (20 mg/kg) of reconstituted lyophilized ONC dispersion was administered to rats. Results: The prepared lyophilized ONC containing 10% w/v mannitol showed an average particle size of 158 nm, polydispersity index of 0.37, negative zetapotential value equals 33.9 and entrapment efficiency of 90%. Dissolution profile for OM from lyophilized ONC powder filled into hard gelatin capsules (HGC) showed 1.8-fold increase in dissolution rate as compared to the pure drug. In-vivo pharmacokinetics study in rats revealed a significant enhancement in oral bioavailability of OM with 1.6-fold increase for AUC0-24 and 1.9-fold increase for Cmax as compared to marketed product. Conclusion: It is concluded that formulation of lyophilized ONC for OM can significantly enhance its oral bioavailability and consequently, its therapeutic efficacy and patient compliance.

This publication has 20 references indexed in Scilit: