Development of olmesartan medoxomil lipid-based nanoparticles and nanosuspension: preparation, characterization and comparative pharmacokinetic evaluation

Artif Cells Nanomed Biotechnol. 2018 Feb;46(1):126-137. doi: 10.1080/21691401.2017.1299160. Epub 2017 Mar 14.

Abstract

The aim was to enhance the oral bioavailability of olmesartan medoxomil (OM) by preparing solid lipid nanoparticles (SLNs) and comparing with nanosuspension (OM-NS). OM-SLNs and OM-NS were prepared by known methods. Prepared SLNs were evaluated for physical characters and in vivo pharmacokinetic (PK) performance in rats. OM-NS showed more than four-fold increase in the solubility. During DSC and XRD studies, drug incorporated in SLNs was found to be in amorphous form. The relative bioavailability of OM-SLN and OM-NS was 7.21- and 3.52-fold when compared with that of coarse suspension. Further, OM-SLNs also increased the oral bioavailability by two-fold over that of OM-NS.

Keywords: Olmesartan medoxomil; bioavailability; nanosuspension; pharmacokinetics; solid lipid nanoparticles.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Biological Availability
  • Drug Carriers / chemistry*
  • Drug Carriers / pharmacokinetics*
  • Lipids / chemistry*
  • Lipids / pharmacokinetics*
  • Male
  • Nanoparticles / chemistry*
  • Olmesartan Medoxomil / chemistry*
  • Particle Size
  • Rats
  • Rats, Wistar
  • Solubility
  • Suspensions

Substances

  • Drug Carriers
  • Lipids
  • Suspensions
  • Olmesartan Medoxomil