Oral absorption of a valsartan-loaded spray-dried emulsion based on hydroxypropylmethyl cellulose

Int J Biol Macromol. 2014 Aug:69:222-8. doi: 10.1016/j.ijbiomac.2014.05.059. Epub 2014 May 28.

Abstract

The aim of this study was to develop a novel valsartan-loaded spray-dried emulsion based on hydroxypropylmethyl cellulose (HPMC) with enhanced oral absorption. The valsartan-loaded redispersible dry emulsion was prepared by using a high-pressure homogenization and spray-drying process with water, Capryol 90, HPMC, and different surfactants, based on the results of the solubility study. The spray-dried emulsions formed small and homogeneous emulsions with a mean droplet emulsion size ranging from 133.5 to 152.5nm at the dispersion state in water. The valsartan-loaded redispersible dry emulsion with HPMC/poloxamer 407 showed enhanced pH-independent valsartan release, resulting in a dramatically enhanced oral bioavailability of valsartan compared to the raw material and commercial product. Therefore, a formulation strategy using the redispersible dry emulsion with HPMC/poloxamer 407 is very effective for the development of a new dosage form containing valsartan.

Keywords: Bioavailability; Dry emulsion; Valsartan.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Absorption, Physicochemical*
  • Administration, Oral
  • Animals
  • Desiccation*
  • Drug Carriers / chemistry*
  • Emulsions
  • Hypromellose Derivatives / chemistry*
  • Male
  • Oils / chemistry
  • Rats
  • Rats, Sprague-Dawley
  • Surface-Active Agents / chemistry
  • Tetrazoles / administration & dosage
  • Tetrazoles / chemistry*
  • Tetrazoles / pharmacokinetics*
  • Valine / administration & dosage
  • Valine / analogs & derivatives*
  • Valine / chemistry
  • Valine / pharmacokinetics
  • Valsartan
  • Water / chemistry

Substances

  • Drug Carriers
  • Emulsions
  • Oils
  • Surface-Active Agents
  • Tetrazoles
  • Water
  • Hypromellose Derivatives
  • Valsartan
  • Valine