Dissolution and oral absorption of pranlukast nanosuspensions stabilized by hydroxypropylmethyl cellulose

Int J Biol Macromol. 2014 Jun:67:53-7. doi: 10.1016/j.ijbiomac.2014.03.006. Epub 2014 Mar 13.

Abstract

The objective of this study was to investigate the effect of particle size on the dissolution and oral absorption of pranlukast microsuspensions and nanosuspensions stabilized by hydroxypropylmethyl cellulose. Four pranlukast suspensions with different mean particle sizes (0.16, 0.89, 3.13, and 18.21μm) were prepared by various top-down processes such as jet milling, high pressure homogenization, and bead milling. The dissolution rate and oral absorption of pranlukast suspensions were significantly affected by the particle size. The in vivo pharmacokinetic parameters of pranlukast suspensions were increased with decreasing mean particle size of suspensions. Especially, the AUC0→24h and Cmax values of pranlukast nanosuspension with a particle size of 0.16μm were approximately 3.5- and 6.3-fold greater, respectively, than that of pranlukast microsuspension with a particle size of 18.21μm. Therefore, the preliminary results from our study suggest that a pranlukast nanosuspension with a mean particle size of about 0.16μm may have significant potential for clinical application.

Keywords: Bioavailability; Nanosuspenion; Pranlukast.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Chromones / administration & dosage
  • Chromones / chemistry*
  • Drug Liberation
  • Humans
  • Hypromellose Derivatives / administration & dosage
  • Hypromellose Derivatives / chemistry*
  • Nanostructures / administration & dosage
  • Nanostructures / chemistry*
  • Particle Size
  • Suspensions / administration & dosage
  • Suspensions / chemistry

Substances

  • Chromones
  • Suspensions
  • Hypromellose Derivatives
  • pranlukast