Dissolution and bioavailability of lercanidipine-hydroxypropylmethyl cellulose nanoparticles with surfactant

Int J Biol Macromol. 2015 Jan:72:218-22. doi: 10.1016/j.ijbiomac.2014.08.017. Epub 2014 Aug 23.

Abstract

The objective of this study was to develop lercanidipine-hydroxypropylmethyl cellulose (HPMC) nanoparticles with high oral bioavailability. The lercanidipine-HPMC nanoparticles with/without surfactants were manufactured using a supercritical antisolvent (SAS) process. Gelucire 44/14, poloxamer 407, and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) were evaluated as surfactants. Spherical lercanidipine-HPMC nanoparticles with a mean particle size less than 400 nm were successfully prepared using a SAS process. The dissolution and oral bioavailability of lercanidipine was significantly increased by addition of surfactants. Especially lercanidipine-HPMC nanoparticles with TPGS showed a 2.47-fold higher oral bioavailability than raw material. Furthermore, the dissolution efficiency was strongly correlated to the in vivo Cmax and AUC0 → 24h. Therefore, the preparation of HPMC nanoparticles with TPGS using a SAS process is a highly effective formulation strategy for enhanced oral bioavailability of lercanidipine.

Keywords: Bioavailability; Lercanidipine; Nanoparticle.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Biological Availability*
  • Dihydropyridines / administration & dosage
  • Dihydropyridines / chemistry*
  • Drug Compounding
  • Humans
  • Hypromellose Derivatives / administration & dosage
  • Hypromellose Derivatives / chemistry*
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Particle Size
  • Poloxamer / chemistry
  • Polyethylene Glycols / chemistry
  • Solubility
  • Vitamin E / chemistry

Substances

  • Dihydropyridines
  • Poloxamer
  • gelucire 44-14
  • Vitamin E
  • Hypromellose Derivatives
  • Polyethylene Glycols
  • tocophersolan
  • lercanidipine