Enhanced bioavailability of orally administered flurbiprofen by combined use of hydroxypropyl-cyclodextrin and poly(alkyl-cyanoacrylate) nanoparticles

Eur J Drug Metab Pharmacokinet. 2014 Mar;39(1):61-7. doi: 10.1007/s13318-013-0138-9. Epub 2013 May 23.

Abstract

Flurbiprofen was formulated into nanoparticle suspension to improve its oral bioavailability. Hydroxypropyl-β-cyclodextrin inclusion-flurbiprofen complex (HP-β-CD-FP) was prepared, then incorporating this complex into poly(alkyl-cyanoacrylate) (PACA) nanoparticles. HP-β-CD-FP-PACA nanoparticle was prepared by the emulsion solvent polymerization method. The zeta potential was -26.8 mV, the mean volume particle diameter was 134 nm, drug encapsulation efficiency was 53.3 ± 3.6 % and concentration was 1.5 mg/mL. The bioavailability of flurbiprofen from optimized nanoparticles was assessed in male Wistar rats at a dose of 15 mg/kg. As compared to the flurbiprofen suspension, 211.6 % relative bioavailability was observed for flurbiprofen nanoparticles. The reduced particle size and increased surface area may contribute to improve oral bioavailability of flurbiprofen.

Publication types

  • Comparative Study

MeSH terms

  • 2-Hydroxypropyl-beta-cyclodextrin
  • Administration, Oral
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Biological Availability
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Crystallography, X-Ray
  • Cyanoacrylates / chemistry*
  • Drug Carriers*
  • Emulsions
  • Flurbiprofen / administration & dosage*
  • Flurbiprofen / chemistry
  • Flurbiprofen / pharmacokinetics*
  • Male
  • Nanoparticles*
  • Particle Size
  • Powder Diffraction
  • Rats
  • Rats, Wistar
  • Solvents / chemistry
  • Surface Properties
  • beta-Cyclodextrins / chemistry*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyanoacrylates
  • Drug Carriers
  • Emulsions
  • Solvents
  • beta-Cyclodextrins
  • 2-Hydroxypropyl-beta-cyclodextrin
  • Flurbiprofen