Cubic phase nanoparticles for sustained release of ibuprofen: formulation, characterization, and enhanced bioavailability study

Int J Nanomedicine. 2013:8:845-54. doi: 10.2147/IJN.S40547. Epub 2013 Feb 26.

Abstract

In order to improve the oral bioavailability of ibuprofen, ibuprofen-loaded cubic nanoparticles were prepared as a delivery system for aqueous formulations. The cubic inner structure was verified by cryogenic transmission electron microscopy. With an encapsulation efficiency greater than 85%, the ibuprofen-loaded cubic nanoparticles had a narrow size distribution around a mean size of 238 nm. Differential scanning calorimetry and X-ray diffraction determined that ibuprofen was in an amorphous and molecular form within the lipid matrix. The in vitro release of ibuprofen from cubic nanoparticles was greater than 80% at 24 hours, showing sustained characteristics. The pharmacokinetic study in beagle dogs showed improved absorption of ibuprofen from cubic nanoparticles compared to that of pure ibuprofen, with evidence of a longer half-life and a relative oral bioavailability of 222% (P < 0.05). The ibuprofen-loaded cubic nanoparticles provide a promising carrier candidate with an efficient drug delivery for therapeutic treatment.

Keywords: bioavailability; cubic nanoparticles; ibuprofen; oral drug delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Area Under Curve
  • Biological Availability
  • Delayed-Action Preparations
  • Dogs
  • Drug Carriers / administration & dosage*
  • Drug Carriers / chemistry*
  • Drug Carriers / pharmacokinetics
  • Female
  • Ibuprofen / administration & dosage*
  • Ibuprofen / blood
  • Ibuprofen / chemistry*
  • Ibuprofen / pharmacokinetics
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Particle Size

Substances

  • Delayed-Action Preparations
  • Drug Carriers
  • Ibuprofen