Preparation, in-vitro and in-vivo characterisation of CoQ10 microparticles: electrospraying-enhanced bioavailability

J Pharm Pharmacol. 2016 Feb;68(2):159-69. doi: 10.1111/jphp.12502. Epub 2016 Jan 4.

Abstract

Objectives: This study aimed to prepare Coenzyme Q10 (CoQ10) microparticles using electrospraying technology, and evaluate the in-vitro properties and in-vivo oral bioavailability.

Key findings: Electrospraying was successfully used to prepare CoQ10 to enhance its solubility and dissolution properties. In-vitro evaluation of the electrosprayed microparticles showed bioavailability-enhancing properties such as reduced crystallinity and particle size. The formulation was evaluated using dissolution study and in-vivo oral bioavailability using rat model. The dissolution study revealed enhanced dissolution properties of electrosprayed microparticles compared with physical mixture and raw material. The absorption profiles showed increasing mean plasma levels CoQ10 in the following order: raw material < physical mixture < electrosprayed microparticles.

Conclusion: Based on the findings in this study, electrospraying is a highly prospective technology to produce functional nano- and micro-structures as delivery vehicles for drugs with poor oral bioavailability due to rate-limiting solubility.

Keywords: CoQ10; amorphisation; bioavailability; dissolution; electrospraying; microparticles.

MeSH terms

  • Absorption, Physiological
  • Administration, Oral
  • Animals
  • Biological Availability
  • Electrochemical Techniques / instrumentation
  • Electrochemical Techniques / methods*
  • Equipment Design
  • Male
  • Microscopy, Electron, Scanning
  • Particle Size
  • Rats, Sprague-Dawley
  • Solubility
  • Surface Properties
  • Technology, Pharmaceutical / instrumentation
  • Technology, Pharmaceutical / methods*
  • Ubiquinone / administration & dosage
  • Ubiquinone / analogs & derivatives*
  • Ubiquinone / blood
  • Ubiquinone / chemistry

Substances

  • Ubiquinone
  • coenzyme Q10