Coaxial electrospray formulations for improving oral absorption of a poorly water-soluble drug

Mol Pharm. 2011 Jun 6;8(3):807-13. doi: 10.1021/mp100401d. Epub 2011 Mar 25.

Abstract

Development of oral dosage forms containing poorly water-soluble drugs is a major challenge in the pharmaceutical industry. This paper describes the use of coaxial electrospray deposition as a promising formulation technology for oral delivery of poorly water-soluble drugs. The technology produced core-shell particles composed of griseofulvin and poly(methacrylic acid-co-methyl methacrylate) (Eudragit L-100), with a diameter of around 1 μm. The drug phase was in an amorphous state when the griseofulvin core was coated with the Eudragit L-100 shell. The in vitro dissolution and in vivo oral absorption studies revealed that the core-shell formulation significantly improved dissolution and absorption behaviors, presumably because of a reduction in particle size, improvement in dispersity, and amorphization. Results demonstrated that coaxial electrospray deposition possesses great potential as novel formulation technology for enhancing oral absorption of poorly water-soluble drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral*
  • Animals
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Griseofulvin / administration & dosage*
  • Griseofulvin / chemistry
  • Griseofulvin / pharmacokinetics*
  • Male
  • Microscopy, Electron, Scanning
  • Rats
  • Rats, Sprague-Dawley
  • Solubility
  • X-Ray Diffraction

Substances

  • Griseofulvin