Physicochemical characterization and in vivo evaluation of solid self-nanoemulsifying drug delivery system for oral administration of docetaxel

J Microencapsul. 2013;30(4):307-14. doi: 10.3109/02652048.2012.726280. Epub 2012 Oct 26.

Abstract

To formulate a self-nanoemulsifying drug delivery system (SNEDDS) for the oral administration of docetaxel as an alternative to commercial docetaxel-loaded injectable products, it was prepared by spray-drying an aqueous solution containing liquid SNEDDS and colloidal silica. Its physicochemical properties and oral bioavailability were investigated compared to a clear docetaxel solution administered intravenously or orally to rats. In the docetaxel-loaded solid SNEDDS prepared with colloidal silica, the liquid SNEDDS composed of Capryol 90, Cremophore EL and Transcutol HP (45/35/20, volume ratio) was absorbed inside the pores of carriers, and docetaxel was present in a changed amorphous state. The solid SNEDDS with 3.3% (w/v) docetaxel produced nanoemulsions, and showed about 12.5% absolute bioavailability in rats. Thus, this solid SNEDDS may be a potential candidate for oral pharmaceutical product with improved oral bioavailability of docetaxel.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacokinetics
  • Antineoplastic Agents* / pharmacology
  • Biological Availability
  • Docetaxel
  • Drug Delivery Systems
  • Emulsions
  • Male
  • Nanoparticles / chemistry*
  • Rats, Sprague-Dawley
  • Silicon Dioxide* / chemistry
  • Silicon Dioxide* / pharmacokinetics
  • Silicon Dioxide* / pharmacology
  • Taxoids* / chemistry
  • Taxoids* / pharmacokinetics
  • Taxoids* / pharmacology

Substances

  • Antineoplastic Agents
  • Emulsions
  • Taxoids
  • Docetaxel
  • Silicon Dioxide