Development and in vitro evaluation of solid dispersions as strategy to improve albendazole biopharmaceutical behavior

Ther Deliv. 2018 Sep;9(9):623-638. doi: 10.4155/tde-2018-0037.

Abstract

Aim: Solid dispersions using Poloxamer 407 as carrier were developed to improve albendazole (ABZ) solubility and dissolution profiles.

Methods: ABZ/poloxamer solid dispersions were prepared, and dissolution profiles were mathematically modeled and compared with physical mixtures, pharmaceutical ABZ and a commercial formulation.

Results: Poloxamer 407 increased exponentially ABZ solubility, in about 400% when 95% w/w of polymer compared with its absence. Solid dispersions initial dissolution rate was three to 20-fold higher than physical mixtures, the drug and the commercial formulation. All the solid dispersions required less than 2.2 min to reach an 80% of ABZ dissolution, while the commercial formulation needed around 40 min.

Conclusion: Solid dispersions improved ABZ solubility and dissolution rate, which could result in a faster absorption and an increased bioavailability.

Keywords: albendazole; dissolution efficiency; initial dissolution rate; lumped model; poloxamer; solid dispersions; solubility.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Absorption, Physicochemical
  • Albendazole / administration & dosage
  • Albendazole / chemistry
  • Albendazole / pharmacokinetics*
  • Biological Availability
  • Chemistry, Pharmaceutical
  • Drug Carriers / chemistry*
  • Drug Compounding / methods
  • Drug Liberation*
  • Poloxamer / chemistry*
  • Solubility

Substances

  • Drug Carriers
  • Poloxamer
  • Albendazole