Compounding of a topical drug with prospective natural surfactant-stabilized pharmaceutical bases: physicochemical and in vitro/in vivo characterization--a ketoprofen case study

Eur J Pharm Biopharm. 2012 Jan;80(1):164-75. doi: 10.1016/j.ejpb.2011.09.001. Epub 2011 Sep 10.

Abstract

Recently, healthcare professionals again began realizing the benefits of preparing customized medications to meet specific patient needs. The objective of this work was to develop and evaluate simple pharmaceutical bases stabilized with natural-origin surfactant of alkyl polyglucoside (APG) type as prospective ready-to-use bases and compare them to widely used pharmacopoeial ones. Additionally, the ability of the formulated bases to sustain isopropyl alcohol was assessed as well as its influence on ketoprofen skin absorption (as a co-solvent and potential penetration enhancer). In order to evaluate the manifold characteristics a topical drug product should possess, a comprehensive characterization was performed using different techniques. Physicochemical characterization demonstrated satisfactory physical stability of APG-stabilized bases upon the addition of alcohol. In vitro release/permeation studies failed to show significant difference in ketoprofen liberation/permeation profiles from different bases. However, the extent of ketoprofen delivery in vivo was clearly increased from APG bases, relative to that obtained from pharmacopoeia quality one, implying a distinct influence of the emulsion systems' colloidal structures. Taking also into account the rheological behavior of APG bases, revealing their ameliorated sensory characteristics, it could be concluded that the investigated APG bases could be considered as preferential option in drug compounding related to the conventional ones.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2-Propanol / chemistry
  • Administration, Topical
  • Adult
  • Chemistry, Pharmaceutical / methods
  • Colloids / chemistry
  • Colloids / pharmacology
  • Drug Compounding / methods
  • Emulsions / chemistry
  • Emulsions / pharmacology
  • Female
  • Humans
  • Ketoprofen / chemistry*
  • Ketoprofen / pharmacokinetics
  • Ketoprofen / pharmacology*
  • Male
  • Permeability
  • Prospective Studies
  • Rheology / methods
  • Skin / drug effects*
  • Skin / metabolism*
  • Skin Absorption
  • Skin, Artificial
  • Solvents / chemistry
  • Surface-Active Agents / chemistry*
  • Surface-Active Agents / pharmacokinetics
  • Surface-Active Agents / pharmacology
  • Young Adult

Substances

  • Colloids
  • Emulsions
  • Solvents
  • Surface-Active Agents
  • Ketoprofen
  • 2-Propanol