A dynamic topical hydrofluoroalkane foam to induce nanoparticle modification and drug release in situ

Eur J Pharm Biopharm. 2009 Aug;72(3):521-8. doi: 10.1016/j.ejpb.2009.03.002. Epub 2009 Mar 19.

Abstract

Topical nanoparticles are usually applied using semi-solid formulations, but the delivery process is often inefficient due to the poor drug release from the particles. The aim of this study was to investigate the capability of a dynamic foam to break open nanoparticles upon application to the skin and enhance drug delivery efficiency. Vitamin E acetate (VEAc) was selected as a model drug and loaded into lipid nanoparticles (50-60 nm) prepared by phase inversion. The highest drug loading was 18.9+/-1.2 mg/ml and the corresponding encapsulation efficiency was 81.5+/-4.1%. Dynamic foams were generated by emulsifying VEAc-loaded nanoparticle suspensions with hydrofluoroalkane using pluronic L62D. An in vitro permeation study demonstrated that VEAc did not release from the nanoparticles when administered as an aqueous suspension, but attained a flux of 18.0+/-2.1 (microg cm(-2) h(-1)) when applied using the foam. Drug release from the foam was shown to be a consequence of nanoparticle modification after dose administration and this led to the foam delivering 0.7+/-0.3% VEAc into the stratum corneum (SC) when applied to human skin.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Aerosol Propellants / administration & dosage*
  • Aerosol Propellants / pharmacokinetics
  • Drug Carriers / administration & dosage*
  • Drug Carriers / pharmacokinetics
  • Humans
  • Hydrocarbons, Fluorinated / administration & dosage*
  • Hydrocarbons, Fluorinated / pharmacokinetics
  • In Vitro Techniques
  • Nanoparticles / administration & dosage*
  • Skin Absorption / drug effects
  • Skin Absorption / physiology

Substances

  • Aerosol Propellants
  • Drug Carriers
  • Hydrocarbons, Fluorinated
  • apaflurane