Permeation and skin retention of quercetin from microemulsions containing Transcutol® P

Drug Dev Ind Pharm. 2012 Sep;38(9):1128-33. doi: 10.3109/03639045.2011.641564. Epub 2011 Dec 22.

Abstract

A microemulsion for the cutaneous release of quercetin was prepared. An aqueous phase, containing 40% Transcutol® P as solubilizing agent and permeation enhancer, was emulsified with Labrafil® as oil phase and Labrasol®/Capryol™ 90 as Solvent/Co-solvent. Quercetin was dissolved in the microemulsion at the concentration of 1%. Ternary phase diagrams were generated to determine the optimal concentration of each excipient composing the microemulsion. The physicochemical properties of the microemulsion, such as pH, viscosity, refractive index, and particle size distribution were determined. The microemulsion was stable for 12 months at the storing conditions of 25.0 ± 1.0°C. The in vitro quercetin permeability into and through the abdominal hairless pig skin was determined by vertical Franz's cells. Quercetin showed hardly any permeability through the skin when dissolved in water- and Transcutol® P-free media, whereas a remarkable increase in cutaneous permeability was observed when quercetin was formulated in the microemulsion or when simply dissolved in Transcutol® P. These two last formulations are those showing the lower skin retention.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Antioxidants / administration & dosage
  • Antioxidants / chemistry
  • Antioxidants / metabolism*
  • Chemistry, Pharmaceutical
  • Dermatologic Agents / administration & dosage
  • Dermatologic Agents / chemistry
  • Dermatologic Agents / metabolism
  • Diffusion
  • Drug Stability
  • Emulsifying Agents / chemistry*
  • Emulsions
  • Ethylene Glycols / chemistry*
  • Excipients / chemistry*
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • Kinetics
  • Particle Size
  • Permeability
  • Quercetin / administration & dosage
  • Quercetin / chemistry
  • Quercetin / metabolism*
  • Skin / chemistry*
  • Skin / drug effects
  • Solubility
  • Sus scrofa
  • Viscosity

Substances

  • Antioxidants
  • Dermatologic Agents
  • Emulsifying Agents
  • Emulsions
  • Ethylene Glycols
  • Excipients
  • Quercetin
  • carbitol