Comparison of PLGA and lecithin/chitosan nanoparticles for dermal targeting of betamethasone valerate

J Drug Target. 2013 Jul;21(6):542-50. doi: 10.3109/1061186X.2013.769106. Epub 2013 Feb 8.

Abstract

Poly(lactide-co-glycolide) (PLGA) and lecithin/chitosan (LC) nanoparticles were prepared to evaluate the difference in the behavior upon administration on skin, for steroidal treatment. For this purpose, betamethasone-17-valerate (BMV)-loaded nanoparticles with a narrow size distribution and high entrapment efficiency were prepared. Permeation studies showed that both polymeric nanoparticles enhanced the amount of BMV in epidermis, which is the target site of topical steroidal treatment, when compared with commercial formulation. 1.58-Fold increase was determined in the epidermis concentration of BMV by LC nanoparticles with respect to PLGA nanoparticles. Nanoparticles were diluted in chitosan gel (10%, w/w) to prepare suitable formulation for topical application. Accumulation from both gel formulations were found significantly higher than commercial formulation in skin layers (p < 0.05). In addition, pharmacodynamic responses were also investigated as anti-inflammatory and skin-blanching parameters. Both formulations significantly improved these parameters although they contained 10 times less amount of BMV than commercial cream. Moreover, TEWL measurement exhibited no barrier function changes upon the application of nanoparticles on skin. Overall, both nanoparticles improved the localization of BMV within skin layers; but when compared with PLGA nanoparticles, the LC nanoparticles could be classified as a better candidate for topical delivery vehicle in the treatment of various dermatological inflammatory diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / chemistry
  • Betamethasone Valerate / administration & dosage*
  • Betamethasone Valerate / chemistry
  • Betamethasone Valerate / pharmacokinetics
  • Chemistry, Pharmaceutical / methods
  • Chitosan / administration & dosage*
  • Chitosan / chemistry
  • Chitosan / pharmacokinetics
  • Dermis / drug effects
  • Dermis / metabolism*
  • Drug Delivery Systems / methods
  • Epidermis / drug effects
  • Epidermis / metabolism
  • Lactic Acid / administration & dosage*
  • Lactic Acid / chemistry
  • Lecithins / administration & dosage*
  • Lecithins / chemistry
  • Lecithins / pharmacokinetics
  • Male
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Nanoparticles / metabolism
  • Particle Size
  • Permeability / drug effects
  • Polyglycolic Acid / administration & dosage*
  • Polyglycolic Acid / chemistry
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Rats
  • Rats, Wistar
  • Skin Absorption / drug effects

Substances

  • Anti-Inflammatory Agents
  • Lecithins
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Chitosan
  • Betamethasone Valerate