Transdermal absorption enhancement through rat skin of gallidermin loaded in niosomes

Int J Pharm. 2010 Jun 15;392(1-2):304-10. doi: 10.1016/j.ijpharm.2010.03.064. Epub 2010 Apr 8.

Abstract

Gallidermin (Gdm) loaded in anionic niosomes composed of Tween 61/CHL/DP (1:1:0.05 molar ratio) gave the highest entrapment efficiency (45.06%). This formulation gave antibacterial activity against Propionibacterium acnes and Staphylococcus aureus with the MIC and MBC of 3.75 and 7.5; 7.5 and 15 microg/microl, respectively. Gdm loaded in niosomes was more chemically stable than Gdm in aqueous solution of about 1.5 times. Gdm loaded and unloaded in niosomes were not found in the receiver solution investigated by vertical Franz diffusion cells at 37 degrees C for 6h. Gdm loaded in niosomes showed higher cumulative amounts in viable epidermis and dermis (VED) of rat skin of about 2 times more than unloaded Gdm. Gdm loaded in niosomes and incorporated in gel exhibited the highest cumulative amounts (82.42+/-9.28 microg cm(-2)) and fluxes (13.74+/-1.55 microg cm(-2)h(-1)) in stratum corneum (SC) and comparative cumulative amounts (183.16+/-30.32 microg cm(-2)) and fluxes (25.74+/-5.05 microg cm(-2)h(-1)) in VED to the unloaded Gdm incorporated in gel. This study has suggested that Gdm loaded in anionic niosomes and incorporated in gel is the superior topical antibacterial formulation because of the high accumulation in the skin with no risk of systemic effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / pharmacokinetics
  • Bacteriocins / administration & dosage*
  • Bacteriocins / pharmacokinetics
  • Chromatography, High Pressure Liquid
  • Drug Compounding
  • Drug Stability
  • In Vitro Techniques
  • Liposomes
  • Male
  • Microbial Sensitivity Tests
  • Microscopy, Electron, Transmission
  • Particle Size
  • Peptides / administration & dosage*
  • Peptides / pharmacokinetics
  • Propionibacterium acnes / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Skin / drug effects*
  • Skin / metabolism
  • Skin Absorption / drug effects*
  • Staphylococcus aureus / drug effects
  • Surface Properties

Substances

  • Anti-Bacterial Agents
  • Bacteriocins
  • Liposomes
  • Peptides
  • gallidermin