Development and characterization of dutasteride bearing liposomal systems for topical use

Curr Drug Discov Technol. 2011 Jun;8(2):136-45. doi: 10.2174/157016311795563901.

Abstract

Dutasteride loaded liposomal system were developed for topical application in order to avoid the side effects associated with the oral administration of the drug. Drug-loaded multilamellar liposomes were prepared using thin-film hydration method followed by sonication and optimized with respect to entrapment efficiency, drug payload, size and lamellarity. The vesicular systems consisting of egg phosphatidylcholine (100 mg), cholesterol (50 mg), and dutasteride (5 mg) showed highest drug entrapment efficiency (94.6%) and drug payload (31.5 µg/mg of total lipids). Mean vesicle size of these liposomes was noted to be 1.82 ± 0.15 µm. Significantly higher skin permeation of dutasteride through excised abdominal mouse skin was achieved via the developed liposomal formulations as compared to hydro-alcoholic solution and conventional gels. The formulation exhibited about seven fold higher deposition of drug in skin. Stability studies indicated that the liposomal formulations were quite stable in the refrigerated conditions for 10 weeks with negligible drug leakage or vesicle size alteration. Results of the current studies exhibited improved and localized drug action in the skin and thus could be formulated as a better option to cure androgenetic alopecia.

MeSH terms

  • 5-alpha Reductase Inhibitors / administration & dosage*
  • 5-alpha Reductase Inhibitors / chemistry
  • 5-alpha Reductase Inhibitors / metabolism
  • Administration, Cutaneous
  • Alcohols / chemistry
  • Animals
  • Azasteroids / administration & dosage*
  • Azasteroids / chemistry
  • Azasteroids / metabolism
  • Chemistry, Pharmaceutical
  • Cholesterol / chemistry*
  • Cold Temperature
  • Drug Compounding
  • Drug Stability
  • Dutasteride
  • Gels
  • Liposomes
  • Mice
  • Particle Size
  • Permeability
  • Phosphatidylcholines / chemistry*
  • Skin / metabolism
  • Skin Absorption
  • Sonication
  • Technology, Pharmaceutical / methods

Substances

  • 5-alpha Reductase Inhibitors
  • Alcohols
  • Azasteroids
  • Gels
  • Liposomes
  • Phosphatidylcholines
  • Cholesterol
  • Dutasteride