Liposomal delivery system enhances anti-inflammatory properties of curcumin

J Pharm Sci. 2012 Feb;101(2):598-609. doi: 10.1002/jps.22785. Epub 2011 Oct 11.

Abstract

Curcumin is a well-established natural antioxidant and anti-inflammatory agent. Up till now its potential in treatment of vaginal inflammation has not been evaluated. We are aiming at developing liposomal delivery system for curcumin targeting vaginal administration. Liposomes as nanosized phospholipid-based vesicles are expected to solubilize curcumin and enhance its activity, thus serving as an advanced topical formulation in the treatment of vaginal inflammation. Curcumin and curcuminoids were analyzed by the high-performance liquid chromatography method. Liposomes containing curcumin/curcuminoids of various sizes were prepared and characterized. Antioxidant activities of curcumin and liposomal curcumin were compared based on 1,1-diphenyl-2-picrylhydrazyl radical scavenging and superoxide dismutase activities. The anti-inflammatory activities were determined by measuring the inhibition of lipopolysaccharide -induced nitric oxide, interleukin-1β, and tumor necrosis factor-α production in macrophage RAW 264.7 cells. Curcumin/curcuminoids were encapsulated in phosphatidylcholine vesicles with high yields. Vesicles in the size range around 200 nm were selected for stability and cell experiments. Liposomal curcumin were found to be twofold to sixfold more potent than corresponding curcuminoids. Moreover, the mixture of curcuminoids was found to be more potent than pure curcumin in regard to the antioxidant and anti-inflammatory activities. Liposomal delivery systems for curcumin are promising formulations for the treatment of vaginal inflammation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / administration & dosage*
  • Anti-Inflammatory Agents / pharmacology
  • Cell Line
  • Chromatography, High Pressure Liquid
  • Curcumin / administration & dosage*
  • Curcumin / pharmacology
  • Drug Delivery Systems
  • Interleukin-1beta / biosynthesis
  • Liposomes*
  • Macrophages, Peritoneal / enzymology
  • Macrophages, Peritoneal / metabolism
  • Mice
  • Nitric Oxide / biosynthesis
  • Superoxide Dismutase / metabolism
  • Tumor Necrosis Factor-alpha / biosynthesis

Substances

  • Anti-Inflammatory Agents
  • Interleukin-1beta
  • Liposomes
  • Tumor Necrosis Factor-alpha
  • Nitric Oxide
  • Superoxide Dismutase
  • Curcumin