Targeting of liposomal andrographolide to L. donovani-infected macrophages in vivo

Drug Deliv. Oct-Dec 2000;7(4):209-13. doi: 10.1080/107175400455137.

Abstract

Despite the rapid development in medicinal and pharmaceutical technology, the targeting of drugs to phagocytic cells in macrophage-related diseases still remains a major unsolved problem. By using the mannosyl-fucosyl receptors on macrophages, attempts were made to target antileishmanial drugs encapsulated in mannosylated or fucosylated liposomes to treat experimental leishmaniasis in the hamster model. Mannosylated liposomes were found to be more potent in delivering antileishmanial drugs to phagocytic cells. Liposomes loaded with an indigenous drug, andrographolide, a labdane diterpenoid isolated from Indian medicinal plant Andrographis paniculata, were prepared and tested against experimental leishmaniasis in a hamster model. Mannosylated liposomes loaded with the drug were found to be most potent in reducing the parasitic burden in the spleen as well as in reducing the hepatic and renal toxicity. In addition, mannosylated drug-loaded liposome-treated animals showed a normal blood picture and splenic tissue histoarchitecture when compared with those treated with free drug or regular liposomal drug. Such a drug-vehicle formulation may be considered for clinical trials.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents / administration & dosage*
  • Antiprotozoal Agents / pharmacology*
  • Antiprotozoal Agents / toxicity
  • Coloring Agents
  • Cricetinae
  • Diterpenes / administration & dosage*
  • Diterpenes / pharmacology*
  • Diterpenes / toxicity
  • Drug Carriers
  • Drug Delivery Systems
  • Leishmania donovani / drug effects*
  • Leishmaniasis, Visceral / drug therapy
  • Leishmaniasis, Visceral / parasitology
  • Liposomes
  • Liver Function Tests
  • Macrophages / drug effects
  • Macrophages / parasitology*
  • Mesocricetus
  • Mice
  • Mice, Inbred BALB C
  • Trypan Blue

Substances

  • Antiprotozoal Agents
  • Coloring Agents
  • Diterpenes
  • Drug Carriers
  • Liposomes
  • andrographolide
  • Trypan Blue