Carbon nanotube based betulin formulation shows better efficacy against Leishmania parasite

Parasitol Int. 2014 Dec;63(6):772-6. doi: 10.1016/j.parint.2014.07.008. Epub 2014 Jul 31.

Abstract

We report a novel antileishmanial formulation of betulin (BET) attached to functionalized carbon nanotubes (f-CNTs). We conjugated betulin, a pentacyclic triterpenoid secondary metabolite, to carboxylic acid chains on f-CNTs to obtain BET attached functionalized carbon nanotubes (f-CNT-Bet). The drug release profile demonstrated a fairly slow release of BET. The in-vitro cytotoxicities of BET, f-CNT and f-CNT-BET on J774A.1 macrophage cell line were 211.05±7.14μg/ml; 24.67±3.11μg/ml and 72.63±6.14μg/ml, respectively. The IC50 of BET and f-CNT-BET against intracellular Leishmania donovani amastigotes were 8.33±0.41μg/ml and 0.69±0.08μg/ml, respectively. The results demonstrate better antileishmanial efficiency of f-CNT-BET formulation than BET alone and with no significant cytotoxicity observed on host cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacokinetics
  • Antiprotozoal Agents / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • Chemistry, Pharmaceutical
  • Humans
  • Leishmania / drug effects*
  • Leishmania donovani / drug effects
  • Leishmaniasis
  • Macrophages / parasitology
  • Nanotubes, Carbon / chemistry*
  • Triterpenes / chemistry
  • Triterpenes / pharmacokinetics
  • Triterpenes / pharmacology*

Substances

  • Antiprotozoal Agents
  • Nanotubes, Carbon
  • Triterpenes
  • betulin