Molecular mechanism and increased antileishmanial activity of carbon nanotube based betulin formulation

The present study describes a novel antileishmanial drug formulation of betulin (BET) attached to functionalized carbon nanotubes (f-CNTs) as macrophage targeted drug delivery system. We conjugated BET; a pentacyclic... [ view full abstract ]

The present study describes a novel antileishmanial drug formulation of betulin (BET) attached to functionalized carbon nanotubes (f-CNTs) as macrophage targeted drug delivery system. We conjugated BET; a pentacyclic triterpenoid secondary metabolite to carboxylic acid chains on f-CNTs to obtain BET attached functionalized carbon nanotubes (f-CNT-Bet). The fourier transform infrared (FTIR) spectroscopy and transmission electron microscopy (TEM) demonstrated the successful construction of f-CNT-BET. The Bet loading efficiency onto the f-CNTs and Bet release profile were monitored spectroscopically. The drug release profile demonstrated a fairly slow release of Bet. The in-vitro cytotoxicity of BET, f-CNT and f-CNT-BET on J774A.1 macrophage cell line were 211.05 ± 7.14 µg/ml; 24.67 ± 3.11 µg/ml and 72.63 ± 6.14 µg/ml respectively as measured by the cytotoxic concentration required to inhibit 50% cell viability (IC50). The IC50 of BET and f-CNT-BET against intracellular L. donovani amastigote in vitro were 8.33 ± 0.41 µg/ml and 0.69 ± 0.08 µg/ml respectively. The results clearly demonstrating the greater antileishmanial efficiency of f-CNT-BET formulation than BET alone and with no significant cytotoxicity observed on host cells, f-CNT-BET boost new hope for significant application of carbon nanotubes in formulating better drug for leishmaniasis with minimum side effects and high treatment efficacy.