Andrographolide nanoparticles in leishmaniasis: characterization and in vitro evaluations

Int J Nanomedicine. 2010 Dec 9;5:1113-1121.

Andrographolide nanoparticles in leishmaniasis: characterization and in vitro evaluations.

Roy P, Das S, Bera T, Mondol S, Mukherjee A.

Department of Chemical Technology, University of Calcutta, Kolkata, West Bengal, India.

Andrographolide (AG) is a diterpenoid lactone isolated from the leaves of Andrographis paniculata. AG is a potent and low-toxicity antileishmanial agent. Chemotherapy applications of AG are, however, seriously constrained because of poor bioavailability, short plasma half-life, and inappropriate tissue localization. Nanoparticulation of AG was therefore envisaged as a possible solution. AG nanoparticles (AGnp) loaded in 50:50 poly(DL-lactide-co-glycolic acid) were prepared for delivery into the monocyte-macrophage cells infested with the amastigote form of leishmanial parasite for evaluation in the chemotherapy of leishmaniasis. Particle characteristics of AGnp were optimized by proportionate application of a stabilizer, polyvinyl alcohol (PVA). Physicochemical characterization of AGnp by photon correlation spectroscopy exhibited an average particle size of 173 nm and zeta potential of -34.8 mV. Atomic force microscopy visualization revealed spherical nanoparticles with a smooth surface. Antileishmanial activity was found to be significant for the nanoparticle preparation with 4% PVA (IC(50) 34 µM) in about one-fourth of the dosage of the pure compound AG (IC(50) 160 µM). AGnp therefore have significant potential to target the infested macrophage cells and prove valuable in chemotherapy of neglected tropical diseases such as leishmaniasis.

PMID: 21270962 [PubMed - as supplied by publisher]