title: Andrographolide nanoparticles in leishmaniasis: characterization and in vitro evaluations.
abstract: 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 (IC₅₀) 34 μM) in about one-fourth of the dosage of the pure compound AG (IC₅₀) 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.
authors.affiliation: Department of Chemical Technology, University of Calcutta, Kolkata, West Bengal, India.
authors.forename: Partha
authors.initials: P
authors.lastname: Roy
authors.forename: Suvadra
authors.initials: S
authors.lastname: Das
authors.forename: Tanmoy
authors.initials: T
authors.lastname: Bera
authors.forename: Subhasis
authors.initials: S
authors.lastname: Mondol
authors.forename: Arup
authors.initials: A
authors.lastname: Mukherjee
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D004224:Diterpenes / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D006801:Humans; D007893:Leishmania donovani / Q000187:drug effects*; D007898:Leishmaniasis, Visceral / Q000378:metabolism*; D008018:Life Cycle Stages / Q000187:drug effects; D017737:Macrophages, Peritoneal / Q000378:metabolism; D051379:Mice; D018625:Microscopy, Atomic Force; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties
chemical_list: D000981:Antiprotozoal Agents; D004224:Diterpenes; C030419:andrographolide