title: Oleanolic acid loaded poly lactic co- glycolic acid- vitamin E TPGS nanoparticles for the treatment of Leishmania donovani infected visceral leishmaniasis.
abstract: Oleanolic acid (OA) has low aqueous solubility and low permeability, which results poor bioavailability. To surmount the inadequacy, our aim was to fabricate oleanolic acid loaded poly lactic co- glycolic acid (PLGA)- d-α- tocopheryl polyethylene glycol 1000 succinate (TPGS) nanoparticles, which could be efficacious for the treatment of Leishmania donovani mediated visceral leishmaniasis (VL). OA loaded PLGA- TPGS nanoparticles were prepared by emulsion solvent evaporation technique. Cellular uptake was investigated. In vitro cumulative drug release study was carried out. In vitro susceptibility was confirmed against the amastigotes of Leishmania donovani AG83 wild and drug resistant strains. In vivo antileishmanial activity was evaluated against wild type amastigotes of L. donovani. OA loaded nanoparticles were successfully formulated. The highest drug loading was found to be 11.08%±0.35%. 85.66%±0.56% was the highest in vitro OA release for 30days among the formulations. In vivo study revealed that, 98.82±1.92% amastigote burden in spleen of BALB/c mice were suppressed by the polymeric nanoformulation of OA. Experimental OA nanoparticle formulation proved itself as an attractive carrier for OA which was significantly efficacious against both in vitro and in vivo amastigote form of Leishmania donovani than pure OA for chemotherapeutic intervention of visceral leishmaniasis.
authors.affiliation: Laboratory of Nanomedicine, Division of Pharmaceutical Biotech., Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700 032, West Bengal, India.
authors.forename: Santanu
authors.initials: S
authors.lastname: Ghosh
authors.affiliation: Laboratory of Nanomedicine, Division of Pharmaceutical Biotech., Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700 032, West Bengal, India.
authors.forename: Nabanita
authors.initials: N
authors.lastname: Kar
authors.affiliation: Laboratory of Nanomedicine, Division of Pharmaceutical Biotech., Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700 032, West Bengal, India. Electronic address: proftanmoybera@gmail.com.
authors.forename: Tanmoy
authors.initials: T
authors.lastname: Bera
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000008:administration & dosage*; D004353:Drug Evaluation, Preclinical; D005260:Female; D020128:Inhibitory Concentration 50; D019344:Lactic Acid / Q000737:chemistry; D007893:Leishmania donovani / Q000187:drug effects; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000008:administration & dosage*; D009828:Oleanolic Acid / Q000008:administration & dosage*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D014344:Trypanocidal Agents / Q000008:administration & dosage*; D014810:Vitamin E / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D014344:Trypanocidal Agents; D014810:Vitamin E; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D009828:Oleanolic Acid
keywords: In vivo antileishmanial activity; Oleanolic acid; PLGA nanoparticle