title: Mannose-conjugated chitosan nanoparticles loaded with rifampicin for the treatment of visceral leishmaniasis.
abstract: The aim of current research work was to develop and investigate the potential of rifampicin (RIF) loaded mannose-conjugated chitosan nanoparticulate system for selective delivery to the macrophages in the management of visceral leishmaniasis (VL). RIF loaded mannose-conjugated chitosan nanoparticles (mCNPs) were prepared and characterized for shape, size, entrapment efficiency and in vitro drug release. The in vivo bio-distribution in albino rats and ex vivo drug uptake by macrophage were also evaluated. It was observed that extent of accumulation of mCNPs in macrophage rich organs, particularly in liver and spleen, were significantly higher compared to free drug. Ex vivo uptake of mCNPs was 2.31 times higher compared to unconjugated chitosan nanoparticles (CNPs). The macrophage uptake of mCNPs was inhibited significantly on pre-incubation with 0.05 M mannose in a parallel experiment, being suggestive of receptor mediated uptake of mannosylated nanoparticles. Our results indicate that mCNPs could be a promising carrier for selective delivery of RIF to macrophages for effective management of VL.
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, India. Electronic address: cpramil@gmail.com.
authors.forename: Pramila
authors.initials: P
authors.lastname: Chaubey
authors.forename: Brahmeshwar
authors.initials: B
authors.lastname: Mishra
mesh_terms: D000818:Animals; D001692:Biological Transport; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D008297:Male; D008358:Mannose / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D051381:Rats; D012293:Rifampin / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D004337:Drug Carriers; D048271:Chitosan; D008358:Mannose; D012293:Rifampin
keywords: Leishmaniasis; Macrophages; Mannose-conjugated chitosan; Nanoparticles; Rifampicin