title: A new approach for the delivery of artemisinin: formulation, characterization, and ex-vivo antileishmanial studies.
abstract: OBJECTIVE
  Artemisinin, a potential antileishmanial compound with poor bioavailability and stability has limited efficacy in visceral leishmaniasis. Encapsulating artemisinin into poly lactic-co glycolic nanoparticles may improve its effectiveness and reduce toxicity.
  
  
  METHODS
  Artemisinin-loaded nanoparticles were prepared, optimized (using Box-Behnken design) and characterized by dynamic light scattering technique, Atomic force microscopy (AFM), Transmission electron microscopy (TEM) and Fourier Transform-Infra Red spectroscopy. Release kinetics of artemisinin from optimized nanoformulation was studied by dialysis method at pH 7.4 and 5.5. Cytotoxicity and antileishmanial activity of these nanoparticles was tested on murine macrophages by MTT assay and macrophage-infested Leishmania donovani amastigotes ex vivo, respectively.
  
  
  RESULTS
  Artemisinin-loaded nanoparticles were 221±14nm in diameter, with polydispersity index, zeta potential, drug loading and entrapment efficiency of 0.1±0.015, -9.07±0.69mV, 28.03±1.14 and 68.48±1.97, respectively. AFM and TEM studies indicated that the particles were spherical in shape. These colloidal particles showed a sustained release pattern in vitro. Treatment with artemisinin-loaded nanoparticles significantly reduced the number of amastigotes per macrophage and percent infected macrophages ex vivo compared to free artemisinin. These nanoparticles were also non-toxic to macrophages compared to artemisinin alone.
authors.affiliation: Parasite Immunology Laboratory, Department of Biotechnology, Jamia Hamdard (Hamdard University), New Delhi 110062, India.
authors.forename: Muzamil Yaqub
authors.initials: MY
authors.lastname: Want
authors.affiliation: Parasite Immunology Laboratory, Department of Biotechnology, Jamia Hamdard (Hamdard University), New Delhi 110062, India.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Islamuddin
authors.affiliation: Parasite Immunology Laboratory, Department of Biotechnology, Jamia Hamdard (Hamdard University), New Delhi 110062, India.
authors.forename: Garima
authors.initials: G
authors.lastname: Chouhan
authors.affiliation: Department of Biophysics and Biochemistry, Ballygunge Science College, University of Calcutta, Kolkata 700019, India.
authors.forename: Anjan Kumar
authors.initials: AK
authors.lastname: Dasgupta
authors.affiliation: Department of Chemistry, University of Kalyani, West Bengal 741235, India.
authors.forename: Asoke Prasun
authors.initials: AP
authors.lastname: Chattopadhyay
authors.affiliation: Parasite Immunology Laboratory, Department of Biotechnology, Jamia Hamdard (Hamdard University), New Delhi 110062, India. Electronic address: afrin_farhat@yahoo.co.in.
authors.forename: Farhat
authors.initials: F
authors.lastname: Afrin
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology; D037621:Artemisinins / Q000737:chemistry / Q000494:pharmacology; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D019344:Lactic Acid / Q000493:pharmacokinetics / Q000494:pharmacology; D007893:Leishmania donovani / Q000254:growth & development*; D007898:Leishmaniasis, Visceral / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D017737:Macrophages, Peritoneal / Q000378:metabolism / Q000469:parasitology / Q000473:pathology; D051379:Mice; D008807:Mice, Inbred BALB C; D011100:Polyglycolic Acid / Q000493:pharmacokinetics / Q000494:pharmacology; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D000981:Antiprotozoal Agents; D037621:Artemisinins; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C031327:artemisinin
keywords: Antileishmanial; Artemisinin; Box–Behnken design; L. donovani; Nanomedicine; Nanoparticles; Nanoprecipitation; PLGA; Toxicity; Visceral leishmaniasis