title: Submicron-size biodegradable polymer-based didanosine particles for treating HIV at early stage: an in vitro study.
abstract: Human immunodeficiency viruses (HIV) hide themselves in macrophages at the early stage of infection. Delivering drug in a sustained manner from polymeric nanoparticles in those cells could control the disease effectively. The study was intended to develop poly(d,l-lactic-co-glycolic acid)-based nanoparticles containing didanosine and to observe their uptake by macrophages in vitro. Various physicochemical evaluations related to nanoparticles, such as drug-excipient interaction, surface morphology, particle size, zeta potential, polydispersity index, drug loading, in vitro drug release and nanoparticle-uptake by macrophages in vitro were determined. Homogenising speeds and drug-polymer ratio varied drug loading and polydispersity index of nanoparticles, providing sustained drug release. Dimethyl sulphoxide/polyethylene glycol improved drug loading predominantly. Nanoparticle-uptake by macrophages was concentration dependent. Experimental nanoparticles successfully transported didanosine to macrophages in vitro, suggesting reduction of dose, thus minimising toxicity and side effects. Developed nanoparticle may control HIV infection effectively at an early stage.
authors.affiliation: Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
authors.forename: Gurudutta
authors.initials: G
authors.lastname: Pattnaik
authors.forename: Biswadip
authors.initials: B
authors.lastname: Sinha
authors.forename: Biswajit
authors.initials: B
authors.lastname: Mukherjee
authors.forename: Saikat
authors.initials: S
authors.lastname: Ghosh
authors.forename: Sandip
authors.initials: S
authors.lastname: Basak
authors.forename: Subhasish
authors.initials: S
authors.lastname: Mondal
authors.forename: Tanmoy
authors.initials: T
authors.lastname: Bera
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002478:Cells, Cultured; D003692:Delayed-Action Preparations; D016049:Didanosine / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D005260:Female; D006678:HIV; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D017737:Macrophages, Peritoneal / Q000166:cytology / Q000378:metabolism*; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D019380:Anti-HIV Agents; D003692:Delayed-Action Preparations; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D016049:Didanosine