title: PLGA-soya lecithin based micelles for enhanced delivery of methotrexate: Cellular uptake, cytotoxic and pharmacokinetic evidences.
abstract: Biocompatible and biodegradable polymers like PLGA have revolutionized the drug delivery approaches. However, poor drug loading and substantially high lipophilicity, pave a path for further tailing of this promising agent. In this regard, PLGA was feathered with biocompatible phospholipid and polymeric micelles were developed for delivery of Methotrexate (MTX) to cancer cells. The nanocarriers (114.6nm±5.5nm) enhanced the cytotoxicity of MTX by 2.13 folds on MDA-MB-231 cells. Confocal laser scanning microscopy confirmed the increased intracellular delivery. The carrier decreased the protein binding potential and enhanced the bioavailable fraction of MTX. Pharmacokinetic studies vouched substantial enhancement in AUC and bioresidence time, promising an ideal carrier to effectively deliver the drug to the site of action. The developed nanocarriers offer potential to deliver the drug in the interiors of cancer cells in an effective manner for improved therapeutic action.
authors.affiliation: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist. Ajmer, Rajasthan, 305 817, India.
authors.forename: Anupama
authors.initials: A
authors.lastname: Singh
authors.affiliation: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist. Ajmer, Rajasthan, 305 817, India.
authors.forename: Nagarani
authors.initials: N
authors.lastname: Thotakura
authors.affiliation: UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles and Nanocomposites, Panjab University, Chandigarh, 160 014, India.
authors.forename: Rajendra
authors.initials: R
authors.lastname: Kumar
authors.affiliation: UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles and Nanocomposites, Panjab University, Chandigarh, 160 014, India; Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160 014, India.
authors.forename: Bhupinder
authors.initials: B
authors.lastname: Singh
authors.affiliation: Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160 014, India.
authors.forename: Gajanand
authors.initials: G
authors.lastname: Sharma
authors.affiliation: Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160 014, India.
authors.forename: Om Prakash
authors.initials: OP
authors.lastname: Katare
authors.affiliation: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Dist. Ajmer, Rajasthan, 305 817, India. Electronic address: drkaisar@curaj.ac.in.
authors.forename: Kaisar
authors.initials: K
authors.lastname: Raza
mesh_terms: D000818:Animals; D001692:Biological Transport; D002417:Cattle; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics / Q000633:toxicity; D065546:Drug Liberation; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry* / Q000378:metabolism* / Q000493:pharmacokinetics / Q000633:toxicity; D054709:Lecithins / Q000737:chemistry*; D008727:Methotrexate / Q000737:chemistry*; D008823:Micelles; D011100:Polyglycolic Acid / Q000737:chemistry* / Q000378:metabolism* / Q000493:pharmacokinetics / Q000633:toxicity; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D012710:Serum Albumin, Bovine / Q000378:metabolism; D013025:Glycine max / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D054709:Lecithins; D008823:Micelles; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D012710:Serum Albumin, Bovine; D019344:Lactic Acid; D008727:Methotrexate
keywords: Anti-neoplastic agent; Biodegradability; Nanoparticulate system; Protein binding and confocal laser scanning microscopy