title: Anti-cancerous efficacy and pharmacokinetics of 6-mercaptopurine loaded chitosan nanoparticles.
abstract: 6-Mercaptopurine is a cytotoxic and immunosuppressant drug. The use of this drug is limited due to its poor bioavailability and short plasma half-life. In order to nullify these drawbacks, 6-mercaptopurine-chitosan nanoparticles (6-MP-CNPs) were prepared and evaluated to study the influence of preparation conditions on the physicochemical properties by using DLS, SEM, XRD and FTIR. The in vitro drug release profile at pH 4.8 and 7.4 revealed sustained release patterns for a period of 2 days. The nanoformulations showed enhanced in vitro anti-cancer activities (MTT assay, apoptosis assay, cell cycle arrest and ROS indices) on HT-1080 and MCF-7 cells. In vivo pharmacokinetics profiles of 6-MP-CNPs showed improved bioavailability. Thus, the results of the present study revealed that, the prepared 6-MP-CNPs have a significant role in increasing anti-cancer efficacy, bioavailability and in vivo pharmacokinetics profiles.
authors.affiliation: Department of Toxicology, Bioneeds India Private Limited, Bangalore, Karnataka, India; Department of Veterinary Pharmacology and Toxicology, Veterinary College, Bangalore, Karnataka, India. Electronic address: drpremkamal@gmail.com.
authors.forename: G Prem
authors.initials: GP
authors.lastname: Kumar
authors.affiliation: Department of Veterinary Pharmacology and Toxicology, Veterinary College, Bangalore, Karnataka, India.
authors.forename: Jagadeesh S
authors.initials: JS
authors.lastname: Sanganal
authors.affiliation: Nano Research for Advanced Materials and Technologies, Bangalore, Karnataka, India.
authors.forename: A R
authors.initials: AR
authors.lastname: Phani
authors.affiliation: Department of Veterinary Pharmacology and Toxicology, Veterinary College, Bangalore, Karnataka, India.
authors.forename: C
authors.initials: C
authors.lastname: Manohara
authors.affiliation: College of Veterinary Science and Animal Husbandry, Anjora, Durg, Chhattisgarh, India.
authors.forename: Syamantak M
authors.initials: SM
authors.lastname: Tripathi
authors.affiliation: School of Medicine, College of Medical and Health Sciences, Wollega University, P.O. Box: 395, Nekemte, Ethiopia.
authors.forename: H L
authors.initials: HL
authors.lastname: Raghavendra
authors.affiliation: Stellixir Biotech Private Limited, T. Dasarahalli, Bangalore, Karnataka, India.
authors.forename: P B
authors.initials: PB
authors.lastname: Janardhana
authors.affiliation: Department of Veterinary Pharmacology and Toxicology, Veterinary College, Bangalore, Karnataka, India.
authors.forename: S
authors.initials: S
authors.lastname: Amaresha
authors.affiliation: Department of Veterinary Pharmacology and Toxicology, Veterinary College, Bangalore, Karnataka, India.
authors.forename: K B
authors.initials: KB
authors.lastname: Swamy
authors.affiliation: Faculty of Pharmaceutical Sciences, Asian Metropolitan University, Selangor, Kualalumpur, Malaysia.
authors.forename: R G S V
authors.initials: RG
authors.lastname: Prasad
mesh_terms: D000970:Antineoplastic Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001682:Biological Availability; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D048271:Chitosan / Q000008:administration & dosage*; D003692:Delayed-Action Preparations / Q000493:pharmacokinetics / Q000494:pharmacology; D004337:Drug Carriers / Q000008:administration & dosage; D016503:Drug Delivery Systems / Q000379:methods; D006801:Humans; D061986:MCF-7 Cells; D015122:Mercaptopurine / Q000493:pharmacokinetics* / Q000494:pharmacology*; D053758:Nanoparticles / Q000008:administration & dosage*; D010316:Particle Size
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D048271:Chitosan; D015122:Mercaptopurine
keywords: Apoptosis; Chitosan nanoparticles; Cytotoxic; ROS and bioavailability