title: Improved delivery of the natural anticancer drug tetrandrine.
abstract: The study aims at designing a nanoparticle-based delivery system to improve the efficacy of the natural compound tetrandrine against lung cancer. Nanoparticles from poly(lactic-co-glycolic acid) (PLGA) were prepared by the emulsion solvent diffusion method and characterized for their physicochemical properties and drug-loading efficiency. Furthermore, the cellular uptake and the anti-cancerous activity was studied on A549 cell line. To investigate the surface properties and uptake, three different stabilizers were used to analyze the effect on size and zeta potential of nanoparticles as well as the effect on the cellular uptake. Nanoparticles in the size range of 180-200 nm with spherical shape were obtained with polyvinyl alcohol (PVA), Pluronic-F127 (PF127) and didodecyldimethylammonium bromide (DMAB), 2%, 1% and 0.1%, respectively. An entrapment efficiency of 50-60% with a loading of 1.5-2% was observed. In vitro release profile at pH 7.4 PBS solution showed a consistent release over 168 h. All particle systems showed an improved performance over the pure drug at the same drug concentration. DMAB stabilized particles demonstrated the most pronounced effect against A549 cells compared to pure drug while PVA stabilized particles were least effective in terms of antitumor activity.
authors.affiliation: Pharmaceutics and Biopharmacy, Philipps University, 35037 Marburg, Germany; Wuhan Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430022 Wuhan, China.
authors.forename: Chen
authors.initials: C
authors.lastname: Shi
authors.affiliation: Pharmaceutics and Biopharmacy, Philipps University, 35037 Marburg, Germany.
authors.forename: Saeed
authors.initials: S
authors.lastname: Ahmad Khan
authors.affiliation: Wuhan Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430022 Wuhan, China.
authors.forename: Kaiping
authors.initials: K
authors.lastname: Wang
authors.affiliation: Pharmaceutics and Biopharmacy, Philipps University, 35037 Marburg, Germany. Electronic address: marc.schneider@pharmazie.uni-marburg.de.
authors.forename: Marc
authors.initials: M
authors.lastname: Schneider
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D044182:Benzylisoquinolines / Q000008:administration & dosage* / Q000737:chemistry; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D016503:Drug Delivery Systems; D065546:Drug Liberation; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D020442:Poloxamer / Q000008:administration & dosage / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011142:Polyvinyl Alcohol / Q000008:administration & dosage / Q000737:chemistry; D000644:Quaternary Ammonium Compounds / Q000008:administration & dosage / Q000737:chemistry; D013501:Surface-Active Agents / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D044182:Benzylisoquinolines; D000644:Quaternary Ammonium Compounds; D013501:Surface-Active Agents; D020442:Poloxamer; C046112:didodecyldimethylammonium; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; C009438:tetrandrine; D019344:Lactic Acid; D011142:Polyvinyl Alcohol
keywords: Anti-cancer activity; Cell uptake; Drug delivery; PLGA; Surface properties