title: Preparation and in vitro-in vivo evaluation of teniposide nanosuspensions.
abstract: Teniposide (TEN) is a potent, broad spectrum antitumor agent, especially for cerebroma. But the application in clinic was limited because of its poor solubility. In this paper, teniposide nanosuspensions drug delivery system (TEN-NSDDS) for intravenous administration was developed for the first time. Specifically, TEN nanosuspensions were prepared by an anti-solvent sonication-precipitation method and evaluated in comparison with teniposide injection (VUMON) in vitro and in vivo. TEN nanosuspensions prepared showed rod-like morphology and the size was 151 ± 11 nm with a narrow poly dispersion index 0.138 determined by dynamic light scattering. The obtained TEN nanosuspensions were physically stable at least 10 days at 4°C. And the freeze-drying preparations were stable during 3 months. The cytotoxicity of TEN nanosuspensions were considerable to that of VUMON against U87MG and C6 cells in vitro. When tested in rats bearing C6 tumors, the TEN concentration in the tumors treated by the nanosuspensions was more than 20 times than that by the TEN solution at 2h. The TEN nanosuspensions exhibited significant tumor growth inhibition. Overall, the results suggested that nanosuspensions was an alternative formulation for teniposide to be administered intravenously, and it would be a promising formulation in clinic.
authors.affiliation: Department of Pharmaceutical Sciences, Medical College, Henan University of Science & Technology, Luoyang 471003, PR China. Electronic address: hesuna-2008@haust.edu.cn.
authors.forename: Suna
authors.initials: S
authors.lastname: He
authors.affiliation: Department of Pharmaceutical Sciences, Medical College, Henan University of Science & Technology, Luoyang 471003, PR China.
authors.forename: Hui
authors.initials: H
authors.lastname: Yang
authors.affiliation: Department of Marketing, Henan University of Animal Husbandry and Economy, Zhengzhou 450045, PR China.
authors.forename: Ruizhi
authors.initials: R
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Sciences, Medical College, Henan University of Science & Technology, Luoyang 471003, PR China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Pharmaceutical Sciences, Medical College, Henan University of Science & Technology, Luoyang 471003, PR China.
authors.forename: Lengxin
authors.initials: L
authors.lastname: Duan
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004355:Drug Stability; D006801:Humans; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use / Q000648:ultrastructure; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D010316:Particle Size; D011205:Povidone / Q000737:chemistry; D017208:Rats, Wistar; D013535:Suspensions; D013713:Teniposide / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D047368:Tumor Burden / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D013535:Suspensions; D013713:Teniposide; D011205:Povidone
keywords: Anti-solvent sonication–precipitation method; Antitumor activity; Nanosuspensions; Stability; Teniposide