title: Nanocarrier improves the bioavailability, stability and antitumor activity of camptothecin.
abstract: Camptothecin (CPT) nanosuspension was prepared by anti-solvent precipitation with TPGS as stabilizer to improve the solubility, stability and antitumor activity of CPT. And an increased solubility, stability and dissolution rate was achieved after nanosuspension being prepared. While, enhanced intracellular accumulation and cellular cytotoxicity was also observed for CPT nanosuspension than that of CPT solution.In addition, nanosuspension could increase bioavailability and intratumor accumulation of CPT in vivo after intravenous administration, and then produced a much higher antitumor effect and biocompatibility than that of CPT solution. Meanwhile, an enhanced cellular CPT uptake in hypoxic or acid conditions could also be observed for nanosuspension. As a result, nanosuspension represents a potentially feasible formation for insoluble drug in antitumor research.
authors.affiliation: Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China.
authors.forename: Xin-Jiang
authors.initials: XJ
authors.lastname: Tang
authors.affiliation: Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China. Electronic address: hanmin2@zju.edu.cn.
authors.forename: Min
authors.initials: M
authors.lastname: Han
authors.affiliation: Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China.
authors.forename: Bo
authors.initials: B
authors.lastname: Yang
authors.affiliation: Center for Bionanoengineering and State Key Laboratory of Chemical Engineering, Zhejiang University, Hangzhou 310027, PR China.
authors.forename: You-Qing
authors.initials: YQ
authors.lastname: Shen
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, Liaoning, PR China.
authors.forename: Zhong-Gui
authors.initials: ZG
authors.lastname: He
authors.affiliation: The Second Affiliated Hospital of Zhejiang University, Hangzhou 310001, PR China.
authors.forename: Dong-Hang
authors.initials: DH
authors.lastname: Xu
authors.affiliation: Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China. Electronic address: gaojianqing@zju.edu.cn.
authors.forename: Jian-Qing
authors.initials: JQ
authors.lastname: Gao
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D001682:Biological Availability; D002166:Camptothecin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D005260:Female; D007275:Injections, Intravenous; D061986:MCF-7 Cells; D008297:Male; D008819:Mice, Nude; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013499:Surface Properties; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D002166:Camptothecin
keywords: Antitumor effect; Camptothecin; Nanosuspension; Side effect