title: Preparation, Characterization, and In Vivo Study of 7-Ethyl-14-Aminocamptothecin-Loaded Poly(Ethylene Glycol)2000 -Poly(Lactic Acid)2000 Polymeric Micelles Against H460 Human Nonsmall Cell Lung Carcinoma.
abstract: This work aims to improve the solubility of 7-ethyl-14-aminocamptothecin (EACPT) by encapsulating it into monomethoxy poly(ethylene glycol)2000 -poly(lactic acid)2000 (MPEG-PLA) polymeric micelles. Micelles were prepared by a solid dispersion method; the properties including particle size distribution, morphology, drug loading, entrapment efficiency, crystallography property, solubility, and stability were characterized in detail. The results demonstrated that the EACPT-loaded MPEG-PLA polymeric micelle (EACPT-M) was successfully developed with a small particle size of 20.7 ± 0.2 nm, and the solubility was increased approximately 800-fold compared with free drug. In vitro release study showed sustained-release behavior of EACPT-M. Cytotoxicity assay suggested the incorporated EACPT maintained the potent antitumor effect of free drug. Furthermore, the obtained EACPT-M (1 mg/mL) did not induce hemolysis in vitro. Additionally, EACPT-M exhibited significant tumor growth inhibition in H460 human tumor xenograft model. The results indicated that the EACPT-M was a water-soluble, safe, and effective delivery system for human cancer chemotherapy.
authors: State Key laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, People's Republic of China.
authors: Xia
authors: X
authors: Cheng
authors: Department of Chemical and Pharmaceutical engineering, College of Materials and Chemistry and Chemical Engineering, Chengdu University of Technology, Chengdu 610059, People's Republic of China.
authors: Neng
authors: N
authors: Qiu
authors: State Key laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, People's Republic of China.
authors: Jianhong
authors: J
authors: Yang
authors: Department of Bio-pharmaceutical Engineering, School of Chemical Engineering, Sichuan University, Chengdu 610065, People's Republic of China.
authors: Huili
authors: H
authors: Liu
authors: State Key laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, People's Republic of China.
authors: Jiaolin
authors: J
authors: Wen
authors: State Key laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, People's Republic of China.
authors: Wenwen
authors: W
authors: Wang
authors: State Key laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, People's Republic of China.
authors: Zhoufeng
authors: Z
authors: Wang
authors: State Key laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, People's Republic of China. Electronic address: chenlijuan125@163.com.
authors: Lijuan
authors: L
authors: Chen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use; D002166:Camptothecin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000737:chemistry*; D005260:Female; D056945:Hep G2 Cells; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry; D008168:Lung / Q000187:drug effects / Q000473:pathology; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D008819:Mice, Nude; D008823:Micelles; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry
chemical_list: C558738:7-ethyl-14-aminocamptothecin; D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D008823:Micelles; D011091:Polyesters; D011108:Polymers; C492425:methoxy poly(ethylene glycol)-poly(lactide); D019344:Lactic Acid; D011092:Polyethylene Glycols; C033616:poly(lactide); D002166:Camptothecin
keywords: 7-ethyl-14-aminocamptothecin; PLA; cancer chemotherapy; micelle; solid dispersion; solubility