title: Encapsulated paclitaxel nanoparticles exhibit enhanced anti-tumor efficacy in A549 non-small lung cancer cells.
abstract: In the present study, paclitaxel (PTX) were encapsulated with polyethylene glycol (PEG)-polylactide (PLA)/D-α tocopheryl polyethylene glycol 1000 succinate (TPGS) (PEG-PLA/TPGS) and the enhanced anti-tumor activity of this PTX mixed micelles (PTX-MM) was evaluated in lung cancer cells. The PTX-MM prepared by a solvent evaporation method was demonstrated to have high drug-loading efficiency (23.2%), high encapsulation efficiency (76.4%), and small size (59 nm). In vitro release assay showed the slow release behavior of PTX-MM, suggesting the good stability of the PTX-MM essential for long circulation time. In vitro kinetics assay demonstrated that PTX-MM could promote absorption and increase relative bioavailability. The anti-cancer efficiency of PTX-MM was also examined by both in vitro and in vivo studies. PTX-MM exhibits obvious cytotoxicity against lung cancer cells with much lower IC50 value when compared with commercial formulated PTX or PTX + TPGS. The xenograft tumor model studies on nude mice indicated that PTX-MM inhibits tumor growth more effectively than other formulations. It was also found that most of mixed micelles were integral in tumor site to exhibit anti-cancer activity. Our results suggested that the use of PTX-MM as an anti-cancer drug may be an effective approach to treat lung cancer.
authors.affiliation: Department of Cardiothoracic Surgery, First Affiliated Hospital, Soochow University, Suzhou 215006, China Department of Thoracic Surgery, Second Affiliated Hospital of Southeast University, Nanjing 210003, China.
authors.forename: Guojin
authors.initials: G
authors.lastname: Huang
authors.affiliation: Department of Cardiothoracic Surgery, First Affiliated Hospital, Soochow University, Suzhou 215006, China Department of Thoracic Surgery, Huai'an First People's Hospital, Nanjing Medical University, Huai'an 223300, China.
authors.forename: Bao
authors.initials: B
authors.lastname: Zang
authors.affiliation: Department of Thoracic Surgery, Huai'an First People's Hospital, Nanjing Medical University, Huai'an 223300, China.
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Wang
authors.affiliation: Department of Orthopaedics, Huai'an First People's Hospital, Nanjing Medical University, Huai'an 223300, China.
authors.forename: Gang
authors.initials: G
authors.lastname: Liu
authors.affiliation: Department of Thoracic Surgery, Huai'an First People's Hospital, Nanjing Medical University, Huai'an 223300, China zangbaofq@sina.com.
authors.forename: Jianqiang
authors.initials: J
authors.lastname: Zhao
mesh_terms: D000072283:A549 Cells; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry*; D001682:Biological Availability; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy*; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D031541:Fluorescence Resonance Energy Transfer; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008175:Lung Neoplasms / Q000188:drug therapy*; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008823:Micelles; D053758:Nanoparticles / Q000737:chemistry*; D017239:Paclitaxel / Q000008:administration & dosage*; D012997:Solvents / Q000737:chemistry; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D008823:Micelles; D012997:Solvents; D017239:Paclitaxel
keywords: lung cancer; nanoparticle; paclitaxel (PTX)