title: Self-assembled Micelle Loading Cabazitaxel for therapy of Lung Cancer.
abstract: Lung cancer is a leading cause of cancer deaths worldwide, chemotherapy has improved overall survival but remains limited at <12 months median overall survival. Cabazitaxel is hopeful to do the same in advanced lung cancer as well as in metastatic prostate cancer. However, its clinical application was restricted due to its high hydrophobicity and severe side effects. To overcome these problems, we developed self-assembled micelle loading cabazitaxel (CBZ-PM) for therapy of lung cancer. The CBZ-PM has high drug loading (10.52%) and encapsulation efficiency (99.30%) with particle size of 28.77 ± 0.52 nm and polydisperse index of 0.114 ± 0.012. The transmission electron microscope image presented its spherical and homogeneous appearance. In vitro release profile showed CBZ-PM has a sustained-release behavior. Furthermore, the result of cell proliferation assays proved that CBZ-PM could induce the Lewis lung carcinoma (LLC) cells death through G2/M arrest more effectively than free CBZ. In vivo anti-tumor activity of CBZ-PM was further studied in mice model of LLC. The tumor inhibitory rate of CBZ-PM was more than 50% and the survival time of LLC bearing mice was efficiently prolonged following administration of CBZ-PM. In addition, the immunohistochemical study showed that more apoptosis cells were detected in the tumor tissue of CBZ-PM group than that of the positive control group. All these indicated that CBZ-PM served as a potential anti-lung cancer agent.
authors.affiliation: Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; The 66007 Troops of Chinese People's Liberation Army, Baoding 072154, China.
authors.forename: Bo
authors.initials: B
authors.lastname: Zhuang
authors.affiliation: Center for Disease Prevention and Control of Jinan Military Command, Jinan 250014, China.
authors.forename: Liang
authors.initials: L
authors.lastname: Du
authors.affiliation: Wendeng Hospital of Tranditional Chinese Orthopedics and Traumatology of Shandong Province, Weihai 264400, China.
authors.forename: Hongxia
authors.initials: H
authors.lastname: Xu
authors.affiliation: Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
authors.forename: Xuelian
authors.initials: X
authors.lastname: Xu
authors.affiliation: Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China. Electronic address: cheng13980029671@163.com.
authors.forename: Cheng
authors.initials: C
authors.lastname: Wang
authors.affiliation: Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
authors.forename: Yingfang
authors.initials: Y
authors.lastname: Fan
authors.affiliation: Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
authors.forename: Mengyi
authors.initials: M
authors.lastname: Cong
authors.affiliation: Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
authors.forename: Jiaqi
authors.initials: J
authors.lastname: Yin
authors.affiliation: Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
authors.forename: Hongxia
authors.initials: H
authors.lastname: Li
authors.affiliation: Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
authors.forename: Huashi
authors.initials: H
authors.lastname: Guan
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy* / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D003692:Delayed-Action Preparations; D057927:Hydrophobic and Hydrophilic Interactions; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D008810:Mice, Inbred C57BL; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D015996:Survival Rate; D043823:Taxoids / Q000008:administration & dosage* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D008823:Micelles; D043823:Taxoids; C552428:cabazitaxel
keywords: Antitumor; Cabazitaxel; Cabazitaxel (PubChem CID: 9854073); Ethylene glycol (PubChem CID: 174); Lewis lung carcinoma; Polymeric micelle; Stannous octoate (PubChem CID: 9318); ε-Caprolactone (PubChem CID: 10401)