title: Preparation, characterization, and efficacy of thermosensitive liposomes containing paclitaxel.
abstract: To increase the anti-tumor activity of paclitaxel (PTX), novel temperature-sensitive liposomes loading paclitaxel (PTX-TSL) were developed. In vitro, characteristics of PTX-TSL were evaluated. The mean particle diameter was about 100 nm, and the entrapment efficiency was larger than 95%. The phase-transition temperature of PTX-TSL determined by differential scanning calorimetry was about 42 °C. The result of in vitro drug release from PTX-TSL illustrated that release rate at 37 °C was obviously lower than that at 42 °C. Stability data indicated that the liposome was physically and chemically stable for at least 3 months at -20 °C. In vivo study, after three injections with hyperthermia in the xenograft lung tumor model, PTX-TSL showed distinguished tumor growth suppression, compared with non-temperature-sensitive liposome and free drug. The results of intratumoral drug concentration indicated that PTX-TSL combined with hyperthermia delivered more paxlitaxel into the tumor location than the other two paxlitaxel formulations. In summary, PTX-TSL combined with hyperthermia significantly inhibited tumor growth, due to the increased targeting efficiency of PTX to tumor tissues. Such approach may enhance the delivery efficiency of chemotherapeutics into solid tumors.
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .|b State Key Laboratory of Toxicology and Medical Countermeasures , Beijing , China .
authors.forename: Zhi-Yuan
authors.initials: ZY
authors.lastname: Wang
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .|b State Key Laboratory of Toxicology and Medical Countermeasures , Beijing , China .
authors.forename: Hui
authors.initials: H
authors.lastname: Zhang
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .|b State Key Laboratory of Toxicology and Medical Countermeasures , Beijing , China .
authors.forename: Yang
authors.initials: Y
authors.lastname: Yang
authors.affiliation: c Wuhan General Hospital of Guangzhou Military Command , Wuhan , China , and.
authors.forename: Xiang-Yang
authors.initials: XY
authors.lastname: Xie
authors.affiliation: d Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College , Beijing , China.
authors.forename: Yan-Fang
authors.initials: YF
authors.lastname: Yang
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .|b State Key Laboratory of Toxicology and Medical Countermeasures , Beijing , China .
authors.forename: Zhiping
authors.initials: Z
authors.lastname: Li
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .
authors.forename: Ying
authors.initials: Y
authors.lastname: Li
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .|b State Key Laboratory of Toxicology and Medical Countermeasures , Beijing , China .
authors.forename: Wei
authors.initials: W
authors.lastname: Gong
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .|b State Key Laboratory of Toxicology and Medical Countermeasures , Beijing , China .
authors.forename: Fang-Lin
authors.initials: FL
authors.lastname: Yu
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .|b State Key Laboratory of Toxicology and Medical Countermeasures , Beijing , China .
authors.forename: Zhenbo
authors.initials: Z
authors.lastname: Yang
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .|b State Key Laboratory of Toxicology and Medical Countermeasures , Beijing , China .
authors.forename: Ming-Yuan
authors.initials: MY
authors.lastname: Li
authors.affiliation: a Beijing Institute of Pharmacology and Toxicology , Beijing , China .|b State Key Laboratory of Toxicology and Medical Countermeasures , Beijing , China .
authors.forename: Xing-Guo
authors.initials: XG
authors.lastname: Mei
mesh_terms: D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D004317:Doxorubicin / Q000737:chemistry / Q000493:pharmacokinetics*; D065546:Drug Liberation; D005334:Fever; D006801:Humans; D008081:Liposomes; D008175:Lung Neoplasms / Q000737:chemistry / Q000503:physiopathology*; D017239:Paclitaxel / Q000737:chemistry / Q000493:pharmacokinetics*; D044366:Transition Temperature; D023041:Xenograft Model Antitumor Assays
chemical_list: D008081:Liposomes; D004317:Doxorubicin; D017239:Paclitaxel
keywords: Antitumor efficiency; control release; drug delivery; hyperthermia; temperature-sensitivity