Preparation, characterization, and pharmacodynamics of thermosensitive liposomes containing docetaxel.
A novel thermosensitive liposome (TL) containing docetaxel (DTX) was designed to enhance DTX-targeted delivery and antitumor effect. TL loading DTX (DTX-TL) were prepared by thin film hydration. The mean particle size of the liposomes was about 100 nm, and the drug entrapment efficiency was more than 95%. The phase transition temperature of liposomes was about 42 °C. In vitro drug release showed that drug released at 37 °C was obviously less than that at 42 °C. For in vivo experiments, the human breast tumor model was established by subcutaneous xenotransplantation on nude mice; liposomes and injection containing DTX were injected i.v. in nude mice, followed by exposure of the tumors to hyperthermia (HT) for 30 min after administration. The tumor inhibition ratio of DTX-TL group was significantly higher than the normal injection group. Combining TL with HT enhanced the delivery of DTX and thereby its antitumor effects. The liposomes reported in this paper could potentially produce viable clinical strategies for improved targeting and delivery of DTX for the treatment of breast cancer.
Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P.R. China.
Hui
H
Zhang
Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P.R. China.
Wei
W
Gong
Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P.R. China.
Zhi-Yuan
ZY
Wang
Beijing Institute of Radiation Medicine, Beijing 100850 P.R. China.
Shou-Jun
SJ
Yuan
Wuhan General Hospital of Guangzhou Military Command, Wuhan 430070P.R. China.
Xiang-Yang
XY
Xie
Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P.R. China.
Yan-Fang
YF
Yang
Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P.R. China.
Yang
Y
Yang
Beijing Institute of Radiation Medicine, Beijing 100850 P.R. China.
Shan-Shan
SS
Wang
Beijing Institute of Radiation Medicine, Beijing 100850 P.R. China.
De-Xuan
DX
Yang
Beijing Institute of Radiation Medicine, Beijing 100850 P.R. China.
Zi-Xue
ZX
Xuan
Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P.R. China. Electronic address: newdds@126.com.
Xing-Guo
XG
Mei
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D002152:Calorimetry, Differential Scanning; D000077143:Docetaxel; D004337:Drug Carriers; D004339:Drug Compounding / Q000379:methods*; D065546:Drug Liberation; D005260:Female; D006801:Humans; D006979:Hyperthermia, Induced; D008081:Liposomes; D061986:MCF-7 Cells; D008819:Mice, Nude; D010316:Particle Size; D043823:Taxoids / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D044366:Transition Temperature; D023041:Xenograft Model Antitumor Assays
D000970:Antineoplastic Agents; D004337:Drug Carriers; D008081:Liposomes; D043823:Taxoids; D000077143:Docetaxel
antitumor effect; controlled release; docetaxel; drug delivery systems; hyperthermia; liposomes; nanotechnology; pharmacodynamics; thermosensitive; thin film hydration