Pharmacokinetics, Efficacy, and Safety Evaluation of Docetaxel/Hydroxypropyl-Sulfobutyl-beta-Cyclodextrin Inclusion Complex

作者：Huang, Xing-Xing; Zhou, Cheng-Liang; Wang, Hui; Chen, Cheng; Yu, Shu-Qin^*; Xu, Qian; Zhu, Yin-Yan; Ren, Yong

来源：AAPS PHARMSCITECH, 2011, 12(2): 665-672.

DOI：10.1208/s12249-011-9631-0

• antitumor efficacy
• biodistribution
• DTX/HP-SBE-beta-CD
• pharmacokinetics
• safety evaluation

Hydroxypropyl-sulfobutyl-beta-cyclodextrin (HP-SBE-beta-CD) inclusion complex was developed and used as a drug delivery system for DTX (DTX/HP-SBE-beta-CD). The objective of the present study was to evaluate and compare the biological properties of DTX/HP-SBE-I'-CD with TaxotereA (R). The pharmacokinetics, biodistribution, antitumor efficacy in vivo and in vitro, and safety evaluation of DTX/HP-SBE-beta-CD were studied. The most significant finding was that it was possible to prepare a Polysorbate-80-free inclusion complex for DTX. Studies based on pharmacokinetics, biodistribution, and antitumor efficacy indicated that DTX/HP-SBE-beta-CD had similar pharmacokinetic properties and antitumor efficacy both in vitro and in vivo as TaxotereA (R). Fortunately, this new drug delivery system attenuated the side effects when used in vivo. As a consequence, DTX/HP-SBE-beta-CD may be a promising alternative to TaxotereA (R) for cancer chemotherapy treatment with reduced side effects. The therapeutic potential against a variety of human tumors and low toxicity demonstrated in a stringent study clearly warrant clinical investigation of DTX/HP-SBE-beta-CD for possible use against human tumors.

• 出版日期2011-6
• 单位东南大学; 南京师范大学