Jiangsu Key Laboratory for Supramolecular Medicinal Materials and Applications, College of Life Sciences, Nanjing Normal University, China.
AAPS PharmSciTech. 2011 Jun;12(2):665-72. doi: 10.1208/s12249-011-9631-0. Epub 2011 May 17.
Hydroxypropyl-sulfobutyl-β-cyclodextrin (HP-SBE-β-CD) inclusion complex was developed and used as a drug delivery system for DTX (DTX/HP-SBE-β-CD). The objective of the present study was to evaluate and compare the biological properties of DTX/HP-SBE-Β-CD with Taxotere®. The pharmacokinetics, biodistribution, antitumor efficacy in vivo and in vitro, and safety evaluation of DTX/HP-SBE-β-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-β-CD had similar pharmacokinetic properties and antitumor efficacy both in vitro and in vivo as Taxotere®. Fortunately, this new drug delivery system attenuated the side effects when used in vivo. As a consequence, DTX/HP-SBE-β-CD may be a promising alternative to Taxotere® 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-β-CD for possible use against human tumors.
羟丙基磺丁基-β-环糊精（HP-SBE-β-CD）包合物被开发并用作 DTX（DTX/HP-SBE-β-CD）的药物递送系统。本研究的目的是评估和比较 DTX/HP-SBE-β-CD 与 Taxotere®的生物学特性。研究了 DTX/HP-SBE-β-CD 的药代动力学、生物分布、体内和体外抗肿瘤疗效以及安全性评价。最显著的发现是有可能为 DTX 制备不含聚山梨酯 80 的包合物。基于药代动力学、生物分布和抗肿瘤疗效的研究表明，DTX/HP-SBE-β-CD 在体内和体外均具有与 Taxotere®相似的药代动力学特性和抗肿瘤疗效。幸运的是，这种新的药物递送系统减轻了体内使用时的副作用。因此，DTX/HP-SBE-β-CD 可能是 Taxotere®治疗癌症的有前途的替代品，可降低副作用。在一项严格的研究中，对多种人类肿瘤的治疗潜力和低毒性表明，DTX/HP-SBE-β-CD 可能具有临床应用于人类肿瘤的潜力。
