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多西他赛与磺丁基醚β-环糊精的包合物：制备、体外细胞毒性及体内安全性

Inclusion Complex of Docetaxel with Sulfobutyl Ether β-Cyclodextrin: Preparation, In Vitro Cytotoxicity and In Vivo Safety.

作者信息

Ren Lili, Yang Xiaolong, Guo Weilu, Wang Jin, Chen Guoguang

机构信息

School of Pharmacy, Nanjing Tech University, 5th Mofan Road, Nanjing 210094, China.

Department of Microbiology and Immunology, Stanford University, Stanford, CA 94305, USA.

出版信息

Polymers (Basel). 2020 Oct 13;12(10):2336. doi: 10.3390/polym12102336.

DOI:10.3390/polym12102336
PMID:33066097
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7601231/
Abstract

Docetaxel (DTX), as a first-line anti-tumor drug, has been studied for decades for its diverse bioactivities. However, DTX presents poor solubility in water, low bioavailability and serious toxic side effects which has hindered its application in the clinic. To address these problems, docetaxel-sulfobutyl ether-β-cyclodextrin inclusion complex (DTX-SBE-β-CD) was prepared successfully by saturated aqueous solution method. Sulfobutyl ether β-cyclodetrin (SBE-β-CD) is used as delivery material. For this study, the inclusion complex of docetaxel with sulfobutyl ether β-cyclodetrin (DTX-SBE-β-CD) was prepared and optimized its properties to enhance the cytotoxicity of cancer cells. A large number of physical characterization results showed that DTX-SBE-β-CD inclusion complex was successfully prepared by saturated aqueous solution method. DTX-SBE-β-CD inclusion complex was optimized by Central Composite Design. DTX-SBE-β-CD had an inhibitory effect on the in vitro determination of MCF-7 and HepG2 cells by MTT assay. Pharmacokinetic studies were carried out on male Sprague-Dawley rats by tail injection, including the distribution, metabolism and elimination of DTX-SBE-β-CD in vivo. In the experimental study of inhibition of cancer cells, DTX and DTX-SBE-β-CD showed apparent concentration-dependent inhibitory actions on tumor cells and the inhibition of DTX-SBE-β-CD group was more obvious.

摘要

多西他赛（DTX）作为一线抗肿瘤药物，因其多样的生物活性已被研究了数十年。然而，多西他赛在水中溶解度低、生物利用度低且毒副作用严重，这阻碍了其在临床上的应用。为了解决这些问题，采用饱和水溶液法成功制备了多西他赛-磺丁基醚-β-环糊精包合物（DTX-SBE-β-CD）。磺丁基醚β-环糊精（SBE-β-CD）用作递送材料。本研究制备了多西他赛与磺丁基醚β-环糊精的包合物（DTX-SBE-β-CD），并优化其性质以增强对癌细胞的细胞毒性。大量物理表征结果表明，通过饱和水溶液法成功制备了DTX-SBE-β-CD包合物。采用中心复合设计对DTX-SBE-β-CD包合物进行优化。通过MTT法体外测定，DTX-SBE-β-CD对MCF-7和HepG2细胞有抑制作用。通过尾静脉注射对雄性Sprague-Dawley大鼠进行药代动力学研究，包括DTX-SBE-β-CD在体内的分布、代谢和消除。在癌细胞抑制实验研究中，DTX和DTX-SBE-β-CD对肿瘤细胞均表现出明显的浓度依赖性抑制作用，且DTX-SBE-β-CD组的抑制作用更明显。

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