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基于三元共轭物的pH响应性10-羟基喜树碱前药纳米胶束递送系统的药代动力学

Pharmacokinetics of a ternary conjugate based pH-responsive 10-HCPT prodrug nano-micelle delivery system.

作者信息

Liu Yang, Li Juan, Li Zhi, Tang Xing, Zhang Zhenzhong

机构信息

School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.

School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, China.

出版信息

Asian J Pharm Sci. 2017 Nov;12(6):542-549. doi: 10.1016/j.ajps.2017.05.005. Epub 2017 May 23.

Abstract

A pH-responsive conjugate based 10-hydroxycamptothecin-thiosemicarbazide-polyethene glycol 2000 (10-HCPT-hydro-PEG) nano-micelles were prepared in our previous study. In the present study, ultra-performance liquid chromatography (UPLC-MS) method is developed to investigate its pharmacokinetics and biodistribution in tumor bearing mice. The results demonstrated that the conjugate circulated for a much longer time in the blood circulation system than commercial 10-HCPT injection, and bioavailability was significantly improved compared with 10-HCPT. biodistribution study showed that the conjugate could enhance the targeting and residence time in tumor site.

摘要

在我们之前的研究中制备了一种基于pH响应性共轭物的10-羟基喜树碱-硫代氨基脲-聚乙二醇2000(10-HCPT-hydro-PEG)纳米胶束。在本研究中,开发了超高效液相色谱(UPLC-MS)方法来研究其在荷瘤小鼠体内的药代动力学和生物分布。结果表明,与市售10-HCPT注射液相比,该共轭物在血液循环系统中的循环时间长得多,并且与10-HCPT相比生物利用度显著提高。生物分布研究表明,该共轭物可以增强在肿瘤部位的靶向性和停留时间。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbc3/7032114/5df9f732c775/ajps443-ga-5001.jpg

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