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

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

doi:10.1016/j.ajps.2017.05.005

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

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

Authors

Yang Liu^{1

2

3}, Juan Li², Zhi Li², Xing Tang¹, Zhenzhong Zhang²

Affiliations

¹ School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
² School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou 450001, China.
³ Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Zhengzhou 450001, China.

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. In vivo biodistribution study showed that the conjugate could enhance the targeting and residence time in tumor site.

Keywords: 10-Hydroxycamptothecin; Conjugate; Nano-micelle; PH-responsive; Pharmacokinetics.