A Supramolecular Nanovehicle Featuring a pH/Enzyme Co‐Response for Targeted Delivery of the Antitumor Compound

Author:

Nie Zhengquan1,Zhu Fangdao1,Chen Shuai1,Xu Junxin1,Yang Jianmei1,He Junnan1,Liu Xiaoqing2,Zhao Yan1ORCID,Zhang Jin1

Affiliation:

1. College of Chemistry and Chemical Engineering Yunnan Normal University Kunming 650500 P. R. China

2. Shenzhen Kewode Technology Co., Ltd Shenzhen 518028 P. R. China

Abstract

AbstractTriptolide (TPL) has gained much attention as an antitumor compound with potential applications. However, TPL suffers from low bioavailability, severe toxic side effects, and limited targeted uptake by tumor cells, thus restricting the conversion of its clinical application. Here, a supramolecular nanovehicle, named TSCD/MCC NPs, featuring pH/AChE co‐response was designed and prepared for loading, delivery, and targeted release of TPL. The cumulative release rate of TPL from TPL@TSCD/MCC NPs reached ∼90 % within 60 h at pH 5.0 and AChE co‐stimulation. Bhaskar model is used to study TPL release procedure. In cell experiments, TPL@TSCD/MCC NPs showed high toxicity to the four tumor cells lines A549, HL‐60, MCF‐7, and SW480, and favorable biosafety to normal cells BEAS‐2B. Furthermore, TPL@TSCD/MCC NPs containing relatively small amounts of TPL presented similar apoptosis rates to those of intrinsic TPL. We anticipate that TPL@TSCD/MCC NPs may facilitate the conversion of TPL into clinical applications through further studies.

Publisher

Wiley

Subject

General Chemistry

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