基于还原门控的pH转变点可调递送系统用于肿瘤精准成像

doi:10.3969/j.issn.1006-7795.2026.03.003

首都医科大学学报 ›› 2026, Vol. 47 ›› Issue (3): 417-427.doi: 10.3969/j.issn.1006-7795.2026.03.003

• 从分子机制到临床应用:创新药物新突破 • 上一篇下一篇

基于还原门控的pH转变点可调递送系统用于肿瘤精准成像

夏鹤铭^1#,周步舒^2,3#,汪贻广^2,3,陈斌龙^2,3*

1.北京大学第三医院药学部，北京 100191；2.北京大学药学院药剂学系，北京 100191；3.天然药物及仿生药物全国重点实验室，北京 100191

收稿日期:2026-02-02 修回日期:2026-03-13 出版日期:2026-06-21 发布日期:2026-06-26
通讯作者: 陈斌龙 E-mail:binlong.chen@pku.edu.cn
基金资助:
国家自然科学基金青年科学基金项目(B 类,82522084)，国家自然科学基金面上项目(82373804)，北京市科技新星计划项目(20250484828)。

A reduction-gated pH transition-switchable delivery system for precise tumor imaging

Xia Heming^1#， Zhou Bushu^2,3#， Wang Yiguang^2,3， Chen Binlong^2,3*

1.Department of Pharmacy, Peking University Third Hospital, Beijing 100191, China; 2.Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China; 3.State Key Laboratory of Natural and Biomimetic Drugs, Beijing 100191, China

Received:2026-02-02 Revised:2026-03-13 Online:2026-06-21 Published:2026-06-26
Supported by:
This study was supported by National Natural Science Foundation of China(82522084 and 82373804), Beijing Nova Program (20250484828 ).

摘要/Abstract

摘要： 目的探讨基于还原门控的pH转变点可调递送系统（reduction-gated pH transition-switchable delivery system, RPS）在肿瘤成像中的效率与机制。方法合成还原敏感单体（HEMA-SS-C3和AMA-SS-C3），通过原子转移自由基聚合制备不同比例聚合物，并构建纳米胶束。通过动态光散射、荧光光谱、磁共振氢谱表征聚合物以及胶束的理化性质；利用流式细胞术和小动物活体成像评价细胞摄取及体内肿瘤成像效果。结果 RPS胶束粒径为30~50 nm，还原响应后pH转变点由5.5上调至6.5，体外细胞摄取显著提高；体内成像显示，RPS胶束具有良好的肿瘤成像效应。结论 RPS具有还原门控介导的pH转变点可调特性，为肿瘤精准成像及药物递送提供了新的设计理念及研究基础。

关键词: 智能响应型递送系统, 肿瘤微环境, 还原响应, 谷胱甘肽, pH超敏感聚合物, 肿瘤成像

Abstract: Objective To investigate the efficiency and mechanism of the reduction-gated pH transition-switchable delivery system (RPS) in tumor imaging. Methods Reduction-sensitive monomers (HEMA-SS-C3 and AMA-SS-C3) were synthesized, and polymers with different monomer ratios were prepared via atom transfer radical polymerization (ATRP) to construct RPS polymers. The physicochemical properties of polymers and micelles were characterized by using dynamic light scattering (DLS), fluorescence spectroscopy, and nuclear magnetic resonance hydrogen spectroscopy (1H-NMR). Cellular uptake and in vivo tumor imaging effects were evaluated through flow cytometry and living imaging system. Results The RPS micelles exhibited a particle size of 30-50 nm. After reduction response, the pH transition point increased from approximately 5.5 to 6.5, and in vitro cellular uptake was significantly enhanced. In vivo imaging revealed that RPS micelles exhibited favorable tumor-imaging effects. Conclusion RPS possesses a reduction-gated pH transition-tunable property, providing a novel design concept and research basis for precise tumor imaging and drug delivery.

Key words: stimuli-responsive delivery system, tumor microenvironment, reduction response, glutathione, ultra-pH-sensitive polymers, tumor imaging

中图分类号:

R318.08
R943

夏鹤铭, 周步舒, 汪贻广, 陈斌龙. 基于还原门控的pH转变点可调递送系统用于肿瘤精准成像[J]. 首都医科大学学报, 2026, 47(3): 417-427.

Xia Heming, Zhou Bushu, Wang Yiguang, Chen Binlong . A reduction-gated pH transition-switchable delivery system for precise tumor imaging[J]. Journal of Capital Medical University, 2026, 47(3): 417-427.

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基于还原门控的pH转变点可调递送系统用于肿瘤精准成像

A reduction-gated pH transition-switchable delivery system for precise tumor imaging

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