Citation: Yi Li, Jianbin Shi, Xinxin Sun, Zhixiao Zhang, Jin Sun, Zhonggui He, Cong Luo, Shenwu Zhang. Small-molecule self-assembled nanodrugs: Molecular design, assembly dynamics and biomedical applications[J]. Chinese Chemical Letters, ;2026, 37(11): 112266. doi: 10.1016/j.cclet.2025.112266 shu

Small-molecule self-assembled nanodrugs: Molecular design, assembly dynamics and biomedical applications

Yi Li ^{a, 1} ,
Jianbin Shi ^{a, 1} ,
Xinxin Sun ^a ,
Zhixiao Zhang ^c ,
Jin Sun ^{a, b} ,
Zhonggui He ^{a, b} ,
Cong Luo ^{a, b, *,} ,
Shenwu Zhang ^{a, *,}

a.
Department of Pharmaceutics, Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China
b.
Joint International Research Laboratory of Intelligent Drug Delivery Systems, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China
c.
Department of Pharmacy, The First Affiliated Hospital of Jinzhou Medical University, Jinzhou 121000, China

luocong@syphu.edu.cn

zhangshenwu@syphu.edu.cn

Received Date: 21 August 2025
Revised Date: 9 December 2025
Accepted Date: 10 December 2025
Available Online: 13 December 2025

Figures(3)

Small-molecule self-assembled nanodrugs (SMSNDs), as an emerging therapeutic strategy in nanomedicine, have shown great potential for biomedical applications. SMSNDs are created through the spontaneous assembly of small molecules via non-covalent interactions, which provides structural flexibility, responsiveness to stimuli, and a high capacity for drug loading. These features improve drug solubility, facilitate targeted delivery, reduce systemic toxicity, and enhance therapeutic accuracy. They hold significant promise across various biomedical fields, including cancer, cardiovascular and cerebrovascular diseases, neurodegenerative and metabolic diseases management, and antimicrobial therapy. This review first explores the assembly mechanisms, drug release strategies, and structural patterns of SMSNDs. Additionally, it thoroughly presents the research progress of SMSNDs in various biological applications, including diagnostics and therapeutics. Finally, the review addresses the challenges faced by SMSNDs. It discusses future directions for their development, aiming to provide a solid theoretical foundation and practical guidance for the clinical translation of these nanodrugs.
- Small-molecule,
- Self-assembled nanodrugs,
- Assembly and release mechanism,
- Structural patterns of SMSNDs,
- Biomedical applications
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沈阳化工大学材料科学与工程学院沈阳 110142