2. Academic Validation
  3. A single molecule carrier for ocular posterior segment diseases

A single molecule carrier for ocular posterior segment diseases

  • J Control Release. 2024 Dec:376:1316-1328. doi: 10.1016/j.jconrel.2024.10.052.
Xiao-Ling Zhang 1,  Yu-Xin Yue 2,  Yang Yang 1,  An-Kang Ying 2,  Rong Ma 2,  Jie Chen 2,  Fang-Yuan Chen 2,  Xiao-Yun Hou 1,  Yu-Chen Pan 2,  Da-Zhuang Ren 1,  Tao Yang 1,  Zhi-Qing Li 3,  Dong-Sheng Guo 4
Affiliations

Affiliations

  • 1 Tianjin Key Laboratory of Retinal Functions and Diseases, Tianjin Branch of National Clinical Research Center for Ocular Disease, Eye Institute and School of Optometry, Tianjin Medical University Eye Hospital, Tianjin 300392, China.
  • 2 Tianjin Eye Hospital, College of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Key Laboratory of Functional Polymer Materials (Ministry of Education), Frontiers Science Center for New Organic Matter, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Nankai University, Tianjin 300071, China.
  • 3 Tianjin Key Laboratory of Retinal Functions and Diseases, Tianjin Branch of National Clinical Research Center for Ocular Disease, Eye Institute and School of Optometry, Tianjin Medical University Eye Hospital, Tianjin 300392, China. Electronic address: drzhiqing_li@163.com.
  • 4 Tianjin Eye Hospital, College of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Key Laboratory of Functional Polymer Materials (Ministry of Education), Frontiers Science Center for New Organic Matter, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Nankai University, Tianjin 300071, China. Electronic address: dshguo@nankai.edu.cn.
PMID: 39490420 DOI: 10.1016/j.jconrel.2024.10.052
Abstract

Eye drops are envisaged as the most promising non-invasive formulation for the treatment of the ocular posterior segment diseases, while it is hindered by a series of complex ocular barriers, both static and dynamic in nature. In this context, we propose a single molecule nanomedicine based on host-guest chemistry to achieve highly efficient drug delivery targeted to ocular posterior segment. Sulfonated azocalix[4]arene (SAC4A) serves as the single molecule carrier, owing the multiple features of small size (24.0 Å in length, 21.2 Å in width, 14.8 Å in height with a Van der Waals volume of 930 Å3), negative charge, hydrophilicity, loading universality and hypoxia-triggered release. As a proof-of-concept, an eye drop formed by the complexation of SAC4A with sunitinib (SUN) is prepared to treat wet age-related macular degeneration (wAMD). SAC4A successfully transports SUN to the ocular posterior segment (the amount of SUN reaching the retinal-choroid tissue in the SUN@SAC4A group was 2.47 times larger than that in the SUN group at 30 min), significantly enhancing its anti-choroidal neoangiogenesis effect of SUN to wAMD, which played a key role in the treatment. We believe that the single molecule nanomedicine paradigm is highly amenable for treating various ocular posterior segment diseases in the future.

Keywords

Drug delivery; Eye drop; Host-guest recognition; Ocular posterior segment disease; Single molecule carrier.

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