Ding Yuxun, Hu Xiaowen, Piao Yinzi, Huang Rong, Xie Lingping, Yan Xiaojian, Sun Hui, Li Yuanfeng, Shi Linqi, Liu Yong
Translational Medicine Laboratory, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou Institute, University of Chinese Academy of Sciences, Wenzhou, Zhejiang 325001, China.
College of Materials Science and Optoelectronic Technology, University of Chinese Academy of Sciences, Beijing 100049, China.
ACS Nano. 2023 Apr 11;17(7):6601-6614. doi: 10.1021/acsnano.2c12233. Epub 2023 Mar 31.
Prodrug nanoassemblies combine the advantages of prodrug and nanomedicines, offering great potential in targeting the lesion sites and specific on-demand drug release, maximizing the therapeutic performance while minimizing their side effects. However, there is still lacking a facile pathway to prepare the lipid prodrug nanoassemblies (LPNAs). Herein, we report the LPNAs via the dynamic covalent boronate between catechol and boronic acid. The resulting LPNAs possess properties like drug loading in a dynamic covalent manner, charge reversal in an acidic microenvironment, and specific drug release at an acidic and/or oxidative microenvironment. Our methodology enables the encapsulation and delivery of three model drugs: ciprofloxacin, bortezomib, and miconazole. Moreover, the LPNAs are often more efficient in eradicating pathogens or cancer cells than their free counterparts, both and . Together, our LPNAs with intriguing properties may boost the development of drug delivery and facilitate their clinical applications.
前药纳米组装体结合了前药和纳米药物的优点，在靶向病变部位和特定的按需药物释放方面具有巨大潜力，可在将副作用降至最低的同时最大化治疗效果。然而，目前仍缺乏一种简便的途径来制备脂质前药纳米组装体（LPNAs）。在此，我们报道了通过儿茶酚和硼酸之间的动态共价硼酸酯制备LPNAs。所得的LPNAs具有以动态共价方式载药、在酸性微环境中电荷反转以及在酸性和/或氧化微环境中特定药物释放等特性。我们的方法能够包封和递送三种模型药物：环丙沙星、硼替佐米和咪康唑。此外，LPNAs在根除病原体或癌细胞方面通常比其游离对应物更有效，无论是在体外还是体内。总之，我们具有有趣特性的LPNAs可能会推动药物递送的发展并促进其临床应用。
