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Lipid Prodrug Nanoassemblies via Dynamic Covalent Boronates
Yuxun Ding1, Xiaowen Hu1,2, Yinzi Piao1,2
1Translational Medicine Laboratory, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou Institute, University of Chinese Academy of Sciences, Wenzhou, Zhejiang 325001, China.
ACS Nano
|March 31, 2023
Summary
Researchers developed novel lipid prodrug nanoassemblies (LPNAs) using dynamic covalent chemistry. These LPNAs offer targeted drug delivery, controlled release, and enhanced therapeutic efficacy against pathogens and cancer cells.
Area of Science:
- Biomaterials Science
- Nanomedicine
- Drug Delivery Systems
Background:
- Prodrug nanoassemblies merge prodrug benefits with nanomedicine for targeted delivery and controlled release.
- Current methods for preparing lipid prodrug nanoassemblies (LPNAs) lack facile pathways.
Purpose of the Study:
- To develop a facile method for creating lipid prodrug nanoassemblies (LPNAs).
- To characterize the properties and therapeutic potential of these novel LPNAs.
Main Methods:
- Utilized dynamic covalent boronate chemistry between catechol and boronic acid to form LPNAs.
- Demonstrated encapsulation and delivery of model drugs: ciprofloxacin, bortezomib, and miconazole.
- Evaluated *in vitro* and *in vivo* efficacy of LPNAs against pathogens and cancer cells.
Main Results:
- Successfully synthesized LPNAs with dynamic covalent drug loading.
- Observed charge reversal in acidic microenvironments and triggered release in acidic/oxidative conditions.
- LPNAs exhibited enhanced efficacy in eradicating pathogens and cancer cells compared to free drugs.
Conclusions:
- The developed methodology provides a facile route to LPNAs with tunable properties.
- These LPNAs show significant potential for improved drug delivery and clinical applications.
- Dynamic covalent chemistry offers a promising strategy for advanced nanomedicine development.

