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溶剂介导的可扩展天然多酚胶体球的解体/重组的通用纳米医学平台。

General Nanomedicine Platform by Solvent-Mediated Disassembly/Reassembly of Scalable Natural Polyphenol Colloidal Spheres.

机构信息

National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, P. R. China.

Engineering Research Center in Biomaterials, Sichuan University, Chengdu 610064, P. R. China.

出版信息

ACS Appl Mater Interfaces. 2020 Aug 26;12(34):37914-37928. doi: 10.1021/acsami.0c11650. Epub 2020 Aug 14.

Abstract

The current strategy using the assembly of medicines and active functional molecules to develop nanomedicines often requires both molecules to have a specific matched chemical molecular structure; however, this is often difficult to predict, execute, and control in practical applications. Herein, we reported a general solvent-mediated disassembly/reassembly strategy for preparing nanomedicines based on epigallocatechin gallate (EGCG) active molecules. The polyphenol colloidal spheres (CSs) were self-assembled from molecular condensed EGCG in aqueous solution but disassembled in organic solvents and reassembled in aqueous solution. The solvent-mediated disassembly and reassembly capability of CSs gave rise to the active binding of condensed EGCG to various hydrophilic and hydrophobic guest molecules. The maximum encapsulation and drug-loading rate of reassembled CSs/DOX were 90 and 44%, respectively, and the nanomedicines could reverse drug resistance of tumor cells and exhibit enhanced therapeutic effects for breast cancer. Last but not least, 37.3 g of polyphenol CSs was massively produced at one time with a yield of 74.6%, laying a solid foundation for the practical applications of reassembled nanomedicines. The present strategy leading to a general nanomedicines platform was concise and highly efficient for both hydrophilic and hydrophobic drugs, making a breakthrough for low loading dilemma of current nanomedicines, and would open up a new direction for the preparation of nanocarriers, nanocomposites, and nanomedicines from natural polyphenols.

摘要

目前,利用药物和活性功能分子的组装来开发纳米药物的策略通常需要这两种分子具有特定的匹配化学分子结构;然而,在实际应用中,这往往很难预测、执行和控制。在此,我们报道了一种基于表没食子儿茶素没食子酸酯(EGCG)活性分子的通用溶剂介导的组装/解组装策略来制备纳米药物。多酚胶体球(CSs)在水溶液中由分子缩合的 EGCG 自组装而成,但在有机溶剂中解组装,并在水溶液中重新组装。CSs 的溶剂介导的解组装和再组装能力导致了缩合 EGCG 与各种亲水性和疏水性客体分子的有效结合。再组装的 CSs/DOX 的最大包封率和载药率分别为 90%和 44%,纳米药物可以逆转肿瘤细胞的耐药性,并表现出增强的乳腺癌治疗效果。最后但并非最不重要的是,一次大规模生产了 37.3 克多酚 CSs,产率为 74.6%,为再组装纳米药物的实际应用奠定了坚实的基础。这种导致通用纳米药物平台的策略对于亲水性和疏水性药物都简洁高效,突破了当前纳米药物载药量低的困境,为天然多酚制备纳米载体、纳米复合材料和纳米药物开辟了新的方向。

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