General Nanomedicine Platform by Solvent-Mediated Disassembly/Reassembly of Scalable Natural Polyphenol Colloidal Spheres
Yi Zeng, Xiangyu Chen, Guangcan Chen, Zhiwen Deng, Qiulan Tong, Zhe Sun, Xiaomin Ma, Wen Su, Lei Ma, Yaqin Ran, Xudong Li
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.