Yu Yue-Ming, Bu Fan-Zhi, Yu Yu, Yan Cui-Wei, Wu Zhi-Yong, Li Yan-Tuan
School of Medicine & Pharmacy & College of Marine Life Science, Ocean University of China, Qingdao, Shandong, 266003, China.
Laboratory for Marine Drugs & Bioproducts, Qingdao National Laboratory for Marine Science & Technology, Shandong, 266003, China.
Nanomedicine (Lond). 2022 Dec;17(30):2215-2229. doi: 10.2217/nnm-2022-0208. Epub 2023 Mar 17.
To explore how to transform cocrystals of the anticancer drug 5-fluorouracil (FL) with caffeic acid (CF; FL-CF-2HO) into a nanoformulation, a self-assembly strategy of cocrystal-loaded micelles is proposed. Nanomicelles were assembled to deliver cocrystal FL-CF-2HO with synergistic activity, and their / properties were evaluated by combining theoretical and experimental methods. More cocrystal was packed into the polymers due to the stronger interaction energy during micellar assembly, producing excellent cytotoxicity and pharmacokinetic behavior, especially synergistic abilities and long-term therapy. This case exemplifies the particular benefits of the self-assembly strategy of cocrystal-loaded micelles in keeping a delicate balance between long-term effects and high efficiency for FL, and offers a feasible technical scheme for cocrystal delivery agents for antitumor drugs.
为探索如何将抗癌药物5-氟尿嘧啶（FL）与咖啡酸（CF；FL-CF-2HO）的共晶体转化为纳米制剂，提出了一种载共晶体胶束的自组装策略。组装纳米胶束以递送具有协同活性的共晶体FL-CF-2HO，并通过理论和实验方法相结合对其性质进行评估。由于胶束组装过程中更强的相互作用能，更多的共晶体被包裹进聚合物中，产生了优异的细胞毒性和药代动力学行为，尤其是协同能力和长期治疗效果。该案例例证了载共晶体胶束自组装策略在保持FL的长期效果和高效性之间微妙平衡方面的特殊优势，并为抗肿瘤药物的共晶体递送剂提供了一种可行的技术方案。
