5-fluorouracil-caffeic acid cocrystal delivery agent with long-term and synergistic high-performance antitumor
Yue-Ming Yu1,2, Fan-Zhi Bu1, Yu Yu3
1School of Medicine & Pharmacy & College of Marine Life Science, Ocean University of China, Qingdao, Shandong, 266003, China.
Abstract:
Aim: To explore how to transform cocrystals of the anticancer drug 5-fluorouracil (FL) with caffeic acid (CF; FL-CF-2H2O) into a nanoformulation, a self-assembly strategy of cocrystal-loaded micelles is proposed. Methods: Nanomicelles were assembled to deliver cocrystal FL-CF-2H2O with synergistic activity, and their in vitro/vivo properties were evaluated by combining theoretical and experimental methods. Result: 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. Conclusion: 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.
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