本研究的目的是开发叶酸（FA）接枝的混合聚合物胶束，负载柠檬酸他莫昔芬（TMXC），以增强其在乳腺组织中的抗肿瘤活性。缀合叶酸 Pluronic 123 (FA-P123) 使用羰基二咪唑交联剂化学制备，并使用 FTIR 和 1HNMR 进行确认。检查了负载 TMXC 的 P123/P84（未共轭）和负载 TMXC 的 FA-P123/P84（共轭）胶束的封装效率、粒径、表面电荷、体外药物释放、细胞毒性作用和乳腺癌细胞的细胞摄取线。负载TMXC的共轭胶束的纳米颗粒尺寸为35.01±1.20 nm，表面电荷为-20.50±0.95 mV，36小时后捕获87.83±5.10％的TMXC并释放67.58±2.47％的TMXC。与负载 TMXC 的未缀合胶束相比，缀合胶束表现出 MCF-7 细胞系对 TMXC 的明显更高的细胞摄取，并且体外细胞毒性提高了 2.48 倍。体内研究结果表明，与负载 TMXC 的未缀合胶束相比，负载 TMXC 的 FA-P123/P84 具有潜在的抗肿瘤活性，荷瘤小鼠的肿瘤体积显着减小。总之，所获得的结果表明，缀合的 FA-P123/P84 胶束可能成为使用 TMXC 治疗乳腺癌的令人鼓舞的载体。© 2023。作者。

The objective of this study was to develop folic acid (FA) grafted mixed polymeric micelles loaded with Tamoxifen citrate (TMXC) to enhance its antitumor activity in breast tissues. The conjugated folic acid Pluronic 123 (FA-P123) was prepared using carbonyl diimidazole cross-linker chemistry and confirmed using FTIR and 1HNMR. TMXC-loaded P123/P84 (unconjugated) and TMXC-loaded FA-P123/P84 (conjugated) micelles were examined for encapsulation efficiency, particle size, surface charge, in vitro drug release, cytotoxic effect, and cellular uptake by a breast cancer cell line. The conjugated TMXC-loaded micelle exhibited a nanoparticle size of 35.01 ± 1.20 nm, a surface charge of-20.50 ± 0.95 mV, entrapped 87.83 ± 5.10% and released 67.58 ± 2.47% of TMXC after 36 h. The conjugated micelles exhibited a significantly higher cellular uptake of TMXC by the MCF-7 cell line and improved in vitro cytotoxicity by 2.48 folds compared to the TMXC-loaded unconjugated micelles. The results of in vivo studies indicated that TMXC-loaded FA-P123/P84 has a potential antitumor activity, as revealed by a significant reduction of tumor volume in tumor-bearing mice compared to TMXC-loaded unconjugated micelles. In conclusion, the obtained results suggested that conjugated FA-P123/P84 micelles could be an encouraging carrier for the treatment of breast cancer with TMXC.© 2023. The Author(s).