Red blood cells (RBCs) are an excellent choice for cell preparation research because of their biocompatibility, high drug loading, and long half-life. In this study, doxorubicin (DOX) was encapsulated with RBCs as the carrier. The biotin-avidin system binding principle was used to modify biotinylated cyclic arginine-glycine-aspartic acid (cRGD) onto RBC surfaces for accurate targeting, high drug loading, and sustained drug release. The RBC drug delivery system (DDS) was characterized, and the concentration of surface sulfur in the energy spectrum was 6.330%. The physical and chemical properties of RBC DDS were as follows: drug content, 0.857 mg/mL; particle size, 3339 nm; potential value, −12.5 mV; and cumulative release rate, 81.35%. There was no significant change in RBC morphology for up to seven days. The results of the targeting and cytotoxicity studies of RBC DDS showed that many RBCs covered the surfaces of U251 cells, and the fluorescence intensity was higher than that of MCF-7 cells. The IC₅₀ value of unmodified drug-loaded RBCs was 2.5 times higher than that of targeted modified drug-loaded RBCs, indicating that the targeting of cancer cells produced satisfactory inhibition. This study confirms that the RBC DDS has the characteristics of accurate targeting, high drug loading, and slow drug release, which increases its likelihood of becoming a clinical cancer treatment in the future.

红细胞 (RBC) 因其生物相容性、高载药量和长半衰期而成为细胞制备研究的绝佳选择。本研究以红细胞为载体封装阿霉素（DOX）。利用生物素-亲和素系统结合原理将生物素化的环精氨酸-甘氨酸-天冬氨酸（cRGD）修饰到红细胞表面，以实现精确靶向、高载药量和持续药物释放。对红细胞给药系统（DDS）进行表征，能谱中表面硫浓度为6.330%。RBC DDS的理化性质如下：药物含量，0.857mg/mL；粒径，3339 nm；电位值，-12.5 mV；累计释放率为81.35%。长达 7 天的红细胞形态没有显着变化。红细胞DDS的靶向性和细胞毒性研究结果显示，U251细胞表面有大量红细胞覆盖，荧光强度高于MCF-7细胞。未修饰载药红细胞的IC ₅₀值比靶向修饰载药红细胞高2.5倍，表明对癌细胞的靶向产生了令人满意的抑制作用。该研究证实RBC DDS具有靶向精准、载药量高、药物释放缓慢的特点，这增加了其未来成为临床癌症治疗药物的可能性。