Abstract：
Local administration of drugs at tumor sites over an extended period of time shows potential as a promising approach for cancer treatment. In the present study, the temperature-induced phase transition of chitosan and poloxamer 407 is used to construct an injectable hydrogel encapsulating 5-FU-loaded nanoerythrosome (5-FU-NER-gel). The 5-FU-NERs were found to be spherical, measuring approximately 115 ± 20 nm in diameter and having a surface potential of -7.06 ± 0.4. The drug loading efficiency was approximately 40 %. In situ gel formation took place within 15 s when the gel was exposed to body temperature or subcutaneous injection. A sustained release profile was observed at pH 7.4 and 6.8, with a total 5-FU release of 76.57 ± 4.4 and 98.07 ± 6.31 in 24 h, respectively. MTT, Live/dead, and migration assays confirmed the cytocompatibility of the drug carrier and its effectiveness as a chemotherapeutic formulation. After in vivo antitumor assessment in a subcutaneous autograft model, it was demonstrated that tumor growth inhibition in 14 days was 90 %. Therefore, the obtained injectable chitosan-based hydrogel containing 5-FU-loaded nanoerythrosomes illustrated promising potential as a candidate for local and enhanced delivery of chemotherapeutics at the tumor site.
摘要：
在肿瘤部位长期局部施用药物显示出作为癌症治疗的有希望的方法的潜力。在本研究中,壳聚糖和泊洛沙姆407的温度诱导的相变用于构建包封5-FU负载的纳米红细胞体(5-FU-NER-凝胶)的可注射水凝胶。发现5-FU-NER是球形的，测量直径约为115±20nm，表面电势为-7.06±0.4。药物装载效率约为40%。当凝胶暴露于体温或皮下注射时，在15s内发生原位凝胶形成。在pH7.4和6.8下观察到持续释放曲线，24小时内5-FU总释放量为76.57±4.4和98.07±6.31，分别。MTT,活/死,和迁移试验证实了药物载体的细胞相容性及其作为化疗制剂的有效性。在皮下自体移植模型中进行体内抗肿瘤评估后，结果表明，14天内肿瘤生长抑制为90%。因此,所获得的含有负载5-FU的纳米红细胞体的基于壳聚糖的可注射水凝胶显示出作为在肿瘤部位局部和增强化疗药物递送的候选药物的有希望的潜力。
