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目的:制备包载光热试剂碳菁类染料Cypate的泡囊,对其进行理化表征并考察其体内外光热效应。方法:采用溶剂注入法制备了Cypate泡囊,进行了形态、粒径和包封率考察,在激光照射下的体外升温效应考察,细胞毒性实验抑瘤作用考察,以荷瘤鼠的组织分布及热成像实验研究Cypate泡囊的光热效应。结果:制得的Cypate泡囊形态为球形、平均粒径(190.1±0.42)nm、包封率95.95%;Cypate以泡囊包载后,体外升温效果在激光照射下提高可达12.4%,抑制4T1肿瘤细胞生长的指标IC50降低74.01%(P<0.01),在荷瘤鼠的组织分布肿瘤部位最强,高于其他脏器1.51~3.92倍。荷瘤鼠的热成像结果显示,在激光照射下,浓度为3.0和5.0 mg·kg~(-1)的Cypate泡囊可使肿瘤部位达到消融肿瘤细胞的温度(>50℃)。结论:本研究Cypate泡囊性好,细胞实验、动物实验表明具有良好的被动靶向性和光热效应,是一种具有良好开发前景的新型光热治疗微粒传输系统。
OBJECTIVE: To prepare the cytoplasm of Cytoplasm containing photocytochemical reagent Cyatocyanine, and to study its physical and chemical properties and to examine its photothermal effects both in vitro and in vivo. Methods: Cypate vesicles were prepared by solvent injection method. Morphology, particle size and entrapment efficiency were investigated. The effect of heating in vitro under laser irradiation and the antitumor effect of cytotoxicity were investigated. Thermal imaging experiments study the photothermal effects of Cypate vesicles. Results: The morphology of Cypate vesicles was spherical with an average diameter of 190.1 ± 0.42 nm and the entrapment efficiency was 95.95%. After Cypate was encapsulated in vesicles, the heating effect in vitro was increased by 12.4% under laser irradiation, The IC50 of 4T1 tumor cells decreased by 74.01% (P <0.01). The tumor distribution in tumor-bearing mice was the strongest, 1.51-3.92 times higher than other organs. Thermal imaging of tumor-bearing mice showed that Cypate vesicles with 3.0 and 5.0 mg · kg -1 concentrations of laser irradiation could reach the site of ablation of tumor cells (> 50 ℃) under laser irradiation. Conclusion: This study shows that Cypate vesicles are good, cell experiments and animal experiments show that they have good passive targeting and photothermal effects. Therefore, it is a new photothermal therapy particle delivery system with good development prospects.