摘要
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 cypate niosomes as a drug delivery system,to characterize its physicochemical properties,and to determine its photothermal effects in vitro and in vivo. Methods： The niosomes were prepared by solvent injection method, and characterized by investigation of their morphology, particle size,encapsulation efficiency and photothermal heating effect in vitro. Through the cytotoxicity experiment,tissue distribution and thermal imaging,photothermal effect of the niosomes in vivo and in vitro were determined. Results：The average diameter of the prepared spherical niosomes was（ 190. 1 ± 0. 42） nm,with the encapsulation efficiency of 95. 95%. Under the laser irradiation,the photothermal heating effect of the niosomes in vitro increased by12. 4%. Compared with the free drug,the niosomes inhibited the growth of 4T1 cells in vitro significantly with the IC50 value decreasing by 74. 01%（ P 0. 01）. The tissue distribution of cypate niosomes in the tumor-bearing mice showed the highest amount of cypate in the tumor,which was 1. 51 ~ 3. 92 times more than it in other organs. The results of thermal imaging showed that when the tumor-bearing mice were treated with cypate niosomes at the doses of 3. 0 and 5. 0 mg·kg^-1,the temperature achieved in the tumor site was getting to 50 ℃,which would be the temperature of thermal ablation. Conclusion： The prepared cypate niosomes show good physical properties,and their positive targeting effect and photothermal effects are demonstrated in the cell and the animal experiments. Theniosomes will be a promising candidate of novel delivery system for photothermal therapeutic antitumor drug with good prospect.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2016年第11期1275-1280,共6页
Chinese Journal of New Drugs
基金
国家自然科学基金资助项目(81473166)
关键词
光热效应
碳菁类染料
泡囊
抗癌作用
photothermal effect
carbocyanine dyes
niosome
antitumor effects
