载姜黄素的 Pluronic/Polycaprolactone 胶束在结直肠腺癌细胞中的体外细胞毒性和细胞摄取。

In vitro cytotoxicity and cellular uptake of curcumin-loaded Pluronic/Polycaprolactone micelles in colorectal adenocarcinoma cells.

机构信息

Division of Biosurface Technology, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences & Technology, Poojappura, Thiruvananthapuram, Kerala 695012, India.

出版信息

J Biomater Appl. 2013 Mar;27(7):811-27. doi: 10.1177/0885328211427473. Epub 2012 Jan 24.

Abstract

Clinical application of curcumin has been limited due to poor aqueous solubility and consequently minimal systemic bioavailability. We investigated the preparation of curcumin-loaded micelles based on amphiphilic Pluronic/Polycaprolactone (Pluronic/PCL) block copolymer, which proved to be efficient in enhancing curcumin's aqueous solubility. Curcumin-loaded micelles of size below 200 nm was characterized by dynamic light scattering and transmission electron microscopy. The critical micelle concentration (CMC) of the amphiphilic polymer was determined using pyrene as a fluorescent probe. Hemolysis and aggregation studies were investigated to evaluate the blood compatibility of the micelles. Sodium dodecyl sulphate polyacrylamide gel electrophoresis was performed to study the stability of the micelles toward plasma proteins. In vitro cytotoxicity and cellular uptake of the curcumin-loaded micelles were demonstrated in colorectal adenocarcinoma (Caco2) cells. The results indicated that Pluronic/PCL micelles could be a promising candidate for curcumin delivery to cancer cells.

摘要

姜黄素的临床应用受到其较差的水溶性和极低的系统生物利用度的限制。我们研究了基于两亲性 Pluronic/聚己内酯(Pluronic/PCL)嵌段共聚物的载姜黄素胶束的制备,结果证明该胶束能有效提高姜黄素的水溶性。通过动态光散射和透射电子显微镜对粒径小于 200nm 的载姜黄素胶束进行了表征。使用芘作为荧光探针测定了两亲性聚合物的临界胶束浓度(CMC)。通过溶血和聚集研究评估了胶束的血液相容性。通过十二烷基硫酸钠聚丙烯酰胺凝胶电泳研究了胶束对血浆蛋白的稳定性。在结肠直肠腺癌(Caco2)细胞中证明了载姜黄素胶束的体外细胞毒性和细胞摄取。结果表明,Pluronic/PCL 胶束可能是一种有前途的姜黄素递药载体,用于向癌细胞输送姜黄素。

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