a Faculdade Guairacá , Guarapuava , Brazil.
b Laboratory of Pharmaceutical Nanotechnology , Universidade Estadual do Centro-Oeste/UNICENTRO , Guarapuava , Brazil.
J Microencapsul. 2018 Aug;35(5):467-474. doi: 10.1080/02652048.2018.1526340. Epub 2018 Nov 30.
Curcumin is a natural compound presenting important antitumour activity. However, due to its low aqueous solubility, instability at physiological pH, and low oral bioavailability, its clinical use is limited. Bovine serum albumin (BSA) nanoparticles have been used as drug carriers to improve the drug properties. In this work, curcumin-loaded BSA nanoparticles were developed and the in vitro cytotoxicity over murine melanoma cells and the in vivo antitumour activity in a murine melanoma model were assessed. Nanoparticles presented 150 nm, polydispersity index of 0.16, negative zeta potential, and 45% of curcumin encapsulation efficiency. Curcumin release from nanoparticles was slow and diffusion dependent. In the cytotoxicity assay, free curcumin was more efficient than curcumin-loaded nanoparticles, probably due to the prolonged curcumin release from nanoparticles. However, in a murine melanoma model, curcumin-loaded nanoparticles presented higher antitumour efficiency than free curcumin. BSA nanoparticles are efficient curcumin carriers that may have relevant applications in melanoma treatment.
姜黄素是一种具有重要抗肿瘤活性的天然化合物。然而，由于其在水中的溶解度低、在生理 pH 值下不稳定以及口服生物利用度低，其临床应用受到限制。牛血清白蛋白（BSA）纳米粒已被用作药物载体以改善药物性质。在这项工作中，开发了负载姜黄素的 BSA 纳米粒，并评估了其对小鼠黑色素瘤细胞的体外细胞毒性和在小鼠黑色素瘤模型中的体内抗肿瘤活性。纳米粒的粒径为 150nm，多分散指数为 0.16，表面带负电荷，姜黄素包封效率为 45%。纳米粒中姜黄素的释放是缓慢的，并且依赖于扩散。在细胞毒性试验中，游离姜黄素比负载姜黄素的纳米粒更有效，这可能是由于纳米粒中姜黄素的释放时间延长。然而，在小鼠黑色素瘤模型中，负载姜黄素的纳米粒比游离姜黄素具有更高的抗肿瘤效率。BSA 纳米粒是有效的姜黄素载体，可能在黑色素瘤治疗中有相关应用。
