Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology, Kolkata, India.
Advanced Pharmacognosy Research Laboratory, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
Sci Rep. 2017 Apr 3;7(1):530. doi: 10.1038/s41598-017-00696-6.
Garcinol (GAR) is a naturally occurring polyisoprenylated phenolic compound. It has been recently investigated for its biological activities such as antioxidant, anti-inflammatory, anti ulcer, and antiproliferative effect on a wide range of human cancer cell lines. Though the outcomes are very promising, its extreme insolubility in water remains the main obstacle for its clinical application. Herein we report the formulation of GAR entrapped PLGA nanoparticles by nanoprecipitation method using vitamin E TPGS as an emulsifier. The nanoparticles were characterized for size, surface morphology, surface charge, encapsulation efficiency and in vitro drug release kinetics. The MTT assay depicted a high amount of cytotoxicity of GAR-NPs in B16F10, HepG2 and KB cells. A considerable amount of cell apoptosis was observed in B16f10 and KB cell lines. In vivo cellular uptake of fluorescent NPs on B16F10 cells was also investigated. Finally the GAR loaded NPs were radiolabeled with technetium-99m with >95% labeling efficiency and administered to B16F10 melanoma tumor bearing mice to investigate the in vivo deposition at the tumor site by biodistribution and scintigraphic imaging study. In vitro cellular uptake studies and biological evaluation confirm the efficacy of the formulation for cancer treatment.
姜黄素（GAR）是一种天然存在的多异戊二烯基酚类化合物。最近研究发现，它具有抗氧化、抗炎、抗溃疡和抗增殖作用，对多种人类癌细胞系均有抑制作用。尽管结果非常有前景，但它在水中的极度不溶性仍然是其临床应用的主要障碍。在此，我们报道了通过纳米沉淀法用维生素 E TPGS 作为乳化剂制备 GAR 包封的 PLGA 纳米粒。对纳米粒的粒径、表面形态、表面电荷、包封效率和体外药物释放动力学进行了表征。MTT 试验表明 GAR-NPs 在 B16F10、HepG2 和 KB 细胞中具有高细胞毒性。在 B16f10 和 KB 细胞系中观察到大量细胞凋亡。还研究了荧光 NPs 在 B16F10 细胞上的体内细胞摄取。最后，用 >95%的标记效率用锝-99m 标记载 GAR 的 NPs，并将其施用于 B16F10 黑色素瘤荷瘤小鼠，通过生物分布和闪烁成像研究来研究在肿瘤部位的体内沉积情况。体外细胞摄取研究和生物学评价证实了该制剂在癌症治疗中的功效。
