Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology, 4 Raja S.C. Mullick Road, Kolkata, 700032, India.
Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus, Kolkata, India.
Pharm Res. 2020 Feb 18;37(3):56. doi: 10.1007/s11095-020-2758-5.
Curcumin (CUR), an antioxidant with p-glycoprotein inhibiting activity may be encapsulated with gemcitabine (GEM) as nanosuspension to enhance its anticancer potentiality synergistically.
Folate conjugated single (CUR/GEM) and dual (CUR + GEM) drug-loaded nanoformulations were prepared and evaluated for P-glycoprotein-1 (pgy-1) gene resistance, followed by in vitro cellular uptake and cytotoxicity assay in cells. The in vivo biodistribution and scintigraphic imaging was done after radiolabeling the nanoparticles with Technetium (99Tc). The tumor inhibition study was conducted in nude mice bearing MDA-MB-231 xenografts.
The folate conjugated dual drug formulations (FCGNPs) gave better results in suppressing the pgy-1 gene and also showed higher cellular uptake, cytotoxicity, apoptosis, and cell cycle arrest. The radiolabeled nanoformulations were highly stable and FCGNPs showed higher accumulation in the MDA-MB-231 tumor region than folate unconjugated dual drug NPs (CGNPs) as evidenced by scintigraphic imaging and biodistribution studies. The in vivo therapeutic efficacy of FCGNPs was higher compared to unconjugated and respective single-drug formulations.
Two drugs in one platform lower breast adenocarcinoma by lowering drug resistance and improving cytotoxic effects.
姜黄素（CUR）是一种具有 P 糖蛋白抑制活性的抗氧化剂，可与吉西他滨（GEM）一起封装成纳米混悬剂，以协同增强其抗癌潜力。
制备叶酸偶联单（CUR/GEM）和双（CUR+GEM）载药纳米制剂，并对其进行 P 糖蛋白-1（pgy-1）基因耐药性评估，随后进行细胞内摄取和细胞毒性测定。用锝（99Tc）标记纳米粒后进行体内生物分布和闪烁成像。在荷 MDA-MB-231 异种移植瘤的裸鼠中进行肿瘤抑制研究。
叶酸偶联双药制剂（FCGNPs）在抑制 pgy-1 基因方面效果更好，且细胞摄取、细胞毒性、细胞凋亡和细胞周期阻滞作用更高。放射性标记的纳米制剂高度稳定，FCGNPs 在 MDA-MB-231 肿瘤部位的积累高于叶酸未偶联双药 NPs（CGNPs），这一点通过闪烁成像和生物分布研究得到了证实。与未偶联和相应的单药制剂相比，FCGNPs 的体内治疗效果更高。
一个平台上的两种药物可通过降低耐药性和提高细胞毒性作用来降低乳腺癌的发生率。
