Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005, UP, India.
Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005, UP, India.
Carbohydr Polym. 2015 Oct 5;130:9-17. doi: 10.1016/j.carbpol.2015.04.062. Epub 2015 May 8.
Soluthin MD(®), a unique phosphatidylcholine-maltodextrin based hydrophilic lipopolysaccharide, which exhibits superior biocompatibility and bioavailability enhancer properties for poorly water soluble drug(s). Curcumin (CUR) is a potential natural anticancer drug with low bioavailability due to poor aqueous solubility. The study aims at formulation and optimization of CUR loaded lipopolysaccharide nanocarriers (C-LPNCs) to enhance oral bioavailability and anticancer efficacy in colon-26 tumor-bearing mice in vitro and in vivo. The Optimized C-LPNCs demonstrated favorable mean particle size (108 ± 3.4 nm) and percent entrapment efficiency (65.29 ± 1.0%). Pharmacokinetic parameters revealed ∼130-fold increase in oral bioavailability and cytotoxicity studies demonstrated ∼23-fold reduction in 50% cell growth inhibition when treated with optimized C-LPNCs as compared to pure CUR. In vivo anticancer study performed with optimized C-LPNCs showed significant increase in efficacy compared with pure CUR. Thus, lipopolysaccharide nanocarriers show potential delivery strategy to improve oral bioavailability and anticancer efficacy of CUR in the treatment of colorectal cancer.
水飞蓟素 MD（®），一种独特的基于磷脂酰胆碱-麦芽糊精的亲水性脂多糖，具有优越的生物相容性和生物利用度增强特性，可用于改善水溶性差的药物（s）。姜黄素（CUR）是一种具有低生物利用度的潜在天然抗癌药物，由于其水溶性差，导致其生物利用度低。本研究旨在制备和优化姜黄素负载的脂多糖纳米载体（C-LPNCs），以提高其在体外和体内结肠-26 荷瘤小鼠中的口服生物利用度和抗癌疗效。优化的 C-LPNCs 表现出良好的平均粒径（108 ± 3.4nm）和包封效率（65.29 ± 1.0%）。药代动力学参数显示，与纯姜黄素相比，口服生物利用度提高了约 130 倍，细胞毒性研究显示，用优化的 C-LPNCs 处理时，细胞生长抑制率降低了约 23 倍。与纯姜黄素相比，用优化的 C-LPNCs 进行的体内抗癌研究显示出显著提高的疗效。因此，脂多糖纳米载体显示出具有潜力的递药策略，可提高姜黄素在治疗结直肠癌中的口服生物利用度和抗癌疗效。
