Introduction: Ginsenoside Rh2, purified from the Panax ginseng root, has been demonstrated to possess anticancer properties against various cancerous cells including colorectal, breast, skin, ovarian, prostate, and liver cancerous cells. However, the poor bioavailability, low stability on gastrointestinal systems, and fast plasma elimination limit further clinical applications of Ginsenoside Rh2 for cancer treatments. In this study, a novel formulation of niosomal Ginsenoside Rh2 was prepared using the thin film hydration technique.
Methods: The niosomal formulation contained Span 60 and cholesterol, and cationic lipid DOTAP was evaluated by determining particle size distribution, encapsulation efficiency, the polydispersity index (PDI), and surface morphology. The cytotoxic effects of free Ginsenoside Rh2 and Ginsenoside Rh2-loaded niosomes were determined using the MTT method in the PC3 prostate cancer cell line. For the investigation of the in vitro cellular uptake of Ginsenoside Rh2-loaded niosome, two formulations were prepared: the Ginsenoside Rh2-loaded niosomal formula containing 5% DOTAP and the Ginsenoside Rh2-loaded niosomal formula without DOTAP.
Results: The mean size, DPI, zeta potential, and encapsulation efficiency of the Ginsenoside Rh2-loaded nanoniosomal formulation containing DOTAP were 93.5± 2.1 nm, 0.203± 0.01, +4.65± 0.65, and 98.32% ± 2.4, respectively. The niosomal vesicles were found to be round and have a smooth surface. The release profile of Ginsenoside Rh2 from niosome was biphasic. Furthermore, a two-fold reduction in the Ginsenoside Rh2 concentration was measured when Ginsenoside Rh2 was administered in a nanoniosomal form compared to free Ginsenoside Rh2 solutions in the PC3 prostate cancer cell line. After storage for 90 days, the encapsulation efficiency, vesicle size, PDI, and zeta potential of the optimized formulation did not significantly change compared to the freshly prepared samples. The cellular uptake experiments of the niosomal formulation demonstrated that by adding DOTAP to the niosomal formulation, the cellular uptake was enhanced.
Discussion: The enhanced cellular uptake and cytotoxic activity of the Ginsenoside Rh2 nanoniosomal formulation on the PC3 cell make it an attractive candidate for application as a nano-sized delivery vehicle to transfer Ginsenoside Rh2 to cancer cells.

Keywords: nanoniosomal, Ginsenoside Rh2, chemotherapy, PC3 prostate cancer cell line


中文翻译：

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评估一种新的人参皂甙 Rh2 纳米脂质体制剂以增强对前列腺癌的抗肿瘤功效：一项体外研究。

简介：从人参根中纯化的人参皂甙 Rh2已被证明对各种癌细胞具有抗癌特性，包括结肠直肠癌、乳腺癌、皮肤癌、卵巢癌、前列腺癌和肝癌细胞。然而，人参皂苷Rh2生物利用度差、对胃肠系统稳定性低和血浆清除快限制了人参皂苷Rh2在癌症治疗中的进一步临床应用。在这项研究中，使用薄膜水合技术制备了一种新的人参皂苷 Rh2 制剂。
方法：niosomal 制剂含有 Span 60 和胆固醇，阳离子脂质 DOTAP 通过测定粒度分布、包封效率、多分散指数 (PDI) 和表面形态来评估。使用 MTT 方法在 PC3 前列腺癌细胞系中测定了游离人参皂苷 Rh2 和负载人参皂苷 Rh2 的 niosomes 的细胞毒性作用。为了研究负载人参皂苷 Rh2 的脂质体的体外细胞摄取，制备了两种制剂：含有 5% DOTAP 的负载人参皂苷 Rh2 的脂质体配方和不含 DOTAP 的负载人参皂苷 Rh2 的脂质体配方。
结果：含有 DOTAP 的负载人参皂甙 Rh2 的纳米脂质体制剂的平均尺寸、DPI、zeta 电位和包封效率分别为 93.5±2.1 nm、0.203±0.01、+4.65±0.65 和 98.32%±2.4。发现 niosomal 囊泡是圆形的并且具有光滑的表面。niosome 中人参皂甙Rh2 的释放曲线是双相的。此外，与 PC3 前列腺癌细胞系中的游离人参皂甙 Rh2 溶液相比，当人参皂甙 Rh2 以纳米脂质体形式给药时，人参皂甙 Rh2 浓度降低了两倍。储存 90 天后，优化配方的包封率、囊泡大小、PDI 和 zeta 电位与新鲜制备的样品相比没有显着变化。
讨论：人参皂甙 Rh2 纳米脂质体制剂对 PC3 细胞的增强细胞摄取和细胞毒活性使其成为将人参皂甙 Rh2 转移到癌细胞的纳米递送载体的有吸引力的候选者。

关键词：纳米脂质体，人参皂甙Rh2，化疗，PC3前列腺癌细胞系