Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University, Lucknow, India.
Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, PR China.
J Liposome Res. 2021 Sep;31(3):304-315. doi: 10.1080/08982104.2020.1820520. Epub 2020 Sep 23.
β-sitosterol (BS), a phytosterol, exhibits ameliorative effects on hepatocellular carcinoma (HCC) due to its antioxidant activities. However, its poor aqueous solubility and negotiated bioavailability and short elimination half-life is a huge limitation for its therapeutic applications. To overcome these two shortcomings, BS-loaded niosomes were made to , film hydration method and process parameters were optimized using a three-factor Box-Behnken design. The optimized formulation (BSF) was further surface-modified with polyethylene glycol (PEG). The resulting niosomes (BSMF) have spherical shapes, particle sizes, 219.6 ± 1.98 nm with polydispersity index (PDI) and zeta potential of 0.078 ± 0.04 and -19.54 ± 0.19 mV, respectively. The drug loading, entrapment efficiency, and drug release at 24 h of the BSMF were found to be 16.72 ± 0.09%, 78.04 ± 0.92%, and 75.10 ± 3.06%, respectively. Moreover, BSMF showed significantly greater cytotoxic potentials on Hep G2 cells with an enhanced cellular uptake relative to pure BS and BSF. The BSMF also displayed potentially improved curative property of HCC in albino wistar rat. Thus, the BSMF could be one of the promising therapeutic modalities for HCC treatment in terms of targeting potential resulting in enhanced therapeutic efficacy.
β-谷甾醇（BS）是一种植物甾醇，由于其抗氧化活性，对肝细胞癌（HCC）具有改善作用。然而，其较差的水溶性和协商生物利用度以及短的消除半衰期对其治疗应用是一个巨大的限制。为了克服这两个缺点，用 BS 制备了脂质体，采用三因素 Box-Behnken 设计优化了薄膜水化法和工艺参数。优化的配方（BSF）进一步用聚乙二醇（PEG）进行表面修饰。所得的脂质体（BSMF）具有球形形状、粒径为 219.6±1.98nm，多分散指数（PDI）和 Zeta 电位分别为 0.078±0.04 和-19.54±0.19mV。BSMF 的载药量、包封率和 24h 的药物释放分别为 16.72±0.09%、78.04±0.92%和 75.10±3.06%。此外，BSMF 对 Hep G2 细胞表现出显著更高的细胞毒性潜力，与纯 BS 和 BSF 相比，具有增强的细胞摄取。BSMF 还显示出在白化 Wistar 大鼠中可能改善 HCC 的治疗作用。因此，BSMF 可能是 HCC 治疗的一种有前途的治疗方法，具有靶向潜力，从而提高治疗效果。
