Department of Pharmaceutical Engineering, Xuzhou Pharmaceutical Higher Vocational School of Jiangsu Province, Xuzhou, China.
School of Pharmaceutical Sciences, Liaoning University, Shenyang, Liaoning, China.
Pak J Pharm Sci. 2023 Mar;36(2):483-490.
Piperlongumine (PL) is a biologically active alkaloid derived from peppers, has significant cytotoxic effects on cancer with no cytotoxicity. This study used Nab technology to prepare PL albumin nanoparticles (PL-BSA-NPs) to improve water solubility and bioavailability. We carried out a pharmacological evaluation of the PL-BSA-NPs. The morphological profile of the PL-BSA-NPs was relatively uniform, with an average particle size of approximately 210 nm, with drug load of 2.1% and encapsulation rate of 87.6%. PL-BSA-NPs were stable for 4 weeks when stored at 4°C. In vitro release behavior of the PL-BSA-NPs showed a sustained release, with a cumulative release of 67.24% in approximately 24 hours. The pharmacokinetic properties of PL-BSA-NPs were shown that PL-BSA-NPs could maintain a certain level of blood drug concentration for a long time, thus demonstrating the sustained release and increased bioavailability of PL. Finally, we investigated the in vitro antitumor activity of the PL-BSA-NPs and found that PL can significantly inhibit HepG2 cell proliferation, and that PL-BSA-NPs enhanced the inhibitory effect of PL on this proliferative effect. Thus, we concluded that PL can destroy liver cancer cells by increasing ROS levels. These results suggested that PL-BSA-NPs show promising potential as a targeted anti-tumor drug.
胡椒碱（PL）是一种从辣椒中提取的具有生物活性的生物碱，对癌症具有显著的细胞毒性作用而无细胞毒性。本研究采用 Nab 技术制备 PL 白蛋白纳米粒（PL-BSA-NPs）以提高其水溶性和生物利用度。我们对 PL-BSA-NPs 进行了药理学评价。PL-BSA-NPs 的形态学特征相对均匀，平均粒径约为 210nm，载药量为 2.1%，包封率为 87.6%。PL-BSA-NPs 在 4°C 下储存 4 周时稳定。PL-BSA-NPs 的体外释放行为呈持续释放，约 24 小时内累积释放 67.24%。PL-BSA-NPs 的药代动力学特性表明，PL-BSA-NPs 可以长时间维持一定的血药浓度水平，从而表现出 PL 的持续释放和生物利用度增加。最后，我们研究了 PL-BSA-NPs 的体外抗肿瘤活性，发现 PL 能显著抑制 HepG2 细胞增殖，PL-BSA-NPs 增强了 PL 对这种增殖作用的抑制作用。因此，我们得出结论，PL 可以通过增加 ROS 水平来破坏肝癌细胞。这些结果表明，PL-BSA-NPs 作为一种靶向抗肿瘤药物具有广阔的应用前景。
