School of Pharmacy, Hangzhou Medical College, Hangzhou, 310013, People's Republic of China.
Department of Traditional Chinese Medicine, Zhejiang Pharmaceutical University, Ningbo, 315500, People's Republic of China.
Int J Nanomedicine. 2024 Jan 25;19:787-803. doi: 10.2147/IJN.S431599. eCollection 2024.
Tetrandrine (Tet), a bisbenzylisoquinoline alkaloid, is a potential candidate for cancer chemotherapy. However, Tet has poor aqueous solubility and a short half-life, which limits its bioavailability and efficacy. Liposomes have been widely utilized to enhance the bioavailability and efficacy of drugs.
In this study, Tet-loaded stealth liposomes (S-LPs@Tet) were prepared by ethanol injection method. Furthermore, physicochemical characterisation, biopharmaceutical behaviour, therapeutic efficacy, and biocompatibility of S-LPs@Tet were assessed.
The prepared S-LPs@Tet had an average particle size of 65.57 ± 1.60 nm, a surface charge of -0.61 ± 0.10 mV, and an encapsulation efficiency of 87.20% ± 1.30%. The S-LPs@Tet released Tet in a sustained manner, and the results demonstrated that the formulation remained stable for one month. More importantly, S-LPs significantly enhanced the inhibitory ability of Tet on the proliferation and migration of lung cancer cells, and enabled Tet to escape phagocytosis by immune cells. Furthermore, in vivo studies confirmed the potential for long-circulation and potent tumor-suppressive effects of S-LPs@Tet. Moreover, ex vivo and in vivo safety experiments demonstrated that the carrier material S-LPs exhibited superior biocompatibility.
Our research suggested that S-LPs@Tet has potential applications in lung cancer treatment.
汉防己甲素（Tet）是一种双苄基异喹啉生物碱，是癌症化疗的潜在候选药物。然而，Tet 的水溶性差，半衰期短，限制了其生物利用度和疗效。脂质体已广泛用于提高药物的生物利用度和疗效。
本研究采用乙醇注入法制备汉防己甲素载药隐形脂质体（S-LPs@Tet）。并对 S-LPs@Tet 的理化性质、生物药剂学行为、治疗效果和生物相容性进行了评估。
所制备的 S-LPs@Tet 的平均粒径为 65.57 ± 1.60nm，表面电荷为-0.61 ± 0.10mV，包封率为 87.20% ± 1.30%。S-LPs@Tet 以持续的方式释放 Tet，结果表明该制剂在一个月内保持稳定。更重要的是，S-LPs 显著增强了 Tet 对肺癌细胞增殖和迁移的抑制能力，并使 Tet 能够逃避免疫细胞的吞噬作用。此外，体内研究证实了 S-LPs@Tet 具有长循环和强大的肿瘤抑制作用的潜力。此外，离体和体内安全性实验表明载体材料 S-LPs 具有优异的生物相容性。
我们的研究表明 S-LPs@Tet 具有在肺癌治疗中的应用潜力。
