Aim: The aim of this study was to improve solubility and antitumour ability in vitro of tetrandrine (Tet) via preparing nanosuspensions (NSs).

Methods: The Tet-NSs were prepared by wet media milling. The Tet-CCS-NS was prepared with croscarmellose sodium (CCS) as single stabiliser. The Tet-HACC-TPGS-NS was manufactured with D-α-tocopheryl polyethylene glycol 1,000 succinate (TPGS) and hydroponically trimethyl ammonium chloride chitosan (HACC) as combined stabilisers. Physicochemical properties of the NSs such as particle size, surface morphologies, crystallinity and molecular interactions were investigated. In addition, the in vitro dissolution and antitumour activities using A549 human lung cancer cells were evaluated.

Results: The mean particle sizes and Zeta potential of freshly prepared Tet-CCS-NS, Tet-HACC-TPGS-NS were 469.1 ± 14nm and 157.3 ± 5nm, −29.4 ± 0.26 mV and 23.3 ± 0.36 mV, respectively. In comparison to pure Tet, the cumulative dissolution of Tet-NSs were increased by 4 ∼ 5 times in 2 h. In vitro antitumour studies on Tet- NSs in A549 cells, the cell survival rate of the Tet-NSs at high concentration (30-50µg/ml) were less than 10% within 48 h. Meanwhile, Tet-NSs were revealed to induce A549 cells apoptosis and promote cell uptake.

Conclusion: The present study has proved that the Tet-NSs can increase Tet solubility as well as improve Tet antitumour activity in vitro.

目的：本研究的目的是通过制备纳米悬浮液（NSs）来提高粉防己碱（Tet）的体外溶解度和抗肿瘤能力。

方法：通过湿法研磨制备Tet-NS。用交联羧甲基纤维素钠（CCS）作为单一稳定剂制备Tet-CCS-NS。Tet-HACC-TPGS-NS是由D-α-生育酚聚乙二醇1,000琥珀酸酯（TPGS）和亲水性三甲基氯化铵壳聚糖（HACC）制成的稳定剂。研究了NS的理化性质，例如粒径，表面形态，结晶度和分子相互作用。另外，评估了使用A549人肺癌细胞的体外溶解和抗肿瘤活性。

结果：新鲜制备的Tet-CCS-NS，Tet-HACC-TPGS-NS的平均粒径和Zeta电位分别为469.1±14nm和157.3±5nm，-29.4±0.26 mV和23.3±0.36 mV。与纯Tet相比，Tet-NS的累积溶解在2小时内增加了4到5倍。对A549细胞中Tet-NSs的体外抗肿瘤研究表明，高浓度（30-50μg/ ml）的Tet-NSs在48小时内的细胞存活率不到10％。同时，发现Tet-NSs诱导A549细胞凋亡并促进细胞摄取。

结论：本研究证明，Tet-可奈米球可提高溶解性的Tet以及改善的Tet的抗肿瘤活性在体外。