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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Preparation and characterisation of tetrandrine nanosuspensions and in vitro estimate antitumour activity on A549 lung cancer cell line
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Preparation and characterisation of tetrandrine nanosuspensions and in vitro estimate antitumour activity on A549 lung cancer cell line

机译：A549肺癌细胞系斯坦宁纳米粒子和体外估计抗肿瘤活性的制备与表征

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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-alpha-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 similar to 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 (30-50 mu g/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.
机译：目的：通过制备纳米混悬剂（NSs），提高粉防己碱（Tet）的溶解度和体外抗肿瘤能力。方法：采用湿磨法制备Tet-NSs。以交联羧甲基纤维素钠（CCS）为单一稳定剂制备了Tet-CCS-NS。以D-α-生育酚聚乙二醇1000琥珀酸酯（TPGS）和水培三甲基氯化铵壳聚糖（HACC）为复合稳定剂，制备了Tet-HACC-TPGS NS。研究了NSs的粒径、表面形貌、结晶度和分子相互作用等物理化学性质。此外，还评估了A549人肺癌细胞的体外溶出和抗肿瘤活性。结果：新制备的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+/-0.26mv和23.3+/-0.36mv。与纯Tet相比，Tet NSs的累积溶出度在2小时内增加了4倍，相当于5倍。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低于10%。同时，Tet NSs可诱导A549细胞凋亡并促进细胞摄取。结论：本研究证明Tet NSs在体外能增加Tet的溶解度，提高Tet的抗肿瘤活性。

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