Riccardi Claudia, Fàbrega Carme, Grijalvo Santiago, Vitiello Giuseppe, D'Errico Gerardino, Eritja Ramon, Montesarchio Daniela
Department of Chemical Sciences, University of Naples Federico II, Via Cintia 21, I-80126, Napoli, Italy.
J Mater Chem B. 2018 Sep 7;6(33):5368-5384. doi: 10.1039/c8tb01563e. Epub 2018 Aug 10.
Niosomes are self-assembled vesicles made up of single chain non-ionic surfactants combined with appropriate amounts of cholesterol or other lipids, exploited as carriers for hydrophilic or lipophilic drugs. Compared to liposomes, niosomes are typically more stable, less expensive and, being generally obtained from synthetic surfactants, more easily derivatizable, providing vesicular structures with a higher versatility and chemical diversity. Herein, we investigated the physico-chemical and biological properties of niosomes loaded with two active ingredients, i.e. the nucleolipidic Ru(iii)-complex HoThyRu, selected as an anticancer agent, and the nucleolin-targeting AS1411 aptamer, allowing selective recognition of cancer cells. The morphology, average size, zeta potential, electrophoretic mobility, and stability over time of the functionalized niosomes were analyzed using different biophysical techniques. These formulations, tested on both cancer and normal cells, showed promising antiproliferative activity on HeLa cells, with a higher efficacy associated with the nanosystems containing both AS1411 and HoThyRu with respect to the controls. In all the tested cell lines, AS1411 proved to markedly enhance the bioactivity of the Ru(iii)-containing niosomes.
非离子表面活性剂囊泡是由单链非离子表面活性剂与适量胆固醇或其他脂质组合而成的自组装囊泡，用作亲水性或亲脂性药物的载体。与脂质体相比，非离子表面活性剂囊泡通常更稳定、成本更低，并且由于通常由合成表面活性剂制备，更易于衍生化，从而为囊泡结构提供更高的通用性和化学多样性。在此，我们研究了负载两种活性成分的非离子表面活性剂囊泡的物理化学和生物学性质，这两种活性成分分别是被选作抗癌剂的核脂质钌（III）配合物HoThyRu，以及能够选择性识别癌细胞的核仁素靶向AS1411适配体。使用不同的生物物理技术分析了功能化非离子表面活性剂囊泡的形态、平均尺寸、zeta电位、电泳迁移率和随时间的稳定性。这些制剂在癌细胞和正常细胞上进行了测试，结果显示对HeLa细胞具有良好的抗增殖活性，相对于对照，含有AS1411和HoThyRu的纳米系统具有更高的疗效。在所有测试的细胞系中，AS1411均显著增强了含钌（III）非离子表面活性剂囊泡的生物活性。
