Dipartimento di Scienze Fisiche e Chimiche, Università degli Studi dell'Aquila, Via Vetoio 10, 67100, Coppito (L'Aquila), Italy; CNR-Istituto per i Sistemi Biologici, Via Salaria km 29.300, 00016, Monterotondo Scalo (RM), Italy.
National Center for Drug Research and Evaluation, National Institute of Health, Viale Regina Elena 299, 00161, Rome, Italy.
Chem Phys Lipids. 2019 Sep;223:104781. doi: 10.1016/j.chemphyslip.2019.05.006. Epub 2019 Jun 20.
The plant alkaloid voacamine (VOA) displays many interesting pharmacological activities thus, considering its scarce solubility in water, its encapsulation into liposome formulations for its delivery is an important goal. Different cationic liposome formulations containing a phospholipid, cholesterol and one of two diasteromeric cationic surfactants resulted able to maintain a stable transmembrane difference in ammonium sulfate concentration and/or pH gradient and to accumulate VOA in their internal aqueous bulk. The fluidity of the lipid bilayer affects both the ability to maintain a stable imbalance of protons and/or ammonium ions across the membrane and the entrapment efficiency. It was shown that VOA loaded into liposomes is more efficient than the free alkaloid to revert resistance of osteosarcoma cells resistant to doxorubicin to an extent depending on their composition.
植物生物碱沃卡明（VOA）具有许多有趣的药理活性，因此，考虑到其在水中的溶解度较低，将其包封到脂质体制剂中进行递送是一个重要的目标。不同的阳离子脂质体制剂含有磷脂、胆固醇和两种非对映体阳离子表面活性剂之一，能够在硫酸铵浓度和/或 pH 梯度的跨膜差保持稳定，并在其内部水相中积累 VOA。脂质双层的流动性既影响维持质子和/或铵离子跨膜稳定失衡的能力，也影响包封效率。结果表明，包封在脂质体中的 VOA 比游离生物碱更有效地逆转对阿霉素耐药的骨肉瘤细胞的耐药性，其程度取决于其组成。
