Ringhieri Paola, Pannunzio Alessandra, Boccarelli Angelina, Morelli Giancarlo, Coluccia Mauro, Tesauro Diego
a Department of Pharmacy and CIRPeB , University of Naples "Federico II" , Naples , Italy .
b Istituto Di Biostrutture E Bioimmagini - CNR , Naples , Italy , and.
J Liposome Res. 2016 Dec;26(4):307-12. doi: 10.3109/08982104.2015.1127257. Epub 2016 Feb 5.
Gynecological tumors are major therapeutic areas of platinum-based anticancer drugs. Here, we report the characterization and in vitro biological assays of cisplatin-containing Egg L-α-phosphatidylcholine liposomes with different amounts of cholesterol. Dynamic light scattering estimated sizes of all obtained liposomes in the 100 nm range that are suitable for in vivo use. On the basis of these data and of the drug loading values, the best formulation has been selected. Stability and drug release properties of platinum-containing liposomes have been verified in serum. The growth inhibitory effects of both liposomal and free drug in a panel of ovarian and breast human cancer cell lines, characterized by a different drug sensitivity, give comparable or better results with respect to free cisplatin drug.
妇科肿瘤是铂类抗癌药物的主要治疗领域。在此,我们报告了含顺铂的、具有不同胆固醇含量的L-α-磷脂酰胆碱脂质体的特性及体外生物学测定。动态光散射估计所有获得的脂质体大小在100 nm范围内,适合体内使用。基于这些数据和载药值,选择了最佳配方。含铂脂质体的稳定性和药物释放特性已在血清中得到验证。在一组具有不同药物敏感性的卵巢和乳腺人类癌细胞系中,脂质体药物和游离药物的生长抑制作用相对于游离顺铂药物给出了相当或更好的结果。