Cavalli R, Bisazza A, Bussano R, Trotta M, Civra A, Lembo D, Ranucci E, Ferruti P
Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, Via P. Giuria 9, 10125 Torino, Italy.
J Drug Deliv. 2011;2011:587604. doi: 10.1155/2011/587604. Epub 2011 Jun 7.
A new poly(amidoamine)-cholesterol (PAA-cholesterol) conjugate was synthesized, characterized and used to produce nanoparticles by the electrospraying technique. The electrospraying is a method of liquid atomization that consists in the dispersion of a solution into small charged droplets by an electric field. Tuning the electrospraying process parameters spherical PAA-chol nanoparticles formed. The PAA-cholesterol nanoparticles showed sizes lower than 500 nm and spherical shape. The drug incorporation capacity was investigated using tamoxifen, a lipophilic anticancer drug, as model drug. The incorporation of the tamoxifen did not affect the shape and sizes of nanoparticles showing a drug loading of 40%. Tamoxifen-loaded nanoparticles exhibited a higher dose-dependent cytotoxicity than free tamoxifen, while blank nanoparticles did not show any cytotoxic effect at the same concentrations. The electrospray technique might be proposed to produce tamoxifen-loaded PAA-chol nanoparticle in powder form without any excipient in a single step.
合成了一种新型聚(酰胺 - 胺)-胆固醇(PAA - 胆固醇)共轭物,对其进行了表征,并通过电喷雾技术用于制备纳米颗粒。电喷雾是一种液体雾化方法,它通过电场将溶液分散成小的带电液滴。通过调整电喷雾工艺参数形成了球形的PAA - 胆固醇纳米颗粒。PAA - 胆固醇纳米颗粒的尺寸小于500纳米且呈球形。使用他莫昔芬(一种亲脂性抗癌药物)作为模型药物研究了药物包载能力。他莫昔芬的包载不影响纳米颗粒的形状和尺寸,药物载量为40%。载有他莫昔芬的纳米颗粒比游离他莫昔芬表现出更高的剂量依赖性细胞毒性,而空白纳米颗粒在相同浓度下未显示任何细胞毒性作用。电喷雾技术可能被用于一步法制备不含任何辅料的粉末形式的载他莫昔芬PAA - 胆固醇纳米颗粒。