Pharmaceutical Sciences Department, University of Salamanca, Licenciado Méndez Nieto s/n, 37007 Salamanca, Spain; Institute of Biomedical Research of University of Salamanca (IBSAL), Paseo de San Vicente 58-182, 37007 Salamanca, Spain.
Pharmaceutical Sciences Department, University of Salamanca, Licenciado Méndez Nieto s/n, 37007 Salamanca, Spain.
Eur J Pharm Sci. 2017 Aug 30;106:159-165. doi: 10.1016/j.ejps.2017.05.066. Epub 2017 Jun 1.
Itraconazole-loaded micro/nanoparticles containing albumin and liposomes were prepared by a technological process that avoids the use of organic solvents and crosslinker agents. The particles were characterized, lyophilized and formulated as tablets. Dynamic light scattering was used to determine the hydrodynamic diameter and zeta potential of the particles; optical and scanning-electron microscopy was used to evaluate their morphology. Spherical shaped particles of different sizes and zeta potential were obtained. An exponential relationship between the zeta potential and the albumin/cationic lipid molar ratio was established. Drug entrapment efficiency values were in the range of 51-68%, with no statistical differences among albumin feeding concentrations. Mannitol was used as lyophilization additive and the freeze-dried cake was directly compressed into tablets, suitable for vaginal administration. The results from the in vitro drug delivery assay show the influence of albumin on the itraconazole delivery profile; a rapid release was observed for particles with higher albumin amount compared to those with lower protein content. According to the results of this study, albumin particles entrapping liposomes prove to be a green pharmaceutical vehicle with a high potential for delivery of hydrophobic and highly albumin-bound drugs.
载酮康唑的白蛋白和脂质体纳米/微球是通过避免使用有机溶剂和交联剂的工艺制备的。对粒子进行了特征描述、冻干和制成片剂。动态光散射用于测定粒子的水动力直径和zeta 电位；光学和扫描电子显微镜用于评估其形态。得到了具有不同大小和 zeta 电位的球形粒子。建立了 zeta 电位与白蛋白/阳离子脂质摩尔比之间的指数关系。药物包封效率值在 51-68%之间，白蛋白喂养浓度之间无统计学差异。甘露醇用作冻干添加剂，将冷冻干燥的蛋糕直接压制成片剂，适用于阴道给药。体外药物释放试验的结果表明白蛋白对酮康唑的递送特性有影响；与蛋白质含量较低的粒子相比，白蛋白含量较高的粒子表现出快速释放。根据这项研究的结果，载脂蛋白体的脂质体证明是一种绿色的药物载体，具有传递疏水性和高度结合白蛋白的药物的巨大潜力。
