Department of Chemistry, Bogazici University, Bebek, Istanbul, Turkey.
Pharm Dev Technol. 2011 Aug;16(4):408-14. doi: 10.3109/10837451003774401. Epub 2010 Apr 30.
Unilamellar liposomes, prepared from synthetic lipid mixture of DMPC and DMPG either by sonication or extrusion, were used to entrap water soluble and water insoluble molecules to investigate the efficacy of encapsulation by different liposome preparation methods. In the case of entrapment of hydrophilic protein cytochrome-C, the solutions were subjected to a series of ultrafiltration steps to eliminate any free protein outside the vesicles. It was observed that the protein could be encapsulated by the vesicles only if cholesterol was present in the bilayer. The release of cytochrome-C was observed spectrophotometrically upon vesicle-breakdown. The amount of protein encapsulated depended on the method of preparation and was found to be 10 times greater in extruded liposomes compared to those produced by sonication. Hydrophobic Vitamin E, on the other hand, could be encapsulated in the liposome bilayer, independently of the presence of cholesterol and the method of preparation. These fundamental results can be used to develop more efficient drug encapsulations and to have better understanding about their release.
单层脂质体，由 DMPC 和 DMPG 的合成脂质混合物通过超声处理或挤压制备而成，用于包裹水溶性和脂溶性分子，以研究不同脂质体制备方法的包裹效果。在包裹亲水性蛋白质细胞色素 C 的情况下，将溶液进行一系列超滤步骤以去除囊泡外的任何游离蛋白质。结果表明，只有在双层膜中存在胆固醇时，蛋白质才能被囊泡包裹。通过囊泡破裂进行分光光度法观察细胞色素 C 的释放。包裹的蛋白质量取决于制备方法，与通过超声处理制备的脂质体相比，挤出的脂质体中包裹的蛋白质量增加了 10 倍。另一方面，疏水性维生素 E 可以独立于胆固醇的存在和制备方法包裹在脂质体双层中。这些基本结果可用于开发更有效的药物包裹，并更好地了解它们的释放。
