Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing City Key Laboratory of Drug Delivery Technology and Novel Formulations, Beijing 100050, People's Republic of China.
Int J Pharm. 2012 Oct 15;436(1-2):291-8. doi: 10.1016/j.ijpharm.2012.07.003. Epub 2012 Jul 11.
Drug-loading transfersomes were prepared with itraconazole, a lipophilic drug, as a model drug to investigate the key factor affecting transfersomes quality and to evaluate their qualities. Drug-loading transfersomes were prepared using film dispersion method. The quality of transfersomes was evaluated by HPLC, transmission electron microscope, particle size analyzer and in vitro release. Itraconazole transfersomes was transparent solution in ivory white color with a mean entrapment efficiency of about 80%. The shape of hollow vesicles was spheroidal with the diameter of approximately 100 nm, and the zeta potential of 45 mV, which had a good transdermal effect. It can be concluded via single-factor investigation that the quality of transfersomes is significantly affected by solvent, salt ion concentration and homogenization pressure and so on. The preparation method obtained through screening and optimizing formulation and technology is feasible and the quality can be controlled.
载药传递体以亲脂性药物伊曲康唑为模型药物进行制备，以研究影响传递体质量的关键因素并评价其质量。采用薄膜分散法制备载药传递体。采用 HPLC、透射电镜、粒径分析仪和体外释放度对传递体的质量进行评价。伊曲康唑传递体呈乳白色透明溶液，平均包封率约为 80%。空心囊泡的形状为球形，直径约为 100nm，Zeta 电位为 45mV，具有良好的经皮渗透效果。通过单因素考察可以得出，传递体的质量显著受到溶剂、盐离子浓度和匀质压力等因素的影响。通过筛选和优化处方和工艺得到的制备方法是可行的，质量可控。
