Ravi S, Peh K K, Darwis Yusrida, Murthy B Krishna, Singh T Raghu Raj, Mallikarjun C
School of Pharmaceutical Sciences, Universiti Sains Malaysia, Gelugor, Pulau Penang, 11800, Malaysia.
Indian J Pharm Sci. 2008 May-Jun;70(3):303-9. doi: 10.4103/0250-474X.42978.
The aim of the present work was to investigate the preparation of microspheres as potential drug carriers for proteins, intended for controlled release formulation. The hydrophilic bovine serum albumin was chosen as a model protein to be encapsulated within poly(D,L-lactide-co-glycolide) (50:50) microspheres using a w/o/w double emulsion solvent evaporation method. Different parameters influencing the particle size, entrapment efficiency and in vitro release profiles were investigated. The microspheres prepared with different molecular weight and hydrophilicity of poly(D,L-lactide-co-glycolide) polymers were non porous, smooth surfaced and spherical in structure under scanning electron microscope with a mean particle size ranging from 3.98 to 8.74 mum. The protein loading efficiency varied from 40 to 71% of the theoretical amount incorporated. The in vitro release profile of bovine serum albumin from microspheres presented two phases, initial burst release phase due to the protein adsorbed on the microsphere surface, followed by slower and continuous release phase corresponding to the protein entrapped in polymer matrix. The release rate was fairly constant after an initial burst release. Consequently, these microspheres can be proposed as new controlled release protein delivery system.
本研究的目的是研究微球作为蛋白质潜在药物载体的制备方法，用于控释制剂。选择亲水性牛血清白蛋白作为模型蛋白，采用水包油包水双乳液溶剂蒸发法将其包裹在聚（D，L-丙交酯-共-乙交酯）（50:50）微球中。研究了影响粒径、包封率和体外释放曲线的不同参数。在扫描电子显微镜下，用不同分子量和亲水性的聚（D，L-丙交酯-共-乙交酯）聚合物制备的微球无孔、表面光滑且呈球形结构，平均粒径范围为3.98至8.74μm。蛋白质负载效率为理论掺入量的40%至71%。牛血清白蛋白从微球中的体外释放曲线呈现两个阶段，由于蛋白质吸附在微球表面而导致的初始突释阶段，随后是对应于包裹在聚合物基质中的蛋白质的较慢且持续的释放阶段。在初始突释后，释放速率相当恒定。因此，这些微球可被提议作为新型控释蛋白质递送系统。
