微孔膜乳化法制备丝裂霉素碘油复乳的研究

 目的 采用新型微孔膜乳化法制备粒径均匀、包埋率高、包埋稳定的抗癌剂碘油复乳药物载体。方法 以丝裂霉素为模型药物，将丝裂霉素的水溶液与碘油混合，用均相乳化器制成W/0型初乳后，用适当压力将W/0型初乳通过微孔膜压入外水相，制备出了W/0/W型药物载体，对该药物载体的粒径分布、包埋率、体外控释等进行了研究。结果 以聚氧乙烯氢化蓖麻油（HC040)作为碘油相乳化剂，碘油与丝裂霉素水溶液体积比为2:1，制备W/0型初乳时的条件为3 minJGOOrmirT1时，所得到的丝裂霉素碘油复乳载体粒径均匀，粒径分布系数值达到13.2%以下，药物包埋率达90%左右，在4尤下储存稳定性可达30 d以上，在37℃下能以适当的速度释放出药物。结论 采用微孔膜乳化法制备的碘油药物载体粒径均匀、包埋率高、储存稳定，有望成为临床靶向给药的一种新剂型。

Preparation of lipiodol double emulsion as drug carrier by a novel emulsification technique

OBJECTIVE To prepare the stable lipiodol double emulsion with uniform size and high encapsulation efficiency as drug carrier by a novel membrane emulsification technique. METHODS Mitomycin C was used as a model drug. After the W/0 emulsion composed of mitomycin C aqueous phase and Lipiodol was prepared by a homogenizer, the W/0 emulsion was pressed through the pores of a porous membrane into the external aqueous phase to form the W/O/W double emulsion. The effects of preparation conditions on the size distribution, encapsulation efficiency and release behavior in vitro were investigated. RESULTS Polyoxyethylene hydrogenerated caster oil (HC040) was used as the emulsifier in oil phase, the volume ratio between Lipiodol and Mitomycin C solution was 2:1，and the W/0 primary emulsion was prepared by emulsification for 3min at 8 600 r.min-1 . The stable double emulsion with uniform size and high encapsulation efficiency was obtained. The size distribution coefficient was lower than 13.2% . The encapsulation efficiency was 90% . The shelf life at 0℃ attained to 30 days, and the drug was released steadily at 371. CONCLUSION The W/O/W Lipiodol double emulsion with uniform size, high encapsulation efficiency and long shelf life can be prepared by the membrane emulsification technique. The double emulsion can be used as a new carrier for controlled release drug system.