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通过探讨制备过程中磁性颗粒不同的加入顺序对其在脂质体结构中分布的影响,制备了具有较高包封率的磁性顺铂(cisplatin,CDDP)脂质体。本研究采用改良水热合成方法一步制备了表面修饰的Fe3O4磁性纳米颗粒并采用薄膜超声法制备了CDDP磁性脂质体,用石墨炉原子吸收分光光度法测定CDDP含量。在制备过程中考察两种不同制备程序对脂质体微观结构的影响,即程序I:将磁性颗粒先与磷脂结合再成膜制备脂质体;程序II:将磁性颗粒分散于药物溶液中水合制备脂质体。用透射电镜(transmission electron microscope,TEM)观察磁性脂质体形态。按正交实验设计筛选最优处方制备磁性脂质体,以程序I制备的脂质体磁性颗粒分布于磷脂双层中,包封率为34.90%,而以程序II制备的脂质体磁性颗粒分布于脂质体中间水相,包封率为28.34%。两者包封率均高于普通脂质体。3种不同脂质体体外释药均符合一级释药规律。程序I制备的磁性脂质体由于磁性颗粒分布于磷脂双层中,改变了磷脂所形成的双层骨架,使其释药t1/2为9 h,比另外两者较短。结果表明,采用程序I实现了纳米磁性颗粒在脂质体中的组装,用此方法制备的磁性脂质体在药物包封率和磁性颗粒的含量上都优于程序II,并且能保证一定的缓释效应。
By discussing the influence of the order of addition of magnetic particles on the distribution in the liposomes during the preparation process, magnetic cisplatin (CDDP) liposomes with high entrapment efficiency were prepared. In this study, surface-modified Fe3O4 magnetic nanoparticles were prepared in one step by the improved hydrothermal synthesis method and CDDP magnetic liposomes were prepared by thin-film ultrasonic method. The content of CDDP was determined by graphite furnace atomic absorption spectrophotometry. In the preparation process, the effects of two different preparation procedures on the microstructure of the liposomes were investigated, ie program I: the magnetic particles were first combined with the phospholipid to form the liposomes again; Procedure II: the magnetic particles were dispersed in the drug solution hydrated Liposomes are prepared. The morphology of magnetic liposomes was observed by transmission electron microscope (TEM). The orthogonal design was used to screen the optimal formulation to prepare magnetic liposomes. The liposome magnetic particles prepared by procedure I were distributed in the phospholipid bilayer and the entrapment efficiency was 34.90%. The liposome magnetic particles Distributed in the aqueous phase of liposomes, encapsulation efficiency was 28.34%. Both encapsulation efficiency are higher than ordinary liposomes. The in vitro release of 3 kinds of liposomes all accord with the first grade drug release rule. The magnetic liposomes prepared in the procedure I, due to the distribution of magnetic particles in the phospholipid bilayer, changed the bilayer skeleton formed by the phospholipid to a release time of t1 / 2 of 9 h, which was shorter than the other two. The results showed that the procedure I was used to assemble the nano-magnetic particles in the liposomes. The magnetic liposome prepared by this method was superior to the program II in terms of drug encapsulation efficiency and magnetic particle content, Slow release effect.