NGR修饰唑来膦酸长循环脂质体制备及其表征研究

目的:制备具有肿瘤血管靶向的NGR修饰唑来膦酸长循环脂质体,并对其进行表征研究。方法：采用薄膜分散法制备NGR修饰唑来膦酸长循环脂质体,,并对其进行表征研究,并测定包封率。结果：制备得到的NGR-PEG-ZOL-LPs平均粒径为(271.43±9.23)nm,Zeta电位为-(36.20±0.20)mv,多分散系数(PDI)为(0.15±0.03),理化性质相对稳定；NGR-PEG-ZOL-LPs包封率为8.41%；电镜下显示NGR-PEG-ZOL-LPs呈类圆形,大小分布均匀,无明显聚集。结论：采用薄膜分散法制备的NGR修饰唑来膦酸长循环脂质体具有较高的稳定性,从而为体内药效学研究奠定基础。

Study of preparation and in vitro characterization of NGR-PEG-ZOL-LPs

Aim:Preparation of NGR-PEG-ZOL-LPs, and evaluation its characteristics in vitro.Method:Film dispersion method was used to prepare the NGR-PEG-ZOL-LPs, then,their characterization studies including the encapsulation efficiency were performed to determine. Results: The average particle size of the prepared NGR-PEG-ZOL-LPs was (271.43±9.23) nm, the Zeta potential was-(36.20±0.20) mv, and the polydispersity coefficient (PDI) was (0.15±0.03). The physical and chemical properties were relatively stable;the encapsulation rate of NGR-PEG-ZOL-LPs was 8.41%;the electron microscopy showed that NGR-PEG-ZOL-LPs had a round shape, uniform size distribution, and no obvious aggregation. CONCLUSION: NGR-modified zoledronic acid long-circulating liposomes prepared by the thin-film dispersion method have high stability, which lays the foundation for pharmacodynamic research in vivo.