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目的:研制顺铂隐形泡囊并比较其连接蛋白质前后的理化性质和体外生物学性质。方法:NHS活化酯法合成PluronicF68-BSA偶联物,以改良注入法制备泡囊,显微镜下目测统计粒径分布,透析分离、紫外法考察包封率和稳定性,并研究其对小鼠巨噬细胞的毒性和吞噬效果。结果:2种泡囊平均粒径分别为3.48和4.49μm,包封率为51.54%和44.02%,一周后渗漏率为20.97%和24.09%,其细胞毒性均与原料药一致。表面连接BSA后,被吞噬率增大。结论:本法工艺简单,条件温和,为进一步连接单抗、制备免疫隐形泡囊提供依据。
OBJECTIVE: To develop cisplatin invisible vesicles and to compare the physicochemical properties and in vitro biological properties of the connective proteins. Methods: Pluronic F68-BSA conjugate was synthesized by NHS activated ester method. The vesicles were prepared by modified injection method. The particle size distribution was observed visually under the microscope. The encapsulation efficiency and stability were investigated by ultraviolet spectrophotometry. Toxicity and phagocytosis of macrophages. Results: The average particle sizes of the two vesicles were 3.48 and 4.49 μm, respectively, and the entrapment efficiencies were 51.54% and 44.02%. After one week, the leakage rates were 20.97% and 24.09%, respectively. The cytotoxicity of the two vesicles was consistent with the drug substance. BSA after the surface was linked to phagocytosis rate increased. Conclusion: The method is simple, mild conditions, to provide further evidence for the preparation of immunostaining vesicles.