靶向肿瘤新生血管纳米粒的构建和质量控制

目的：制备F56多肽修饰的长春新碱纳米粒（F56-VCR-NP），并建立其质量控制方法。方法：乳化－溶剂挥发法优化制备F56．VCR-NP：HPLC法测定其载药量、包封率，透射电镜下观察其形态，激光粒度分析仪测定其粒径和Zeta电位，CBQCA试剂盒测定纳米粒表面多肽密度，XPS进行表面元素分析。结果：优化制备的F56－VCR-NP粒径约为153nm，Zeta电位为－20．8mv，包封率为21．4％，载药量为1．9％，多肽连接效率为26．3％。结论：以聚乙二醇－聚乳酸（PEG-PLA）为原料，长春新碱为模型药物，成功制备出纳米粒子，并建立起有效的质量控制方法，对该实验样品进行了表征。结果表明此类纳米粒子尺寸均匀，表面多价连接F56多肽，载药量和包封率稳定可控，工艺成熟。

Preparation and Quality Control of Nanoparticles Targeting to Tumor Neovasculature

Objective： To prepare vincristine-loaded nanoparticles decorated with F56 peptides （F56-VCR-NP） and establish the method for quality control of the nanopartieles. Methods： Vincristine-loaded nanoparticles decorated with F56 peptides （F56-VCR-NP） was prepared by emulsification-evaporation method. The encapsulation efficiency and drug loading were determined by HPLC. The phormology was measured by transmission electron microscopy （TEM）. The particle sizes, polydispersity, zeta potential were measured by dynamic light scattering assay. F56 density on the nanoparticle surface was determined by CBQCA Protein Quantitation Kit. Relative content ratio of each element on the surface of the samples was determined by X-ray photoelectron spectroscopy （XPS）, Results： The average particle size of F56-VCR-NP obtained was 153 nm. The zeta potential was -20.8 mV; Encapsulating efficiency was 21.4 %; Drug loading was 1.9 %; F56 conjuation efficiency was 26.3 %. Conclusion： With poly（ethylene glycol）-poly（lactic acid）（PEG-PLA） as the material, the vincristine-loaded nanoparticles were successfully prepared. The nanoparticles were characterized and the results showed that particle size, F56 peptide surface connecting efficiency, drug loading and encapsulation efficiency were stable and easy to control, so the process is mature.