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目的考察不同PEG相对分子质量对包载羟基喜树碱的PEG-PHDCA纳米囊泡的理化性质、体外补体活性和巨噬细胞吞噬影响。方法对纳米囊泡的理化性质包括粒径、zeta电位、表面固有水化层厚度、PEG表面密度等进行表征,进一步阐明其理化性质与纳米囊泡的补体消耗和巨噬细胞吞噬之间的关系。结果PEG10 000-PHDCA具有比其他两组更松弛的结构,PEG链表面密度最小;进一步通过固有水化层厚度的测定进行构型模拟表明:囊泡表面PEG发生折叠,柔韧性下降,导致其较差的隐形效果。与PEG2 000-PHDCA囊泡比较,PEG5 000-PHDCA囊泡显示了更佳的zeta电位( -10.03 mV)和水化层厚度(4.20 nm),PEG的表面密度也在较佳范围内(0.49 PEG.nm-2),这些理化性质赋予其最佳的规避补体消耗和巨噬细胞吞噬的作用。结论过长的PEG链对囊泡表面的修饰并不利于其隐形效果,PEG5 000-PHDCA修饰的纳米囊泡具有最佳的规避补体介导和巨噬细胞吞噬作用。
Objective To investigate the physicochemical properties, in vitro complement activity and macrophage phagocytosis of PEG-PHDCA nanocapsules loaded with hydroxycamptothecin with different molecular weights of PEG. Methods The physical and chemical properties of nano-vesicles, including particle size, zeta potential, surface hydration layer thickness and PEG surface density, were characterized to further elucidate the relationship between their physicochemical properties and the complement depletion of nano-vesicles and macrophage phagocytosis . Results PEG10 000-PHDCA had a more relaxed structure than the other two groups, and the surface density of PEG chains was the smallest. Further, the configuration simulation of the hydration layer thickness showed that the PEG on the surface of the vesicles collapsed and the flexibility decreased, Poor invisible effect. PEG5 000-PHDCA vesicles showed better zeta potential (-10.03 mV) and hydration layer thickness (4.20 nm) compared to PEG2 000-PHDCA vesicles, and the surface density of PEG was also better (0.49 PEG .nm-2), these physical and chemical properties to give its best to avoid complement consumption and phagocytosis of macrophages. Conclusion PEGylation of PEG5 000-PHDCA on the surface of vesicles is not conducive to the invisible effect of PEG chains. The PEG5 000-PHDCA-modified vesicles have the best effect of avoiding complement-mediated and macrophage phagocytosis.