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目的:研究不同相对分子质量聚乙二醇(PEG)修饰不同代数树枝状大分子聚酰胺-胺(PAM-AM)得到的产物,测定其对人体角膜上皮细胞(HCECs)的毒性。方法:采用硝基苯氯甲酸酯(p-NPC)将单甲氧基聚乙二醇(mPEG,相对分子质量为750,2 000,5 000)活化成PEG碳酸酯,对第4,5代PAMAM大分子进行修饰;目标产物用FT-IR、1H-NMR进行结构表征;采用WST-8法考察PEG修饰对PAMAM的人角膜上皮细胞(HCECs)毒性的影响。结果:PAMAM经较低浓度PEG修饰后,对HCECs的毒性减弱不明显,经较高浓度PEG修饰后,对HCECs减毒明显减弱,不同相对分子质量的PEG修饰对PAMAM的减毒作用无明显差异。结论:经PEG修饰后,可以降低PAMAM对HCECs的毒性,作为新型眼部给药载体具有良好的前景。
OBJECTIVE: To study the effects of different molecular weight polyethylene glycol (PEG) modified polyamidoamine (PAM-AM) on the degeneration of human dendritic cells (HCECs). Methods: Monomethoxy polyethylene glycol (mPEG, relative molecular mass of 750,2000,5000) was activated to PEG carbonate by nitrobenzene chloroformate (p-NPC) The PAMAM macromolecules were modified. The target product was characterized by FT-IR and 1H-NMR. The WST-8 method was used to investigate the effect of PEG modification on the toxicity of human amniotic epithelial cells (HCECs). Results: The PAMAM modified with lower concentration of PEG showed no obvious cytotoxicity on HCECs. After being modified with higher concentration of PEG, the attenuated attenuation of HCECs was significantly attenuated. The attenuated effect of different molecular weight PEG on PAMAM had no significant difference . CONCLUSION: PEG-modified PAMAM can reduce the toxicity of PAMAM to HCECs and has a good prospect as a novel ocular drug delivery carrier.