聚乙二醇化聚酰胺-胺树枝状材料的制备及其细胞毒性研究

Preparation and in Vitro Cytotoxicity of PEGylation Polyamidoamine Dendrimer

目的聚酰胺-胺树枝状材料(PAMAM)作为药物载体具有较好的结构优势,通过聚乙二醇(PEG)修饰后,制备低毒的复合物。方法调整PAMAM与PEG比例合成PAMAM-PEG复合物,并用^(1-)H-NMR,粒径-Zeta电位仪对其进行表征;采用MTT法检测细胞的存活率和溶血试验考察细胞溶血毒性。结果本实验获得了三种PAMAM-PEG复合物;与PAMAM处理组比较,复合物处理的KB细胞存活率显著提高,细胞的溶血率显著降低,并呈剂量—效应依赖性。结论 PAMAM具有一定的细胞毒性,随聚乙二醇化程度的增加,其对KB细胞体外抑制活性降低,溶血毒性降低。

Objective To prepare the harmless conjugates of polyamidoamine dendrimer （PAMAM）-polyethylene glycol （PEG） for PAMAM with better structure as drug carriers. Methods The products were obtained by adjusting the quality ratio of PAMAM and PEG. The characterizations of products were calculated by 1 H-NMR and Zeta potential and diameter. The cell viability was calculated through the MTT assay and the hemolytic toxicity was detected by the hemolysis test. Results Three products were obtained. Compared with PAMAM group, the KB cell viability increased and the ratio of cell hemolysis decreased significantly in groups of PAMAM-PEG conjugate with good dose-effect relationship. Conclu- sion The PAMAM posses a little cytotoxicity. With the increasing of PEG chains attaching on the PAMAM dendrimer, cytotoxicity and hemolytic toxicity of conjugates become relatively lower.