Polyamidoamine (PAMAM) dendrimer is emerging as an effective nanocarrier for delivering anticancer drugs. Still, unmodified PAMAM dendrimer is hardly used in vivo because of unsatisfied drug release, high tendency of interfering with cellular membranes, and rapid clearance by reticuloendothelial system. In this study, low generation polyamidoamine (PAMAM) dendrimer G3.0 is developed and surface modified with methoxypolyethylene glycol (PAMAM G3.0-mPEG) to overcome its limitations. Specifically, PAMAM G3.0 conjugated with mPEG at different ratios are investigated to effectively eliminate its charge-associated toxicity, in which PAMAM G3.0-mPEG-8 is chosen for oxaliplatin (OX) loading. Results reveal that OX-loaded PAMAM G3.0-mPEG-8 has desirable size, good entrapment efficiency, and sustained release with minimum drug leakage. In addition, Resazurin assay indicates that the toxicity of loaded OX is reduced as compared to free drug but still maintain substantially anticancer activity on HeLa cells, suggesting the potential application of PAMAM G3.0-mPEG-8 for OX delivery in cancer therapy.

聚酰胺胺（PAMAM）树状大分子正成为一种有效的纳米载体，可用于递送抗癌药物。尽管如此，未经修饰的PAMAM树状聚合物仍很少用于体内由于药物释放不满意，干扰细胞膜的趋势高以及网状内皮系统的快速清除。在这项研究中，开发了低代聚酰胺型（PAMAM）树枝状聚合物G3.0，并用甲氧基聚乙二醇（PAMAM G3.0-mPEG）对其进行了表面改性，以克服其局限性。具体而言，研究了以不同比例与mPEG缀合的PAMAM G3.0，以有效消除其电荷相关毒性，其中选择PAMAM G3.0-mPEG-8作为奥沙利铂（OX）负载。结果表明，载有OX的PAMAM G3.0-mPEG-8具有理想的尺寸，良好的包封效率和持续释放性，且药物泄漏最少。此外，刃天青测定结果表明，与游离药物相比，负载的OX的毒性有所降低，但仍对HeLa细胞保持基本的抗癌活性，