Xu Shanshan, Wu Juan, Jiang Wei, Tian Renbing
J Nanosci Nanotechnol. 2016 Feb;16(2):1363-9. doi: 10.1166/jnn.2016.10697.
We prepared a magnetic poly(amido amine) (G2.5)-hydrazine hydrate nanocarrier, denoted by MNPs@PAMAM-H. PAMAM dendrimer was conjugated onto the surface of magnetic nanoparticles (MNPs) to increase the biocompatibility of the nanocarrier and provided a large number of reactive sites for coupling of drug molecules. DOX was covalently attached to the nanocarrier via a pH-sensitive linker, hydrazone bond, which hydrolyzes in the acidic lysosomal environment to allow pH-sensitive release of DOX. DOX was successfully loaded into the nanocarrier with a high drug loading (27.53%) and entrapment efficiency (86.44%). Nearly 88% DOX was released within 60 h at pH 5.0, compared with only 30% at pH 7.4. The in vitro MTT assay in HeLa cells demonstrated that MNPs@PAMAM-DOX exhibited high anti-tumor activity, while the MNPs@PAMAM-H were practically non-toxic. These results revealed that MNPs@ PAMAM-H were biocompatible. The Synthesized nanocarrier had the potential to be used as MR probe and guide DOX to enter target sites in cancer therapy by an outer magnet.
我们制备了一种磁性聚（酰胺胺）（G2.5）-水合肼纳米载体，记为MNPs@PAMAM-H。将聚酰胺胺树枝状大分子共轭到磁性纳米颗粒（MNPs）表面，以提高纳米载体的生物相容性，并为药物分子偶联提供大量反应位点。阿霉素（DOX）通过pH敏感连接子腙键共价连接到纳米载体上，该键在酸性溶酶体环境中水解，从而实现DOX的pH敏感释放。DOX以高载药量（27.53%）和包封率（86.44%）成功载入纳米载体。在pH 5.0时，近88%的DOX在60小时内释放，而在pH 7.4时仅释放30%。在HeLa细胞中进行的体外MTT试验表明，MNPs@PAMAM-DOX表现出高抗肿瘤活性，而MNPs@PAMAM-H几乎无毒。这些结果表明MNPs@PAMAM-H具有生物相容性。合成的纳米载体有潜力用作磁共振探针，并通过外部磁场引导DOX进入癌症治疗的靶位点。
