Beagan Abeer, Lahmadi Shatha, Alghamdi Ahlam, Halwani Majed, Almeataq Mohammed, Alhazaa Abdulaziz, Alotaibi Khalid, Alswieleh Abdullah
Department of Chemistry, College of Science, King Saud University, Riyadh 11451, Saudi Arabia.
Nanomedicine Department, King Abdullah International Medical Research Center, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia.
Polymers (Basel). 2020 Nov 20;12(11):2749. doi: 10.3390/polym12112749.
This work presents the synthesis of pH-responsive poly(2-(diethylamino) ethyl methacrylate) (PDEAEMA) brushes anchored on hollow mesoporous silica nanoparticles (HMSN-PDEAEMA) via a surface-initiated ARGET ATRP technique. The average size of HMSNs was ca. 340 nm, with a 90 nm mesoporous silica shell. The dry thickness of grafted PDEAEMA brushes was estimated to be ca 30 nm, as estimated by SEM and TEM. The halogen group on the surface of PDEAMA brushes was successfully derivatized with glucosamine, as confirmed by XPS. The effect of pH on the size of the hybrid nanoparticles was investigated by DLS. The size of fabricated nanoparticle decreased from ca. 950 nm in acidic media to ca. 500 nm in basic media due to the deprotonation of tertiary amine in the PDEAEMA. The PDEAEMA modified HMSNs nanocarrier was efficiently loaded with doxorubicin (DOX) with a loading capacity of ca. 64%. DOX was released in a relatively controlled pH-triggered manner from hybrid nanoparticles. The cytotoxicity studies demonstrated that DOX@HMSN-PDEAEMA-Glucosamine showed a strong ability to kill breast cancer cells (MCF-7 and MCF-7/ADR) at low drug concentrations, in comparison to free DOX.
本研究通过表面引发的ARGET ATRP技术，合成了锚定在中空介孔二氧化硅纳米粒子（HMSN-PDEAEMA）上的pH响应性聚甲基丙烯酸2-（二乙氨基）乙酯（PDEAEMA）刷。HMSN的平均尺寸约为340nm，具有90nm的介孔二氧化硅壳。通过扫描电子显微镜（SEM）和透射电子显微镜（TEM）估计，接枝的PDEAEMA刷的干厚度约为30nm。X射线光电子能谱（XPS）证实，PDEAMA刷表面的卤素基团已成功用氨基葡萄糖衍生化。通过动态光散射（DLS）研究了pH对杂化纳米粒子尺寸的影响。由于PDEAEMA中叔胺的去质子化，制备的纳米粒子尺寸从酸性介质中的约950nm减小到碱性介质中的约500nm。PDEAEMA修饰的HMSNs纳米载体有效地负载了阿霉素（DOX），负载量约为64%。DOX以相对可控的pH触发方式从杂化纳米粒子中释放。细胞毒性研究表明，与游离DOX相比，DOX@HMSN-PDEAEMA-氨基葡萄糖在低药物浓度下具有很强的杀死乳腺癌细胞（MCF-7和MCF-7/ADR）的能力。
