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首页> 外文期刊>RSC Advances >Chitosan-folate coated mesoporous silica nanoparticles as a smart and pH-sensitive system for curcumin delivery
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Chitosan-folate coated mesoporous silica nanoparticles as a smart and pH-sensitive system for curcumin delivery

机译：壳聚糖叶酸涂层介孔二氧化硅纳米粒子作为姜黄素递送的智能和pH敏感系统

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In this work, normal and large pore size mesoporous silica nanoparticles (NMSNs and LMSNs) were prepared by co-condensation method and coated with (3-aminopropyl)triethoxysilane (APTES) to prepare amine functionalized MSNs (MSN-NH _(2) ). They were then conjugated with succinic anhydride (SA) to obtain carboxylic acid functionalized MSNs (MSN-COOH). Curcumin (CUR) as a hydrophobic drug was loaded into the synthesized MSNs with two different pore sizes to compare the loading capacity and efficiency. The results showed that LMSNs had 2-fold larger loading efficiency and capacity for CUR than NMSNs. Chitosan (CS), as a pH-sensitive polymer, was also conjugated to folic acid (FA) as an active targeting agent and then coated on the surface of carboxylic acid enriched MSNs via electrostatic interaction. The MSNs were fully characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), zeta potential analysis, dynamic light scattering (DLS), nitrogen adsorption/desorption analysis, thermo gravimetric analysis (TGA), XRD analysis, NMR and UV-visible spectroscopies. The mechanism of CUR release from CS-FA coated LMSNs was pH-sensitive and in vitro release modeling revealed that CUR is released via Korsmeyer–Peppas mechanism. No significant toxicity was observed for CUR free MSNs, while the CUR loaded MSNs inhibited proliferation of HeLa and NIH-3T3 cell lines, showing more cytotoxic effect on cancerous HeLa cells. Moreover, the selective cellular uptake of CUR loaded LMSNs-COOH@CS-FA by folate receptor-positive HeLa cells was assessed and confirmed. Hemocompatibility and protein corona of the target carrier were also studied to show negligible hemolytic activity and suitable protein–target LMSNs interactions.
机译：在该工作中，通过共聚方法制备正常和大的孔径介孔二氧化硅纳米粒子（NMSN和LMSNS）并用（3-氨基丙基）三乙氧基硅烷（Aptes）涂覆以制备胺官能化MSN（MSN-NH _（2）） 。然后将它们与琥珀酸酐（SA）缀合，得到羧酸官能化MSNS（MSN-COOH）。用两种不同的孔径将姜黄素（Cur）作为疏水药装入合成的MSN中，以比较负载能力和效率。结果表明，LMSNS的加载效率是2倍的效率和CURS的能力。作为pH-敏感聚合物，壳聚糖（Cs）也作为活性靶向剂与叶酸（Fa）缀合，然后通过静电相互作用涂覆在羧酸富集的MSN的表面上。 MSNS通过扫描电子显微镜（SEM），透射电子显微镜（TEM），Zeta电位分析，动态光散射（DLS），氮吸附/解吸分析，热重量分析（TGA），XRD分析，NMR和UV - 可见光谱。 CS-Fa涂覆的LMSNS的Cur释放机理是pH敏感的，体外释放建模显示，Cur通过Korsmeyer-Peppas机制释放。对于RU的自由MSN没有观察到显着的毒性，而Cur Loaded MSNS抑制了HeLa和NiH-3T3细胞系的增殖，对癌性Hela细胞显示出更多的细胞毒性作用。此外，评估并确认通过叶酸受体阳性HeLa细胞进行Cur负载LMSNS-CoOH-CS-Fa的选择性细胞摄取。还研究了靶载体的血液相色和蛋白质电晕，以显示可忽略不计的溶血活性和合适的蛋白质靶标相互作用。

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