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New method for preparation of delivery systems of poorly soluble drugs on the basis of functionalized mesoporous MCM-41 nanoparticlesud

机译:基于功能化介孔MCM-41纳米粒子制备难溶药物递送系统的新方法 ud

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摘要

MCM-41 silica with spherical morphology and small particle sizes (100 nm) was synthesized and modified by post-synthesis method with amino and/or carboxylic groups. Solid state reaction was applied for the first time for loading of poorly soluble drug mesalazine (5-aminosalicylic acid – 5-ASA). Thenon-loaded and drug loaded mesoporous silicas were characterized by XRD, TEM, N2 physisorption, elemental analysis, thermal analysis, FT-IR and solid state NMR spectroscopy. Quantum-chemical calculations were used to predict the interactions between the drug molecule and the functional groups of the carrier. The nanoparticles were post-coated with sodium alginate and the coating modified the rate of mesalazine release from MCM-41NH2 and MCM-41NH2COOH particles. Cytotoxic evaluation on colon adenocarcinoma cell line revealed that the alginate coating reduced cytotoxicity of mesalazine loaded in the post-coated particles compared to the pure mesalazine. The functionalized, polymer coated mesoporous systems are suitable oral drug delivery systems providing an opportunity to modify drug release.
机译:合成了球形和小粒径(100 nm)的MCM-41二氧化硅,并通过后合成方法用氨基和/或羧基进行了改性。第一次进行固态反应以加载难溶性药物美沙拉嗪(5-氨基水杨酸– 5-ASA)。通过XRD,TEM,N2物理吸附,元素分析,热分析,FT-IR和固态NMR光谱对非负载和药物负载的介孔二氧化硅进行了表征。量子化学计算用于预测药物分子与载体官能团之间的相互作用。用海藻酸钠对纳米颗粒进行后涂覆,该涂层改变了美沙拉嗪从MCM-41NH2和MCM-41NH2COOH颗粒中释放的速率。对结肠腺癌细胞系的细胞毒性评估显示,与纯净的美沙拉嗪相比,藻酸盐涂层降低了后涂层颗粒中装载的美沙拉嗪的细胞毒性。功能化的,聚合物包被的中孔系统是合适的口服药物递送系统,提供了改变药物释放的机会。

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