A pH dependent delivery of mesalazine from polymer coated and drug-loaded SBA-16 systems

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• 作者：Ivalina Trendafilova^a ; Á ; gnes Szegedi^b ; Krassimira Yoncheva^c ; Pavletta Shestakova^a ; Judith Mihá ; ly^b ; Alenka Ristić^d ; Spiro Konstantinov^c ; Margarita Popova^a ; ^{mpopova@orgchm.bas.bg" class="auth_mail" title="E-mail the corresponding author}
• 关键词：SBA-16NH2 ; Surface modification ; Eudragit coating ; Mesalazine ; Drug&ndash ; carrier interaction
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2016
• 出版时间：1 January 2016
• 年：2016
• 卷：81
• 期：Complete
• 页码：75-81
• 全文大小：967 K

文摘

SBA-16 silica was synthesized and modified by post-synthesis method with amino groups. Wet milling in acidic media was applied for loading of poorly soluble drug mesalazine (5-aminosalicylic acid — 5-ASA) in different drug/carrier ratios (1:1; 0.75:1; 0.5:1; 0.25:1). The parent and drug loaded mesoporous silicas were characterized by XRD, TEM, N₂ physisorption, thermal analysis, FT-IR and solid state NMR spectroscopy. The drug loaded mesoporous systems were single-coated with Eudragit S or double-coated with Eudragit S and Eudragit RL. The polymer coating significantly modified the rate of mesalazine release from SBA-16NH₂ materials. Applying the double coating method makes possible the sustained delivery of the drug in the intestinal area avoiding the burst release in the gastric fluid. The functionalized, polymer coated mesoporous system could be considered an appropriate oral delivery system for mesalazine. In addition, reduction of mesalazine cytotoxicity on epithelial cells could be achieved by its loading into mesoporous silica particles.