Shanghai Key Laboratory of Functional Materials Chemistry, School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai 200237, China.
National Facility for Protein Science in Shanghai, Shanghai Advanced Research Institute (Zhang jiang Laboratory), Chinese Academy of Sciences, Shanghai 201210, China.
Colloids Surf B Biointerfaces. 2022 Dec;220:112862. doi: 10.1016/j.colsurfb.2022.112862. Epub 2022 Sep 20.
Iohexol (IOH) is a commonly used second-generation nonionic iodinated contrast agent. However, low gastrointestinal mucosal adherence and high downstream speed limit its application in intestinal Computed tomography (CT) imaging. We hypothesize that oral IOH delivery carriers composed of environmentally responsive materials enable the intestinal targeted delivery and prolong the intestinal residence time of IOH, enhancing the intestinal disease detection efficiency.
An emulsion-filled alginate hydrogel system was developed as the intestinal targeting vehicle for IOH. The formulation optimization was determined by response surface analysis. After a thorough study of the physicochemical properties of this hydrogel matrix, the pH sensitivity and the ability to control release were investigated, followed by a vitro cell experiment evaluating its bioactivity and CT imaging capability.
This alginate hydrogel matrix was sparsely structured and rapidly released IOH at pH 7.4. Meanwhile the swelling degree was 4.4 times higher than that at pH 1.2, indicating a good selective responsiveness to the gastrointestinal simulated environment. It improved the CT visual contrast of A549 cells without affecting cell morphology, suggesting that it would be an effective oral administration for water-soluble nonionic contrast agents and a potential candidate for intestinal disease detection tools.
碘海醇(IOH)是一种常用的第二代非离子型碘造影剂。然而,低胃肠道黏膜黏附性和高下游速度限制了其在肠道计算机断层扫描(CT)成像中的应用。我们假设由环境响应性材料组成的口服 IOH 给药载体能够实现肠道靶向递送并延长 IOH 的肠道驻留时间,从而提高肠道疾病检测效率。
我们开发了一种填充乳剂的海藻酸钠水凝胶系统作为 IOH 的肠道靶向载体。通过响应面分析确定了配方优化。在对这种水凝胶基质的物理化学性质进行了深入研究之后,我们研究了其 pH 敏感性和控制释放能力,然后进行了体外细胞实验以评估其生物活性和 CT 成像能力。
这种海藻酸钠水凝胶基质结构稀疏,在 pH 7.4 时迅速释放 IOH。同时,在 pH 1.2 时的溶胀度是其 4.4 倍,表明其对胃肠道模拟环境具有良好的选择性响应性。它提高了 A549 细胞的 CT 视觉对比,而不影响细胞形态,这表明它将成为水溶性非离子型造影剂的有效口服给药途径,并且是肠道疾病检测工具的潜在候选者。