由甲基丙烯酸缩水甘油酯葡聚糖和聚丙烯酸组成的酶降解和pH敏感水凝胶的药物释放

由甲基丙烯酸缩水甘油酯葡聚糖和聚丙烯酸组成的酶降解和pH敏感水凝胶的药物释放

Hydrogels composed of glycidyl methacrylate dextran (GMD) and poly(acrylic acid, PM) were prepared by UV irradiation method for colon-specific drug delivery. GMD was synthesized by coupling of glycidyl methacrylate to dextran in the presence of 4-(N,N-dimethylamino)pyridine. GMD was photo-polymerized by ammonium peroxydisulfate as initiating system in phosphate­buffered solution (0.1 M, pH 7.4). And then, acrylic acid monomer was added and subsequently heat-polymerized by 2,2'-azobisisobutyronitrile as an initiator. The hydrogels exhibited high swelling ratio (about 20) at $37^{\circ}C$, and showed a pH-dependent swelling behavior. In addition, the swelling ratio of the hydrogel was remarkably enhanced to about 45 times in the presence of dextranase at pH 7.4. The swelling-deswelling behavior proceeded reversibly for the GMD/PM hydrogels between pH 2 and pH 7.4. Release of 5-aminosalicylic acid from the GMD/PAA hydrogels was evaluated in simulated gastrointestinal pH fluids in the absence or presence of dextranase. We concluded that the hydrogels prepared could be used as a dual-sensitive drug carrier for sequential release in gastrointestinal tract.

采用紫外照射法制备了由甲基丙烯酸缩水甘油酯葡聚糖 (GMD) 和聚丙烯酸 (PM) 组成的水凝胶，用于结肠定位药物输送。在 4-(N,N-二甲氨基)吡啶存在下，甲基丙烯酸缩水甘油酯与葡聚糖偶联合成 GMD。以过氧化硫酸铵为引发体系，在磷酸盐缓冲溶液 (0.1 M，pH 7.4) 中对 GMD 进行光聚合。然后，加入丙烯酸单体，随后以 2,2'-偶氮二异丁腈为引发剂进行热聚合。水凝胶在 $37^{\circ}C$ 下表现出高溶胀比 (约 20)，并表现出 pH 依赖性溶胀行为。此外，在 pH 7.4 的葡聚糖酶存在下，水凝胶的溶胀比显著提高至约 45 倍。 GMD/PM 水凝胶在 pH 2 和 pH 7.4 之间可逆地进行膨胀-消膨胀行为。在模拟胃肠道 pH 液体中，在无或有葡聚糖酶的情况下，评估了 GMD/PAA 水凝胶中 5-氨基水杨酸的释放情况。我们得出结论，制备的水凝胶可用作双敏感药物载体，在胃肠道中顺序释放。

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