Biomedical Engineering, University of Texas at Austin, 1 University Station C0400, Austin, TX 78712, USA.
Acta Biomater. 2010 Jan;6(1):48-56. doi: 10.1016/j.actbio.2009.05.032. Epub 2009 May 28.
A novel class of pH-sensitive complexation hydrogels composed of methacrylic acid and functionalized poly(ethylene glycol) (PEG) tethers, referred to as P(MAA-g-EG) WGA, was investigated as an oral protein delivery system. The PEG tethers were functionalized with wheatgerm agglutinin (WGA), a lectin that can bind to carbohydrates in the intestinal mucosa, to improve residence time of the carrier and absorption of the drug at the delivery site. The ability of P(MAA-g-EG) WGA to improve insulin absorption was observed in two different intestinal epithelial models. In Caco-2 cells P(MAA-g-EG) WGA improved insulin permeability 9-fold as compared with an insulin only solution, which was similar to the improvement by P(MAA-g-EG). P(MAA-g-EG) and P(MAA-g-EG) WGA were also evaluated in a mucus-secreting culture that contained Caco-2 and HT29-MTX cells. Insulin permeability was increased 5-fold in the presence of P(MAA-g-EG) and P(MAA-g-EG) WGA. Overall, it is clear that P(MAA-g-EG) WGA enhances insulin absorption and holds great promise as an oral insulin delivery system.
研究了一类新型的 pH 敏感的络合水凝胶,由甲基丙烯酸和功能化的聚乙二醇(PEG)链组成,称为 P(MAA-g-EG)WGA,将其作为口服蛋白质递药系统。PEG 链用麦胚凝集素(WGA)进行了功能化,WGA 是一种可以与肠黏膜上的碳水化合物结合的凝集素,以提高载体的停留时间和药物在给药部位的吸收。在两种不同的肠上皮细胞模型中观察到 P(MAA-g-EG)WGA 提高胰岛素吸收的能力。在 Caco-2 细胞中,与仅胰岛素溶液相比,P(MAA-g-EG)WGA 将胰岛素的通透性提高了 9 倍,这与 P(MAA-g-EG)相似。还在含有 Caco-2 和 HT29-MTX 细胞的分泌黏液的培养物中评价了 P(MAA-g-EG)和 P(MAA-g-EG)WGA。在 P(MAA-g-EG)和 P(MAA-g-EG)WGA 的存在下,胰岛素的通透性增加了 5 倍。总之,很明显 P(MAA-g-EG)WGA 增强了胰岛素的吸收,作为口服胰岛素递药系统具有很大的应用前景。