Grupo de Nuevos Materiales y Espectroscopia Supramolecular, Departamento de Química Física, Facultad de Ciencia y Tecnología, Universidad del País Vasco (UPV/EHU), 644 Bilbao, Spain.
Carbohydr Polym. 2014 Jan 30;101:113-20. doi: 10.1016/j.carbpol.2013.09.014. Epub 2013 Sep 16.
Folate-chitosan conjugates were prepared by a concurrent functionalization and crosslinking reaction with the natural crosslinker genipin. Genipin molecule was employed simultaneously as crosslinker agent and spacer molecule in order to allow the functionalization with folic acid for active tumor targeting. The reaction was carried out in reverse microemulsion which provided colloidal size and monodisperse particle size distribution. The water solubility of the obtained folate-genipin-chitosan nanogels was studied as function of the pH of the medium and all nanoparticles were totally dispersible at physiological pH. The enzymatic degradability of the nanogels in a lysozyme solution was evaluated at acidic and physiological pH. QELS analyses of the swelling behavior of the nanogels with the pH did not show a clear pH-sensitivity. However, the study on the loading and release capacity of 5-fluorouracil revealed an interesting pH-responsive behavior of the nanogels that makes them promising as nanodevices for targeted anticancer drug delivery.
叶酸-壳聚糖缀合物通过与天然交联剂京尼平的同时功能化和交联反应来制备。京尼平分子同时被用作交联剂和间隔分子，以允许与叶酸进行功能化，实现主动肿瘤靶向。该反应在反相微乳液中进行，提供胶体大小和单分散的颗粒尺寸分布。研究了所得叶酸-京尼平-壳聚糖纳米凝胶在介质 pH 值下的水溶性，所有纳米颗粒在生理 pH 值下完全可分散。在酸性和生理 pH 值下，在溶菌酶溶液中评估了纳米凝胶的酶降解性。随着 pH 值的 QELS 分析表明纳米凝胶的溶胀行为没有明显的 pH 敏感性。然而，对 5-氟尿嘧啶的负载和释放能力的研究揭示了纳米凝胶的一种有趣的 pH 响应行为，这使得它们有望成为用于靶向抗癌药物递送的纳米器件。
