Departamento de Farmacia y Tecnología Farmacéutica, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
Carbohydr Polym. 2013 Oct 15;98(1):331-40. doi: 10.1016/j.carbpol.2013.05.091. Epub 2013 Jun 7.
5-Fluorouracil (5-FU)-loaded chitosan microgels for oral and topical chemotherapy were prepared applying a superhydrophobic surface-based encapsulation technology. Drug-loaded chitosan dispersions were cross-linked and then coated with drug-free chitosan or pectin layers at the solid-air interface in a highly efficient and environment-friendly way. The size of the microgels (with diameters of ca. 280 and 557 μm for the chitosan seeds and pectin-coated microgels respectively) was the lowest obtained until now using similar biomimetic methodologies. The microgels were characterized regarding 5-FU release profiles in vitro in aqueous media covering the pH range of the gastrointestinal tract, and cytotoxicity against two cancer cell lines sensitive to 5-FU. Owing to their control of 5-FU release in acidic medium, calcium pectinate-coated microgels can be considered as suitable for oral administration. Growth inhibition of cancer cells by 5-FU was greater when incorporated to chitosan microgels; these being potentially useful for treatment of skin and colorectal tumors.
载 5-氟尿嘧啶（5-FU）的壳聚糖微凝胶可用于口服和局部化疗，是采用基于超疏水表面的包封技术制备的。将载药壳聚糖分散体在固-气界面交联，然后以高效、环保的方式用无载药壳聚糖或果胶层进行包覆。迄今为止，采用类似仿生方法，微凝胶的粒径（壳聚糖种子和果胶包覆微凝胶的直径分别约为 280 和 557μm）是最小的。对微凝胶进行了体外水介质中 5-FU 释放特性的表征，涵盖了胃肠道的 pH 值范围，并测定了它们对两种对 5-FU 敏感的癌细胞系的细胞毒性。由于其在酸性介质中能控制 5-FU 的释放，因此钙果胶包覆的微凝胶可考虑用于口服给药。当将 5-FU 掺入壳聚糖微凝胶时，癌细胞的生长抑制作用更大；这些微凝胶可能对皮肤和结直肠肿瘤的治疗有用。
