Szekalska Marta, Sosnowska Katarzyna, Zakrzeska Agnieszka, Kasacka Irena, Lewandowska Alicja, Winnicka Katarzyna
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2c, Białystok 15-222, Poland.
Department of Biopharmacy, Medical University of Białystok, Mickiewicza 2c, Białystok 15-222, Poland.
Molecules. 2017 Jan 22;22(1):182. doi: 10.3390/molecules22010182.
Sodium alginate is a polymer with unique ability to gel with different cross-linking agents in result of ionic and electrostatic interactions. Chitosan cross-linked alginate provides improvement of swelling and mucoadhesive properties and might be used to design sustained release dosage forms. Therefore, the aim of this research was to develop and evaluate possibility of preparing chitosan cross-linked alginate microparticles containing metformin hydrochloride by the spray-drying method. In addition, influence of cross-linking agent on the properties of microparticles was evaluated. Formulation of microparticles prepared by the spray drying of 2% alginate solution cross-linked by 0.1% chitosan was characterized by good mucoadhesive properties, high drug loading and prolonged metformin hydrochloride release. It was shown that designed microparticles reduced rat glucose blood level, delayed absorption of metformin hydrochloride and provided stable plasma drug concentration. Additionally, histopathological studies of pancreas, liver and kidneys indicated that all prepared microparticles improved degenerative changes in organs of diabetic rats. Moreover, no toxicity effect and no changes in rats behavior after oral administration of chitosan cross-linked alginate microparticles were noted.
海藻酸钠是一种聚合物，由于离子和静电相互作用，它具有与不同交联剂形成凝胶的独特能力。壳聚糖交联海藻酸盐可改善溶胀和粘膜粘附性能，可用于设计缓释剂型。因此，本研究的目的是开发并评估通过喷雾干燥法制备含盐酸二甲双胍的壳聚糖交联海藻酸盐微粒的可能性。此外，还评估了交联剂对微粒性质的影响。通过喷雾干燥2%海藻酸盐溶液并用0.1%壳聚糖交联制备的微粒制剂具有良好的粘膜粘附性能、高载药量和盐酸二甲双胍的缓释特性。结果表明，所设计的微粒降低了大鼠血糖水平，延迟了盐酸二甲双胍的吸收，并提供了稳定的血浆药物浓度。此外，胰腺、肝脏和肾脏的组织病理学研究表明，所有制备的微粒均改善了糖尿病大鼠器官的退行性变化。而且，口服壳聚糖交联海藻酸盐微粒后未观察到对大鼠的毒性作用和行为变化。
