Program of Petrochemistry and Polymer Science, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
Metallurgy and Materials Science Research Institute, Chulalongkorn University, Bangkok 10330, Thailand.
Int J Biol Macromol. 2014 Mar;64:240-6. doi: 10.1016/j.ijbiomac.2013.12.012. Epub 2013 Dec 17.
4-Carboxybenzensulfonamide-chitosan (4-CBS-chitosan) microspheres were prepared by electrospraying with acetazolamide (ACZ) as a model drug. The obtained 4-CBS-chitosan microspheres with or without ACZ-loading were characterized by Fourier transform infrared spectroscopy, differential scanning colorimetry, scanning electron microscopy and particle size analyses. The crystalline form and the stability of ACZ in a basic solution was determined using X-ray single crystal analysis. 4-CBS-chitosan had 90% encapsulation efficiency for ACZ compared to 47% of encapsulation efficiency (EE) obtained from native chitosan, forming 3.1 μm diameter microspheres with a low polydispersity index (0.4). After an initial burst release (58% in 5 min), ACZ-loaded 4-CBS-chitosan gave a sustained release of ACZ (∼ 100% over 3h) in simulated gastric fluid (0.1N HCl; pH 1.2), which was better than that seen for the release from ACZ-loaded chitosan (44% over 1.5h). Thus, 4-CBS-chitosan microspheres are a possible drug carrier in acidic conditions, such as at the gastric mucosal wall.
4-羧苯磺酰胺壳聚糖（4-CBS-壳聚糖）微球通过电喷雾法用乙酰唑胺（ACZ）作为模型药物制备。用傅里叶变换红外光谱、差示扫描量热法、扫描电子显微镜和粒径分析对载有或未载有 ACZ 的所得 4-CBS-壳聚糖微球进行了表征。通过 X 射线单晶分析确定了 ACZ 在碱性溶液中的晶体形式和稳定性。与天然壳聚糖 47%的包封效率相比，4-CBS-壳聚糖对 ACZ 的包封效率为 90%，形成 3.1μm 直径的微球，具有较低的多分散指数（0.4）。在初始突释（5min 内 58%）之后，载有 ACZ 的 4-CBS-壳聚糖在模拟胃液（0.1N HCl；pH 1.2）中能够持续释放 ACZ（3h 内约 100%），优于载有 ACZ 的壳聚糖的释放（1.5h 内 44%）。因此，4-CBS-壳聚糖微球在酸性条件下（如胃黏膜壁）可能是一种药物载体。
