Mooranian Armin, Negrulj Rebecca, Chen-Tan Nigel, Watts Gerald F, Arfuso Frank, Al-Salami Hani
Biotechnology and Drug Development Research Laboratory, School of Pharmacy, Curtin Health Innovation Research Institute, Biosciences Research Precinct, Curtin University, Perth, Australia.
Faculty of Science and Engineering, Curtin University, Perth, Australia.
Drug Des Devel Ther. 2014 Sep 29;8:1673-83. doi: 10.2147/DDDT.S68247. eCollection 2014.
The authors have previously designed, developed, and characterized a novel microencapsulated formulation as a platform for the targeted delivery of therapeutics in an animal model of type 2 diabetes, using the drug probucol (PB). The aim of this study was to optimize PB microcapsules by incorporating the bile acid deoxycholic acid (DCA), which has good permeation-enhancing properties, and to examine its effect on microcapsules' morphology, rheology, structural and surface characteristics, and excipients' chemical and thermal compatibilities. Microencapsulation was carried out using a BÜCHI-based microencapsulating system established in the authors' laboratory. Using the polymer sodium alginate (SA), two microencapsulated formulations were prepared: PB-SA (control) and PB-DCA-SA (test) at a constant ratio (1:30 and 1:3:30, respectively). Complete characterization of the microcapsules was carried out. The incorporation of DCA resulted in better structural and surface characteristics, uniform morphology, and stable chemical and thermal profiles, while size and rheological parameters remained similar to control. In addition, PB-DCA-SA microcapsules showed good excipients' compatibilities, which were supported by data from differential scanning calorimetry, Fourier transform infrared spectroscopy, scanning electron microscopy, and energy dispersive X-ray studies, suggesting microcapsule stability. Hence, PB-DCA-SA microcapsules have good rheological and compatibility characteristics and may be suitable for the oral delivery of PB in type 2 diabetes.
作者先前已设计、开发并表征了一种新型微囊制剂，作为在2型糖尿病动物模型中靶向递送治疗药物的平台，使用的药物是普罗布考（PB）。本研究的目的是通过加入具有良好渗透增强特性的胆汁酸脱氧胆酸（DCA）来优化PB微囊，并研究其对微囊形态、流变学、结构和表面特性以及辅料化学和热相容性的影响。微囊化是使用作者实验室建立的基于BÜCHI的微囊化系统进行的。使用聚合物海藻酸钠（SA），以恒定比例（分别为1:30和1:3:30）制备了两种微囊制剂：PB-SA（对照）和PB-DCA-SA（测试）。对微囊进行了全面表征。加入DCA后，微囊具有更好的结构和表面特性、均匀的形态以及稳定的化学和热特性，而尺寸和流变学参数与对照相似。此外，PB-DCA-SA微囊显示出良好的辅料相容性，差示扫描量热法、傅里叶变换红外光谱、扫描电子显微镜和能量色散X射线研究的数据支持了这一点，表明微囊具有稳定性。因此，PB-DCA-SA微囊具有良好的流变学和相容性特性，可能适用于2型糖尿病中PB的口服给药。
