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微囊化作为潜在抗糖尿病药物普罗布考的一种新型给药方法。

Microencapsulation as a novel delivery method for the potential antidiabetic drug, Probucol.

作者信息

Mooranian Armin, Negrulj Rebecca, Chen-Tan Nigel, Al-Sallami Hesham S, Fang Zhongxiang, Mukkur T K, Mikov Momir, Golocorbin-Kon Svetlana, Fakhoury Marc, Watts Gerald F, Matthews Vance, Arfuso Frank, Al-Salami Hani

机构信息

Biotechnology and Drug Development Research Laboratory School of Pharmacy, Curtin Health Innovation Research Institute, Biosciences Research Precinct, Curtin University, Perth, Western Australia, Australia.

Faculty of Science and Engineering, Curtin University, Perth, Western Australia, Australia.

出版信息

Drug Des Devel Ther. 2014 Sep 9;8:1221-30. doi: 10.2147/DDDT.S67349. eCollection 2014.

Abstract

INTRODUCTION

In previous studies, we successfully designed complex multicompartmental microcapsules as a platform for the oral targeted delivery of lipophilic drugs in type 2 diabetes (T2D). Probucol (PB) is an antihyperlipidemic and antioxidant drug with the potential to show benefits in T2D. We aimed to create a novel microencapsulated formulation of PB and to examine the shape, size, and chemical, thermal, and rheological properties of these microcapsules in vitro.

METHOD

Microencapsulation was carried out using the Büchi-based microencapsulating system developed in our laboratory. Using the polymer, sodium alginate (SA), empty (control, SA) and loaded (test, PB-SA) microcapsules were prepared at a constant ratio (1:30). Complete characterizations of microcapsules, in terms of morphology, thermal profiles, dispersity, and spectral studies, were carried out in triplicate.

RESULTS

PB-SA microcapsules displayed uniform and homogeneous characteristics with an average diameter of 1 mm. The microcapsules exhibited pseudoplastic-thixotropic characteristics and showed no chemical interactions between the ingredients. These data were further supported by differential scanning calorimetric analysis and Fourier transform infrared spectral studies, suggesting microcapsule stability.

CONCLUSION

The new PB-SA microcapsules have good structural properties and may be suitable for the oral delivery of PB in T2D. Further studies are required to examine the clinical efficacy and safety of PB in T2D.

摘要

引言

在先前的研究中,我们成功设计了复杂的多隔室微胶囊,作为2型糖尿病(T2D)中亲脂性药物口服靶向递送的平台。普罗布考(PB)是一种抗高血脂和抗氧化药物,有可能在T2D中显示出益处。我们旨在创建一种新型的PB微囊化制剂,并在体外研究这些微胶囊的形状、大小以及化学、热学和流变学性质。

方法

使用我们实验室开发的基于Büchi的微囊化系统进行微囊化。使用聚合物海藻酸钠(SA),以恒定比例(1:30)制备空的(对照,SA)和负载的(测试,PB-SA)微胶囊。对微胶囊进行形态学、热学曲线、分散性和光谱研究等全面表征,重复进行三次。

结果

PB-SA微胶囊呈现出均匀一致的特性,平均直径为1毫米。微胶囊表现出假塑性-触变性特征,且成分之间未显示出化学相互作用。差示扫描量热分析和傅里叶变换红外光谱研究进一步支持了这些数据,表明微胶囊具有稳定性。

结论

新型PB-SA微胶囊具有良好的结构性质,可能适用于T2D中PB的口服递送。需要进一步研究来考察PB在T2D中的临床疗效和安全性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a59c/4166910/e5c735319c02/dddt-8-1221Fig1.jpg

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