Novel chenodeoxycholic acid-sodium alginate matrix in the microencapsulation of the potential antidiabetic drug, probucol. An in vitro study

被引:34
|
作者
Mooranian, Armin [1 ]
Negrulj, Rebecca [1 ]
Mikov, Momir [2 ,3 ]
Golocorbin-Kon, Svetlana [2 ,3 ]
Arfuso, Frank [4 ]
Al-Salami, Hani [1 ]
机构
[1] Curtin Univ, Sch Pharm, Curtin Hlth Innovat Res Inst, Biotechnol & Drug Dev Res Lab, Perth, WA 6845, Australia
[2] Univ Novi Sad, Dept Pharmacol Toxicol & Clin Pharmacol, Fac Med, Novi Sad 21000, Serbia
[3] Univ Montenegro, Dept Pharm, Fac Med, Podgorica, Montenegro
[4] Curtin Univ, Sch Biomed Sci, Curtin Hlth Innovat Res Inst Aging & Chron Dis, Perth, WA 6845, Australia
关键词
Bile acids; chenodeoxycholic acid; microencapsulation; probucol; Type 2 diabetes mellitus; ARTIFICIAL-CELL MICROENCAPSULATION; PHARMACOLOGICAL PROPERTIES; RELEASE KINETICS; DELIVERY SYSTEM; THERAPEUTIC USE; FORMULATION; CHITOSAN;
D O I
10.3109/02652048.2015.1065922
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Context: We previously designed, developed and characterized a novel microencapsulated formulation as a platform for the targeted delivery of Probucol (PB) in an animal model of Type 2 Diabetes. Objective: The objective of this study is to optimize this platform by incorporating Chenodeoxycholic acid (CDCA), a bile acid with good permeation-enhancing properties, and examine its effect in vitro. Using sodium alginate (SA), we prepared PB-SA (control) and PB-CDCA-SA (test) microcapsules. Results and discussion: CDCA resulted in better structural and surface characteristics, uniform morphology, and stable chemical and thermal profiles, while size and rheological parameters remained unchanged. PB-CDCA-SA microcapsules showed good excipients' compatibilities, as evidenced by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, scanning electron microscopy and energy dispersive X-ray spectroscopy studies. CDCA reduced microcapsule swelling at pH 7.8 at both 37 degrees C and 25 degrees C and improved PB-release. Conclusion: CDCA improved the characteristics and release properties of PB-microcapsules and may have potential in the targeted oral delivery of PB.
引用
收藏
页码:589 / 597
页数:9
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