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    An optimized probucol microencapsulated formulation integrating a secondary bile acid (deoxycholic acid) as a permeation enhancer

    213305_139996_86206_C1_DrugDesignDevThrpy_published.pdf (7.331Mb)
    Access Status
    Open access
    Authors
    Mooranian, Armin
    Negrulj, Rebecca
    Chen-Tan, Nigel
    Watts, G.
    Arfuso, Frank
    Al-Salami, Hani
    Date
    2014
    Type
    Journal Article
    
    Metadata
    Show full item record
    Citation
    Mooranian, A. and Negrulj, R. and Chen-Tan, N. and Watts, G. and Arfuso, F. and Al-Salami, H. 2014. An optimized probucol microencapsulated formulation integrating a secondary bile acid (deoxycholic acid) as a permeation enhancer. Drug Design, Development and Therapy. 214 (8): pp. 1673-1683.
    Source Title
    Drug Design, Development and Therapy
    DOI
    10.2147/DDDT.S68247
    ISSN
    1177-8881
    School
    School of Pharmacy
    Remarks

    This article is published under the Open Access publishing model and distributed under the terms of the Creative Commons Attribution License http://creativecommons.org/licenses/by-nc/3.0/ Please refer to the licence to obtain terms for any further reuse or distribution of this work

    URI
    http://hdl.handle.net/20.500.11937/31430
    Collection
    • Curtin Research Publications
    Abstract

    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.

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