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    Encapsulation of hydrocortisone and mesalazine in zein microparticles

    191706_84785_Encapsulation_of_Hydrocortisone.pdf (672.9Kb)
    Access Status
    Open access
    Authors
    Lau, E.
    Giddings, S.
    Mohammed, S.
    Dubois, Paul
    Johnson, Stuart
    Stanley, R.
    Halley, P.
    Steadman, K.
    Date
    2013
    Type
    Journal Article
    
    Metadata
    Show full item record
    Citation
    Lau, Esther T.L. and Giddings, Steven J. and Mohammed, Salmaan G. and Dubois, Paul and Johnson, Stuart K. and Stanley, Roger A. and Halley, Peter J. and Steadman, Kathryn J. 2013. Encapsulation of hydrocortisone and mesalazine in zein microparticles. Pharmaceutics. 5 (2): pp. 277-293.
    Source Title
    Pharmaceutics
    DOI
    10.3390/pharmaceutics5020277
    ISSN
    1999-4923
    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/3.0/. Please refer to the licence to obtain terms for any further reuse or distribution of this work.

    URI
    http://hdl.handle.net/20.500.11937/33910
    Collection
    • Curtin Research Publications
    Abstract

    Zein was investigated for use as an oral-drug delivery system by loading prednisolone into zein microparticles using coacervation. To investigate the adaptability of this method to other drugs, zein microparticles were loaded with hydrocortisone, which is structurally related to prednisolone; or mesalazine, which is structurally different having a smaller LogP and ionizable functional groups. Investigations into the in vitro digestibility, and the electrophoretic profile of zein, and zein microparticles were conducted to shed further insight on using this protein as a drug delivery system. Hydrocortisone loading into zein microparticles was comparable with that reported for prednisolone, but mesalazine loading was highly variable. Depending on the starting quantities of hydrocortisone and zein, the average amount of microparticles equivalent to 4 mg hydrocortisone, (a clinically used dose), ranged from 60–115 mg, which is realistic and practical for oral dosing. Comparatively, an average of 2.5 g of microparticles was required to deliver 250 mg of mesalazine (a clinically used dose), so alternate encapsulation methods that can produce higher and more precise mesalazine loading are required. In vitro protein digestibility revealed that zein microparticles were more resistant to digestion compared to the zein raw material, and that individual zein peptides are not preferentially coacervated into the microparticles. In combination, these results suggest that there is potential to formulate a delivery system based on zein microparticles made using specific subunits of zein that is more resistant to digestion as starting material, to deliver drugs to the lower gastrointestinal tract.

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      Zein has been proposed as a polymer for targeted-drug delivery via the oral route. Zein microparticles were loaded with prednisolone and evaluated as an oral delivery system. Microparticles were formulated using phase ...
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      Kafirin, a protein extracted from sorghum grain, has been formulated into microparticles and proposed for use as a delivery system owing to the resistance of kafirin to upper gastrointestinal digestion. However, extracting ...
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