Encapsulation of hydrocortisone and mesalazine in zein capsules

Lau, Esther T. L., Giddings, Steven J., Mohammed, Salmaan G., Dubois, Paul, Johnson, Stuart K., Stanley, Roger A., Halley, Peter J. and Steadman, Kathryn J. (2013) Encapsulation of hydrocortisone and mesalazine in zein capsules. Pharmaceutics, 5 2: 277-293. doi:10.3390/pharmaceutics5020277

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Author Lau, Esther T. L.
Giddings, Steven J.
Mohammed, Salmaan G.
Dubois, Paul
Johnson, Stuart K.
Stanley, Roger A.
Halley, Peter J.
Steadman, Kathryn J.
Title Encapsulation of hydrocortisone and mesalazine in zein capsules
Journal name Pharmaceutics   Check publisher's open access policy
ISSN 1999-4923
Publication date 2013-05-10
Year available 2013
Sub-type Article (original research)
DOI 10.3390/pharmaceutics5020277
Open Access Status DOI
Volume 5
Issue 2
Start page 277
End page 293
Total pages 17
Place of publication Basel, Switzerland
Publisher M D P I AG
Collection year 2014
Language eng
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.
Keyword Drug loading
In vitro digestibility
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

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Created: Thu, 13 Jun 2013, 15:07:20 EST by Charna Kovacevic on behalf of School of Pharmacy