Encapsulation of Hydrocortisone and Mesalazine in Zein Microparticles

Lau, Esther T.L., Giddings, Steven, Mohammed, Salmaan, Dubois, Paul, Johnson, Stuart, Stanley, Roger, Halley, Peter, & Steadman, Kathryn (2013) Encapsulation of Hydrocortisone and Mesalazine in Zein Microparticles. Pharmaceutics, 5(2), pp. 277-293.

View at publisher (open access)

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.

Impact and interest:

10 citations in Scopus
Search Google Scholar™

Citation counts are sourced monthly from Scopus and Web of Science® citation databases.

These databases contain citations from different subsets of available publications and different time periods and thus the citation count from each is usually different. Some works are not in either database and no count is displayed. Scopus includes citations from articles published in 1996 onwards, and Web of Science® generally from 1980 onwards.

Citations counts from the Google Scholar™ indexing service can be viewed at the linked Google Scholar™ search.

Full-text downloads:

245 since deposited on 16 Sep 2014
128 in the past twelve months

Full-text downloads displays the total number of times this work’s files (e.g., a PDF) have been downloaded from QUT ePrints as well as the number of downloads in the previous 365 days. The count includes downloads for all files if a work has more than one.

ID Code: 76171
Item Type: Journal Article
Refereed: Yes
Keywords: Drug loading; Electrophoresis; In vitro digestibility; Maize; Microparticles; Protein, hydrocortisone; mesalazine; zein; article; controlled study; drug delivery system; drug formulation; drug solubility; drug structure; electrophoresis; in vitro study; microencapsulation; pH measurement; protein content; protein degradation; protein electr
DOI: 10.3390/pharmaceutics5020277
ISSN: 1999-4923
Subjects: Australian and New Zealand Standard Research Classification > MEDICAL AND HEALTH SCIENCES (110000) > PHARMACOLOGY AND PHARMACEUTICAL SCIENCES (111500) > Pharmaceutical Sciences (111504)
Divisions: Current > Schools > School of Clinical Sciences
Current > QUT Faculties and Divisions > Faculty of Health
Current > Institutes > Institute of Health and Biomedical Innovation
Copyright Owner: Copyright 2013 by the authors; licensee MDPI, Basel, Switzerland.
Copyright Statement: This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/)
Deposited On: 16 Sep 2014 02:42
Last Modified: 17 Dec 2015 23:57

Export: EndNote | Dublin Core | BibTeX

Repository Staff Only: item control page