Sustained-release multiparticulates for oral delivery of a novel peptidic ghrelin agonist: Formulation design and in vitro characterization

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dc.contributor.author Howick, Kenneth P.
dc.contributor.author Alam, Ryan
dc.contributor.author Chruscicka, Barbara
dc.contributor.author Kandil, Dalia
dc.contributor.author Fitzpatrick, Dara
dc.contributor.author Ryan, Aoife M.
dc.contributor.author Cryan, John F.
dc.contributor.author Schellekens, Harriët
dc.contributor.author Griffin, Brendan T.
dc.date.accessioned 2017-11-27T10:12:09Z
dc.date.available 2017-11-27T10:12:09Z
dc.date.issued 2017-11-23
dc.identifier.citation Howick, K., Alam, R., Chruscicka, B., Kandil, D., Fitzpatrick, D., Ryan, A. M., Cryan, J. F., Schellekens, H. and Griffin, B. T. (2017) 'Sustained-Release Multiparticulates for Oral Delivery of a Novel Peptidic Ghrelin Agonist: Formulation Design and In Vitro Characterization', International Journal of Pharmaceutics, 536(1), pp. 63-72. doi: 10.1016/j.ijpharm.2017.11.051 en
dc.identifier.volume 536
dc.identifier.issued 1
dc.identifier.startpage 63
dc.identifier.endpage 72
dc.identifier.issn 0378-5173
dc.identifier.uri http://hdl.handle.net/10468/5092
dc.identifier.doi 10.1016/j.ijpharm.2017.11.051
dc.description.abstract There is an impetus to provide appropriate sustained release oral delivery vehicles to protect biofunctional peptide loads from gastric degradation in vivo. This study describes the generation of a high load capacity pellet formulation for sustained release of a freely water-soluble dairy-derived hydrolysate, FHI-2571. The activity of this novel peptidic ghrelin receptor agonist is reported using in vitro calcium mobilization assays. Conventional extrusion spheronization was then used to prepare peptide-loaded pellets which were subsequently coated with ethylcellulose (EC) film coats using a fluid bed coating system in bottom spray (Wurster) mode. Aqueous-based EC coating dispersions produced mechanically brittle coats which fractured due to osmotic pressure build-up within pellets in simulated media. In contrast, an ethanolic-based EC coating solution provided robust, near zero-order release in both USP Type 1 and Type 4 dissolution studies. Interestingly, the functionality of aqueous-based EC film coats was restored by first layering pellets with a methacrylic acid copolymer (MA) subcoat, thereby hindering pellet core swelling in acidic media. Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS) was utilised as a complementary technique to confirm the results seen in USP dissolution studies. Retention of activity of the ghrelinergic peptide hydrolysate in the final encapsulated product was confirmed as being greater than 80%. The described pellet formulation is amenable to oral dosing in small animal studies in order to assess in vivo efficacy of the whey-derived ghrelinergic hydrolysate. In more general terms, it is also suitable as a delivery vehicle for peptide-based bioactives to special population groups e.g paediatric and geriatric. en
dc.description.sponsorship Enterprise Ireland (grant no. TC20130001) en
dc.format.mimetype application/pdf en
dc.language.iso en en
dc.publisher Elsevier en
dc.relation.uri https://www.sciencedirect.com/science/article/pii/S0378517317311067
dc.rights © 2017 Elsevier B.V. All rights reserved. This manuscript version is made available under the CC BY-NC-ND 4.0 license. en
dc.rights.uri http://creativecommons.org/licenses/by-nc-nd/4.0/ en
dc.subject Pellet en
dc.subject Film coating en
dc.subject Sustained-release en
dc.subject Bioactive peptide en
dc.subject Ghrelin en
dc.title Sustained-release multiparticulates for oral delivery of a novel peptidic ghrelin agonist: Formulation design and in vitro characterization en
dc.type Article (peer-reviewed) en
dc.internal.authorcontactother Kenneth Howick, School Of Pharmacy, University College Cork, Cork, Ireland. +353-21-490-3000 Email: 108331464@umail.ucc.ie en
dc.internal.availability Full text available en
dc.check.info Access to this article is restricted until 12 months after publication by request of the publisher. en
dc.check.date 2018-11-23
dc.description.version Accepted Version en
dc.contributor.funder Enterprise Ireland en
dc.description.status Peer reviewed en
dc.identifier.journaltitle International Journal of Pharmaceutics en
dc.internal.copyrightchecked !!CORA!! en
dc.internal.IRISemailaddress 108331464@umail.ucc.ie
dc.internal.IRISemailaddress a.ryan@ucc.ie en
dc.internal.IRISemailaddress d.fitzpatrick@ucc.ie en
dc.internal.bibliocheck In Press, Nov 2017. Update citation details. Add volume, issue, end page start page.


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© 2017 Elsevier B.V. All rights reserved. This manuscript version is made available under the CC BY-NC-ND 4.0 license. Except where otherwise noted, this item's license is described as © 2017 Elsevier B.V. All rights reserved. This manuscript version is made available under the CC BY-NC-ND 4.0 license.
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