eprintid: 10096859
rev_number: 17
eprint_status: archive
userid: 608
dir: disk0/10/09/68/59
datestamp: 2020-05-06 09:45:20
lastmod: 2021-09-17 22:31:06
status_changed: 2020-05-06 09:45:20
type: article
metadata_visibility: show
creators_name: Varum, F
creators_name: Cristina Freire, A
creators_name: Bravo, R
creators_name: Basit, AW
title: OPTICORE™, an innovative and accurate colonic targeting technology
ispublished: pub
divisions: UCL
divisions: B02
divisions: C08
divisions: D10
divisions: G08
keywords: Colon targeted oral drug products, Colonic drug delivery systems, Gastro resistant film coatings, Gut microbiome, Intestinal microbiota triggered drug release, Mesalazine
note: This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions.
abstract: Inflammatory bowel disease (IBD) is a debilitating condition, estimated to affect 7 million people worldwide. Current IBD treatment strategies are substandard, relying on colonic targeting using the pH gradient along the gastrointestinal tract. Here, we describe an innovative colonic targeting concept, OPTICORE™ coating technology. OPTICORE™ combines two release triggers (pH and enzyme: Phloral™) in the outer layer, with an inner layer promoting a release acceleration mechanism (Duocoat™). The technology comprises an inner layer of partially neutralized enteric polymer with a buffer agent and an outer layer of a mixture of Eudragit® S and resistant starch. 5-aminosalicylic acid (5-ASA) tablets were coated with different inner layers, where the type of polymer, buffer salt concentration and pH of neutralization, were investigated for drug release acceleration. Buffer capacity of polymethacrylate neutralized polymer significantly contributes to the buffer capacity of the inner layer formulation, while buffer salt concentration is a major contributor to dispersion buffer capacity in the case of hypromellose enteric polymers. An interplay between buffer capacity, pH and ionic strength contributes to an accelerated drug release. Resistant starch does not impact the enteric properties but allows for drug release mediated by colonic bacterial enzymes, ensuring complete drug release. Therefore, OPTICORE™ technology is designed to offer significant advantages over standard enteric coatings, particularly for accurate colonic drug delivery in ulcerative colitis patients.
date: 2020-06-15
date_type: published
official_url: http://dx.doi.org/10.1016/j.ijpharm.2020.119372
oa_status: green
full_text_type: other
language: eng
primo: open
primo_central: open_green
verified: verified_manual
elements_id: 1779321
doi: 10.1016/j.ijpharm.2020.119372
pii: S0378-5173(20)30356-2
lyricists_name: Basit, Abdul
lyricists_id: ABASI56
actors_name: Flynn, Bernadette
actors_id: BFFLY94
actors_role: owner
full_text_status: public
publication: International Journal of Pharmaceutics
volume: 583
article_number: 119372
event_location: Netherlands
citation:        Varum, F;    Cristina Freire, A;    Bravo, R;    Basit, AW;      (2020)    OPTICORE™, an innovative and accurate colonic targeting technology.                   International Journal of Pharmaceutics , 583     , Article 119372.  10.1016/j.ijpharm.2020.119372 <https://doi.org/10.1016/j.ijpharm.2020.119372>.       Green open access   
 
document_url: https://discovery.ucl.ac.uk/id/eprint/10096859/1/1-s2.0-S0378517320303562-main.pdf