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The colon targeting efficacies of mesalazine medications and their impacts on the gut microbiome

Laura E. Mccoubrey, Nidhi Seegobin, Nannapat Sangfuang, Frederic Moens, Hans Duyvejonck, Eline Declerck, Arno Dierick, Massimo Marzorati (UGent) and Abdul W. Basit
(2024) JOURNAL OF CONTROLLED RELEASE. 369. p.630-641
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Abstract
Successful treatment of ulcerative colitis (UC) is highly dependent on several parameters, including dosing regimen and the ability to deliver drugs to the disease site. In this study two strategies for delivering mesalazine (5-aminosalicylic acid, 5-ASA) to the colon were compared in an advanced in vitro model of the human gastrointestinal (GI) tract, the SHIME (R) system. Herein, a prodrug strategy employing bacteria-mediated drug release (sulfasalazine, Azulfidine (R)) was evaluated alongside a formulation strategy that utilised pH and bacteria-mediated release (5-ASA, Octasa (R) 1600 mg). SHIME (R) experiments were performed simulating both the GI physiology and colonic microbiota under healthy and inflammatory bowel disease (IBD) conditions, to study the impact of the disease state and ileal pH variability on colonic 5-ASA delivery. In addition, the effects of the products on the colonic microbiome were investigated by monitoring bacterial growth and metabolites. Results demonstrated that both the prodrug and formulation approaches resulted in a similar percentage of 5-ASA recovery under healthy conditions. On the contrary, during experiments simulating the GI physiology and microbiome of IBD patients (the target population) the formulation strategy resulted in a higher proportion of 5-ASA delivery to the colonic region as compared to the prodrug approach (P < 0.0001). Interestingly, the two products had distinct effects on the synthesis of key bacterial metabolites, such as lactate and short chain fatty acids, which varied according to disease state and ileal pH variability. Further, both 5-ASA and sulfasalazine significantly reduced the growth of the faecal microbiota sourced from six healthy humans. The findings support that the approach selected for colonic drug delivery could significantly influence the effectiveness of UC treatment, and highlight that drugs licensed for UC may differentially impact the growth and functioning of the colonic microbiota.
Keywords
Colonic drug delivery, Gastro resistant enteric film coatings, Phloral and opticore technologies, Targeting the large intestine, Microbiome, Mesalamine, Asacol 1600, INTESTINAL TRANSIT TIMES, PH-RESPONSIVE POLYMERS, IN-VIVO PERFORMANCE, 5-AMINOSALICYLIC ACID, DELIVERY, METABOLISM, AMINOSALICYLATES, PROFILES, BACTERIA, LACTATE

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MLA
Mccoubrey, Laura E., et al. “The Colon Targeting Efficacies of Mesalazine Medications and Their Impacts on the Gut Microbiome.” JOURNAL OF CONTROLLED RELEASE, vol. 369, 2024, pp. 630–41, doi:10.1016/j.jconrel.2024.04.016.
APA
Mccoubrey, L. E., Seegobin, N., Sangfuang, N., Moens, F., Duyvejonck, H., Declerck, E., … Basit, A. W. (2024). The colon targeting efficacies of mesalazine medications and their impacts on the gut microbiome. JOURNAL OF CONTROLLED RELEASE, 369, 630–641. https://doi.org/10.1016/j.jconrel.2024.04.016
Chicago author-date
Mccoubrey, Laura E., Nidhi Seegobin, Nannapat Sangfuang, Frederic Moens, Hans Duyvejonck, Eline Declerck, Arno Dierick, Massimo Marzorati, and Abdul W. Basit. 2024. “The Colon Targeting Efficacies of Mesalazine Medications and Their Impacts on the Gut Microbiome.” JOURNAL OF CONTROLLED RELEASE 369: 630–41. https://doi.org/10.1016/j.jconrel.2024.04.016.
Chicago author-date (all authors)
Mccoubrey, Laura E., Nidhi Seegobin, Nannapat Sangfuang, Frederic Moens, Hans Duyvejonck, Eline Declerck, Arno Dierick, Massimo Marzorati, and Abdul W. Basit. 2024. “The Colon Targeting Efficacies of Mesalazine Medications and Their Impacts on the Gut Microbiome.” JOURNAL OF CONTROLLED RELEASE 369: 630–641. doi:10.1016/j.jconrel.2024.04.016.
Vancouver
1.
Mccoubrey LE, Seegobin N, Sangfuang N, Moens F, Duyvejonck H, Declerck E, et al. The colon targeting efficacies of mesalazine medications and their impacts on the gut microbiome. JOURNAL OF CONTROLLED RELEASE. 2024;369:630–41.
IEEE
[1]
L. E. Mccoubrey et al., “The colon targeting efficacies of mesalazine medications and their impacts on the gut microbiome,” JOURNAL OF CONTROLLED RELEASE, vol. 369, pp. 630–641, 2024.
@article{01J2BDK1CHK6D6TFJS50C5FXAH,
  abstract     = {{Successful treatment of ulcerative colitis (UC) is highly dependent on several parameters, including dosing regimen and the ability to deliver drugs to the disease site. In this study two strategies for delivering mesalazine (5-aminosalicylic acid, 5-ASA) to the colon were compared in an advanced in vitro model of the human gastrointestinal (GI) tract, the SHIME (R) system. Herein, a prodrug strategy employing bacteria-mediated drug release (sulfasalazine, Azulfidine (R)) was evaluated alongside a formulation strategy that utilised pH and bacteria-mediated release (5-ASA, Octasa (R) 1600 mg). SHIME (R) experiments were performed simulating both the GI physiology and colonic microbiota under healthy and inflammatory bowel disease (IBD) conditions, to study the impact of the disease state and ileal pH variability on colonic 5-ASA delivery. In addition, the effects of the products on the colonic microbiome were investigated by monitoring bacterial growth and metabolites. Results demonstrated that both the prodrug and formulation approaches resulted in a similar percentage of 5-ASA recovery under healthy conditions. On the contrary, during experiments simulating the GI physiology and microbiome of IBD patients (the target population) the formulation strategy resulted in a higher proportion of 5-ASA delivery to the colonic region as compared to the prodrug approach (P < 0.0001). Interestingly, the two products had distinct effects on the synthesis of key bacterial metabolites, such as lactate and short chain fatty acids, which varied according to disease state and ileal pH variability. Further, both 5-ASA and sulfasalazine significantly reduced the growth of the faecal microbiota sourced from six healthy humans. The findings support that the approach selected for colonic drug delivery could significantly influence the effectiveness of UC treatment, and highlight that drugs licensed for UC may differentially impact the growth and functioning of the colonic microbiota.}},
  author       = {{Mccoubrey, Laura E. and  Seegobin, Nidhi and  Sangfuang, Nannapat and  Moens, Frederic and  Duyvejonck, Hans and  Declerck, Eline and  Dierick, Arno and Marzorati, Massimo and  Basit, Abdul W.}},
  issn         = {{0168-3659}},
  journal      = {{JOURNAL OF CONTROLLED RELEASE}},
  keywords     = {{Colonic drug delivery,Gastro resistant enteric film coatings,Phloral and opticore technologies,Targeting the large intestine,Microbiome,Mesalamine,Asacol 1600,INTESTINAL TRANSIT TIMES,PH-RESPONSIVE POLYMERS,IN-VIVO PERFORMANCE,5-AMINOSALICYLIC ACID,DELIVERY,METABOLISM,AMINOSALICYLATES,PROFILES,BACTERIA,LACTATE}},
  language     = {{eng}},
  pages        = {{630--641}},
  title        = {{The colon targeting efficacies of mesalazine medications and their impacts on the gut microbiome}},
  url          = {{http://doi.org/10.1016/j.jconrel.2024.04.016}},
  volume       = {{369}},
  year         = {{2024}},
}
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