{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T05:01:05Z","timestamp":1787029265908,"version":"build-2736575974"},"reference-count":43,"publisher":"MDPI AG","issue":"4","license":[{"start":{"date-parts":[[2021,4,18]],"date-time":"2021-04-18T00:00:00Z","timestamp":1618704000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/100000002","name":"National Institutes of Health","doi-asserted-by":"publisher","award":["U01 HL127518"],"award-info":[{"award-number":["U01 HL127518"]}],"id":[{"id":"10.13039\/100000002","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000002","name":"National Institutes of Health","doi-asserted-by":"publisher","award":["R01 DK123712"],"award-info":[{"award-number":["R01 DK123712"]}],"id":[{"id":"10.13039\/100000002","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100007028","name":"Leona M. and Harry B. Helmsley Charitable Trust","doi-asserted-by":"publisher","award":["N\/A"],"award-info":[{"award-number":["N\/A"]}],"id":[{"id":"10.13039\/100007028","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>Epicertin (EPT) is a recombinant variant of the cholera toxin B subunit, modified with a C-terminal KDEL endoplasmic reticulum retention motif. EPT has therapeutic potential for ulcerative colitis treatment. Previously, orally administered EPT demonstrated colon epithelial repair activity in dextran sodium sulfate (DSS)-induced acute and chronic colitis in mice. However, the oral dosing requires cumbersome pretreatment with sodium bicarbonate to conserve the acid-labile drug substance while transit through the stomach, hampering its facile application in chronic disease treatment. Here, we developed a solid oral formulation of EPT that circumvents degradation in gastric acid. EPT was spray-dried and packed into enteric-coated capsules to allow for pH-dependent release in the colon. A GM1-capture KDEL-detection ELISA and size-exclusion HPLC indicated that EPT powder maintains activity and structural stability for up to 9 months. Capsule disintegration tests showed that EPT remained encapsulated at pH 1 but was released over 180 min at pH 6.8, the approximate pH of the proximal colon. An acute DSS colitis study confirmed the therapeutic efficacy of encapsulated EPT in C57BL\/6 mice upon oral administration without gastric acid neutralization pretreatment compared to vehicle-treated mice (p &lt; 0.05). These results provide a foundation for an enteric-coated oral formulation of spray-dried EPT.<\/jats:p>","DOI":"10.3390\/pharmaceutics13040576","type":"journal-article","created":{"date-parts":[[2021,4,19]],"date-time":"2021-04-19T06:35:53Z","timestamp":1618814153000},"page":"576","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Spray-Dried Formulation of Epicertin, a Recombinant Cholera Toxin B Subunit Variant That Induces Mucosal Healing"],"prefix":"10.3390","volume":"13","author":[{"given":"Micaela A.","family":"Reeves","sequence":"first","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Louisville School of Medicine, Louisville, KY 40202, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Joshua M.","family":"Royal","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Louisville School of Medicine, Louisville, KY 40202, USA"},{"name":"James Graham Brown Cancer Center, University of Louisville School of Medicine, Louisville, KY 40202, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"David A.","family":"Morris","sequence":"additional","affiliation":[{"name":"James Graham Brown Cancer Center, University of Louisville School of Medicine, Louisville, KY 40202, USA"},{"name":"Center for Predictive Medicine, University of Louisville School of Medicine, Louisville, KY 40202, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jessica M.","family":"Jurkiewicz","sequence":"additional","affiliation":[{"name":"James Graham Brown Cancer Center, University of Louisville School of Medicine, Louisville, KY 40202, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7231-3004","authenticated-orcid":false,"given":"Nobuyuki","family":"Matoba","sequence":"additional","affiliation":[{"name":"Department of Pharmacology and Toxicology, University of Louisville School of Medicine, Louisville, KY 40202, USA"},{"name":"James Graham Brown Cancer Center, University of Louisville School of Medicine, Louisville, KY 40202, USA"},{"name":"Center for Predictive Medicine, University of Louisville School of Medicine, Louisville, KY 40202, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Krystal T.","family":"Hamorsky","sequence":"additional","affiliation":[{"name":"James Graham Brown Cancer Center, University of Louisville School of Medicine, Louisville, KY 40202, USA"},{"name":"Center for Predictive Medicine, University of Louisville School of Medicine, Louisville, KY 40202, USA"},{"name":"Department of Medicine, University of Louisville School of Medicine, Louisville, KY 40202, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2021,4,18]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"91","DOI":"10.3748\/wjg.v20.i1.91","article-title":"Inflammatory bowel disease: Pathogenesis","volume":"20","author":"Zhang","year":"2014","journal-title":"World J. 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