Journal of pharmaceutical sciences

1520-601711332024MarJournal of pharmaceutical sciencesJ Pharm SciSilk Fibroin-Based Coatings for Pancreatin-Dependent Drug Delivery.718724718-72410.1016/j.xphs.2023.09.001S0022-3549(23)00364-7Triggerable coatings, such as pH-responsive polymethacrylate copolymers, can be used to protect the active pharmaceutical ingredients contained within oral solid dosage forms from the acidic gastric environment and to facilitate drug delivery directly to the intestine. However, gastrointestinal pH can be highly variable, which can reduce delivery efficiency when using pH-responsive drug delivery technologies. We hypothesized that biomaterials susceptible to proteolysis could be used in combination with other triggerable polymers to develop novel enteric coatings. Bioinformatic analysis suggested that silk fibroin is selectively degradable by enzymes in the small intestine, including chymotrypsin, but resilient to gastric pepsin. Based on the analysis, we developed a silk fibroin-polymethacrylate copolymer coating for oral dosage forms. In vitro and in vivo studies demonstrated that capsules coated with this novel silk fibroin formulation enable pancreatin-dependent drug release. We believe that this novel formulation and extensions thereof have the potential to produce more effective and personalized oral drug delivery systems for vulnerable populations including patients that have impaired and highly variable intestinal physiology.Copyright © 2023 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.NavamajitiNatsudaNKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Biomedical Engineering Research Center, Faculty of Engineering, Chulalongkorn University, Bangkok, 10330, Thailand.GardnerApoloniaAKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.CaoRuonanRKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Division of Engineering Science, University of Toronto, Toronto, ON M5S 2E4, Canada.SugimotoYutaroYKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Department of Materials Engineering, Faculty of Engineering, The University of Tokyo, Tokyo, 113-0032, Japan.YangJee WonJWKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Department of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91105, USA.LopesAaronAKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.PhanNhi VNVKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.CollinsJoyJKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.HuaTiffanyTKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.DamrongsakkulSiripornSBiomedical Engineering Research Center, Faculty of Engineering, Chulalongkorn University, Bangkok, 10330, Thailand; Department of Chemical Engineering, Faculty of Engineering, Chulalongkorn University, Bangkok, 10330, Thailand; Center of Excellence in Biomaterial Engineering in Medical and Health, Faculty of Engineering, Chulalongkorn University, Bangkok, 10330, Thailand.KanokpanontSoradaSBiomedical Engineering Research Center, Faculty of Engineering, Chulalongkorn University, Bangkok, 10330, Thailand; Department of Chemical Engineering, Faculty of Engineering, Chulalongkorn University, Bangkok, 10330, Thailand; Center of Excellence in Biomaterial Engineering in Medical and Health, Faculty of Engineering, Chulalongkorn University, Bangkok, 10330, Thailand.SteigerChristophCKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Division of Gastroenterology, Department of Medicine, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.RekerDanielDKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Division of Gastroenterology, Department of Medicine, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA. Electronic address: daniel.reker@duke.edu.LangerRobertRKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Department of Chemical Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA. Electronic address: rlanger@mit.edu.TraversoGiovanniGKoch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Division of Gastroenterology, Department of Medicine, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA; Department of Mechanical Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA. Electronic address: ctraverso@bwh.harvard.edu.engP30 CA014051CANCI NIH HHSUnited StatesR01 EB000244EBNIBIB NIH HHSUnited StatesR35 GM151255GMNIGMS NIH HHSUnited StatesR37 EB000244EBNIBIB NIH HHSUnited StatesJournal ArticleResearch Support, N.I.H., ExtramuralResearch Support, Non-U.S. Gov't20230909