Synergistic gastric retention of rebamipide via hollow bioadhesive microspheres for enhanced ulcer therapy
Source abstract
Abstract
To address the low oral bioavailability and frequent dosing requirement of rebamipide, this study developed hollow bioadhesive microspheres based on a synergistic gastroretentive mechanism. The formulation utilizes ethyl cellulose/ Eudragit® EPO as the matrix to achieve buoyancy and is modified with a glyceryl monooleate coating to impart bioadhesion. The optimized microspheres exhibited a regular morphology, demonstrating excellent sustained floating and mucoadhesive properties in vitro. Animal studies confirmed significantly prolonged gastric residence time. Pharmacokinetic analysis revealed a 226% increase in relative bioavailability compared to commercial tablets. In an ethanol-induced gastric ulcer rat model, the system effectively reduced ulcer indices by prolonging local drug exposure, and showed comprehensive therapeutic effects, including anti-inflammatory, antioxidant, and enhanced mucosal defense activities, with no observed significant toxicity. This study provides an effective and safe drug delivery strategy for the local and sustained treatment of gastric ulcers.
Source: europepmc · Quality: candidate unverified · Source record ↗
Research context
OpenAlex topics: Advanced Drug Delivery Systems · Drug Solubulity and Delivery Systems · Helicobacter pylori-related gastroenterology studies
SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.
References (37)
Show source-provided references
1. Standardized aqueous extract of Abutilon theophrasti Medic. ameliorates oxidative stress and inflammatory responses against hydrochloric acid/ethanol-induced gastric ulcer in rats10.3389/fphar.2025.1599810 ↗
2. Green carbon dots derived from atractylodes macrocephala: A potential nanodrug for treating alcoholic gastric ulcer10.1016/j.colsurfb.2023.113492 ↗
3. Helicobacter pylori infection10.1038/s41572-023-00431-8 ↗
4. Rebamipide solution: a novel submucosal injection material to promote healing speed and healing quality of ulcers induced by endoscopic submucosal dissection10.1016/j.gie.2017.09.040 ↗
5. The solid state of rebamipide: Preparation, characterization, and dissolution10.1007/s12272-016-0723-y ↗
6. Effect of gastric residence time on the oral absorption of rebamipide sustained-release tablets in beagle dogs10.1007/s40005-021-00545-9 ↗
7. Repairing gastric ulcer with hyaluronic acid/extracellular matrix composite through promoting M2-type polarization of macrophages10.1016/j.ijbiomac.2023.125556 ↗
8. Helicobacter pylori infection and gastric microbiota: Insights into gastric and duodenal ulcer development10.3748/wjg.v31.i7.100044 ↗
9. Rebamipide nanocrystal with improved physicomechanical properties and its assessment through bio-mimicking 3D intestinal permeability model10.1039/D4NR03137G ↗
10. Design and evaluation of in vivo bioavailability in beagle dogs of bilayer tablet consisting of immediate release nanosuspension and sustained release layers of rebamipide10.1016/j.ijpharm.2022.121718 ↗
11. Biopharmaceutical characterization of rebamipide: The role of mucus binding in regional-dependent intestinal permeability10.1016/j.ejps.2020.105440 ↗
12. Gastro-retentive drug delivery systems and their in vivo success: A recent update
13. Expanding the Manufacturing Approaches for Gastroretentive Drug Delivery Systems with 3D Printing Technology10.3390/pharmaceutics16060790 ↗
14. Current State and Future Perspectives on Gastroretentive Drug Delivery Systems10.3390/pharmaceutics11040193 ↗
15. Overview on gastroretentive drug delivery systems for improving drug bioavailability10.1016/j.ijpharm.2016.05.016 ↗
16. Preparation and evaluation of gastro-floating hollow adhesive microspheres of carbomer/ethyl cellulose encapsulating dipyridamole10.1039/C8NJ06398B ↗
17. Preparation and evaluation of glyceryl monooleate-coated hollow-bioadhesive microspheres for gastroretentive drug delivery10.1016/j.ijpharm.2011.04.030 ↗
18. Glyceryl monooleate-coated bioadhesive hollow microspheres of riboflavin for improved gastroretentivity: optimization and pharmacokinetics10.1007/s13346-013-0143-1 ↗
19. Thiamethoxam-Loaded Ethyl Cellulose Microspheres for Extending the Efficacy Duration and Reducing the Toxicity on the Growth of Maize ( Zea mays L10.1021/acs.langmuir.4c03077 ↗
20. Development and evaluation of gastroretentive raft forming systems incorporating curcumin-Eudragit® EPO solid dispersions for gastric ulcer treatment10.1016/j.ejpb.2015.06.024 ↗
21. Improvement of lipid solubility and oral bioavailability of a poorly water- and poorly lipid-soluble drug, rebamipide, by utilizing its counter ion and SNEDDS preparation10.1016/j.ejps.2021.105721 ↗
22. A lipid-based liquid crystalline matrix that provides sustained release and enhanced oral bioavailability for a model poorly water soluble drug in rats10.1016/j.ijpharm.2007.03.020 ↗
23. Modifications of Ganoderma lucidum spores into digestive-tissue highly adherent porous carriers with selective affinity to hydrophilic or hydrophobic drugs10.1016/j.biomaterials.2023.122177 ↗
24. Physicochemical properties to determine the buoyancy of hollow microspheres (microballoons) prepared by the emulsion solvent diffusion method10.1016/S0939-6411(03)00003-1 ↗
25. Twin Screw Melt Granulation: A Single Step Approach for Developing Self-Emulsifying Drug Delivery System for Lipophilic Drugs10.3390/pharmaceutics15092267 ↗
26. Comparison of two self-nanoemulsifying drug delivery systems using different solidification techniques for enhanced solubility and oral bioavailability of poorly water-soluble celecoxib10.1016/j.colsurfb.2024.114044 ↗
27. Madhuca indica oil-entrapped buoyant galactomannan hydrogel microspheres for controlling epileptic seizures10.1016/j.ijbiomac.2024.132739 ↗
28. Development and evaluation of floating alginate microspheres for oral delivery of anthocyanins – A preliminary investigation10.1002/fsn3.451 ↗
29. Chinese herb pollen derived micromotors as active oral drug delivery system for gastric ulcer treatment
30. Prescription optimization of gastroretentive furosemide hollow-bioadhesive microspheres via box-behnken design: In vitro characterization and in vivo evaluation
31. Bioadhesive microspheres for bioavailability enhancement of raloxifene hydrochloride: Formulation and pharmacokinetic evaluation10.1208/s12249-011-9619-9 ↗
32. Rapid-release and user-friendly costunolide/dehydrocostuslactone hydrophilic nanofibers: Therapeutic effects on acute gastric ulcers10.1016/j.ijpharm.2025.125194 ↗
33. Acyl modified chitosan derivatives for oral delivery of insulin and curcumin10.1007/s10856-010-4073-x ↗
34. Emerging Antibacterial Strategies with Application of Targeting Drug Delivery System and Combined Treatment10.2147/IJN.S311248 ↗
35. In Vitro and In Vivo Test Methods for the Evaluation of Gastroretentive Dosage Forms10.3390/pharmaceutics11080416 ↗
36. Gastrointestinal Transit and Drug Absorption10.1248/bpb.25.149 ↗
37. Metabolic Behaviors of Aconitum Alkaloids in Different Concentrations of Aconiti Lateralis Radix Praeparata and Effects of Aconitine in Healthy Human and Long QT Syndrome Cardiomyocytes10.3390/molecules27134055 ↗