Gastroretentive drug delivery systems: A holy grail in oral delivery

• Published in: Drug discovery today Vol. 30; no. 4; p. 104340
• Main Author: Omidian, Hossein
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.04.2025
• Subjects: Administration, Oral; Animals; Biological Availability; controlled release systems; Delayed-Action Preparations; Drug Delivery Systems - methods; Drug Liberation; enhanced bioavailability; Gastric Mucosa - metabolism; Gastric retention platforms; gastroretentive technologies; Humans; mucoadhesive drug delivery; Nanoparticles; Pharmaceutical Preparations - administration & dosage; Polymers - chemistry; gastroretentive technologies; mucoadhesive drug delivery; Gastric retention platforms; controlled release systems; enhanced bioavailability
• ISSN: 1359-6446; 1878-5832; 1878-5832
• DOI: 10.1016/j.drudis.2025.104340

•Gastroretentive platforms extend gastric residence for up to 24 h for superior drug delivery.•Innovative designs improve bioavailability up to 3.5-fold for narrow absorption window drugs.•Validation techniques such as gamma scintigraphy confirm prolonged retention and optimized drug profiles.•Emerging technologies, including 3D printing and nanocarriers, enhance precision and scalability.•Multifunctional designs combine buoyancy, adhesion, and swelling for robust gastroretentive performance. Gastroretentive drug delivery systems (GRDDSs) offer a promising strategy for enhancing oral drug bioavailability by prolonging gastric residence time and enabling site-specific drug release. This review examines the key materials used in GRDDSs, including polymers for controlled drug release, gas-generating agents for buoyancy, and mucoadhesive components for improved retention and stability. Advances in fabrication techniques, such as 3D printing, spray drying, and nanoparticle encapsulation, have enabled precise modulation of drug release kinetics and retention properties. However, challenges such as inter-subject variability, physiological constraints, and manufacturing scalability remain. Future research will focus on smart materials, multi-drug platforms, and expanding applications to biologics and nutraceuticals, paving the way for more effective and patient-compliant oral drug delivery systems.