Gastroretentive Drug Delivery Systems: Innovative Strategies for Enhanced Gastric Retention and Improved Oral Drug Absorption

Authors

  • Pankaj Chasta
  • Kaushal Kishore Chandrul

Keywords:

Gastroretentive drug delivery systems, bioavailability, mucoadhesive, therapeutic efficacy

Abstract

Oral drug delivery is the preferred route of administration due to its convenience and patient compliance. However, it encounters limitations such as poor solubility, intestinal instability, and incomplete absorption resulting from rapid gastrointestinal transit. Gastroretentive drug delivery systems (GRDDS) have emerged as a strategy to address these challenges by prolonging gastric residence time and enhancing the bioavailability of drugs absorbed in the stomach or upper intestine. This review examines physiological factors influencing gastric retention, including gastric emptying, pH variations, and absorption windows. Various GRDDS approaches—such as floating, swelling/expandable, mucoadhesive, high-density, magnetic, and raft-forming systems—are analyzed with respect to their mechanisms, formulation strategies, and evaluation parameters. Both natural and synthetic polymers play a crucial role in designing these systems, while innovations like 3D printing, smart polymers, and nanotechnology expand their potential. Despite advancements, challenges persist in translating laboratory success to clinical outcomes. GRDDS represent an innovation for improving oral bioavailability, enabling site-specific targeting, and enhancing therapeutic efficacy for drugs with narrow absorption windows or localized gastric action

Downloads

Download data is not yet available.

References

Almansour, M. A., Aldosary, M. S., Almegbel, M. T., Alsubaie, S. A., & Alzahrani, A. M. (n.d.). Recent Innovations in Oral Drug Delivery Systems: Examining Current Challenges and Future Opportunities for Enhanced Therapeutic Efficacy. International Journal of Health Sciences, 7(S1), 3352–3370.

Alqahtani, A. A., Mohammed, A. A., Fatima, F., & Ahmed, M. M. (2023). Fused Deposition Modelling 3D-Printed Gastro-Retentive Floating Device for Propranolol Hcl Tablets. Polymers, 15(17), 3554. https://doi.org/10.3390/polym15173554

Amin, Md. L., Ahmed, T., & Mannan, Md. A. (2016). Development of Floating-Mucoadhesive Microsphere for Site Specific Release of Metronidazole. Advanced Pharmaceutical Bulletin, 6(2), 195–200. https://doi.org/10.15171/apb.2016.027

Awasthi, R., & Kulkarni, G. T. (2016). Decades of research in drug targeting to the upper gastrointestinal tract using gastroretention technologies: Where do we stand? Drug Delivery, 23(2), 378–394. https://doi.org/10.3109/10717544.2014.936535

Azman, M., Sabri, A. H., Anjani, Q. K., Mustaffa, M. F., & Hamid, K. A. (2022). Intestinal Absorption Study: Challenges and Absorption Enhancement Strategies in Improving Oral Drug Delivery. Pharmaceuticals (Basel, Switzerland), 15(8), 975. https://doi.org/10.3390/ph15080975

Bazira, P. J. (2023). Anatomy of the stomach. Surgery (Oxford), 41(11), 698–702.

Blynskaya, E. V., Tishkov, S. V., Vinogradov, V. P., Alekseev, K. V., Marakhova, A. I., & Vetcher, A. A. (2022). Polymeric Excipients in the Technology of Floating Drug Delivery Systems. Pharmaceutics, 14(12), 2779. https://doi.org/10.3390/pharmaceutics14122779

Borade, A. U., Shah, K., Kale, S. N., Katyarmal, A. D., Gajbhiye, S. S., & Kolhe, N. S. (2022). Research on natural polymer in execution of raft forming gastro- retentive drug delivery system. International Journal of Health Sciences. https://doi.org/10.53730/ijhs.v6nS1.7966

Chen, Y.-C., Ho, H.-O., Liu, D.-Z., Siow, W.-S., & Sheu, M.-T. (2015). Swelling/Floating Capability and Drug Release Characterizations of Gastroretentive Drug Delivery System Based on a Combination of Hydroxyethyl Cellulose and Sodium Carboxymethyl Cellulose. PLoS ONE, 10(1), e0116914. https://doi.org/10.1371/journal.pone.0116914

Cong, Y., Geng, J., Wang, H., Su, J., Arif, M., Dong, Q., Chi, Z., & Liu, C. (2019). Ureido-modified carboxymethyl chitosan-graft-stearic acid polymeric nano-micelles as a targeted delivering carrier of clarithromycin for Helicobacter pylori: Preparation and in vitro evaluation. International Journal of Biological Macromolecules, 129, 686–692. https://doi.org/10.1016/j.ijbiomac.2019.01.227

Daihom, B. A., Bendas, E. R., Mohamed, M. I., & Badawi, A. A. (2020). Development and in vitro evaluation of domperidone/Dowex resinate embedded gastro-floatable emulgel and effervescent alginate beads. Journal of Drug Delivery Science and Technology, 59, 101941. https://doi.org/10.1016/j.jddst.2020.101941

Daniels, I. R., & Allum, W. H. (2005). The Anatomy and Physiology of the Stomach. In Upper Gastrointestinal Surgery (pp. 17–37). Springer-Verlag. https://doi.org/10.1007/1-84628-066-4_2

Davanço, M. G., Campos, D. R., & Carvalho, P. de O. (2020). In vitro – In vivo correlation in the development of oral drug formulation: A screenshot of the last two decades. International Journal of Pharmaceutics, 580, 119210. https://doi.org/10.1016/j.ijpharm.2020.119210

Devadasu, V. R., Deb, P. K., Maheshwari, R., Sharma, P., & Tekade, R. K. (2018). Physicochemical, pharmaceutical, and biological considerations in GIT absorption of drugs. In Dosage form design considerations (pp. 149–178). Elsevier. https://www.sciencedirect.com/science/article/pii/B9780128144237000058

Djebbar, M., Chaffai, N., & Bouchal, F. (2020). Development of Floating Tablets of Metformin HCl by Thermoplastic Granulation. Part II: In Vitro Evaluation of the Combined Effect of Acacia Gum/HPMC on Biopharmaceutical Performances. Advanced Pharmaceutical Bulletin, 10(3), 399–407. https://doi.org/10.34172/apb.2020.048

Dupoiron, D., Douillard, T., & Carvajal, G. (2020). Usefulness of imaging for intrathecal drug delivery systems: An update. Medical Research Archives, 8(7). https://esmed.org/MRA/mra/article/view/2175

Faizi, S. M., Rathi, P. N., Tajane, S. V., Burghate, R. M., & Wasankar, S. R. (2012). Drug delivery to absorption window through floating microspheres: A Review. Research Journal of Pharmaceutical Dosage Forms and Technology, 4(3), 135–142.

Gupta, A., Shetty, S., Mutalik, S., Chandrashekar H, R., K, N., Mathew, E. M., Jha, A., Mishra, B., Rajpurohit, S., Ravi, G., Saha, M., & Moorkoth, S. (2023). Treatment of H. pylori infection and gastric ulcer: Need for novel Pharmaceutical formulation. Heliyon, 9(10), e20406. https://doi.org/10.1016/j.heliyon.2023.e20406

Hamed, R., Awadallah, A., Sunoqrot, S., Tarawneh, O., Nazzal, S., AlBaraghthi, T., Al Sayyad, J., & Abbas, A. (2016). pH-Dependent Solubility and Dissolution Behavior of Carvedilol—Case Example of a Weakly Basic BCS Class II Drug. AAPS PharmSciTech, 17(2), 418–426. https://doi.org/10.1208/s12249-015-0365-2

Harshdeep Desai*, T. R. (2024). Beyond Conventional: Recent Advancement on Floating Drug Delivery Systems: An Approach to Oral Controlled and Sustained Drug Delivery Via Gastric Retention. https://doi.org/10.5281/ZENODO.14546659

Huang, W.-J., & Wang, P. S. (2012). Adaptation of gastrointestinal motility to diabetes mellitus. Adaptive Medicine, 4(1), 9–14.

Ibrahim, M., Naguib, Y. W., Sarhan, H. A., & Abdelkader, H. (2019). Gastro-retentive oral drug delivery systems: A promising approach for narrow absorption window drugs. Journal of Advanced Biomedical and Pharmaceutical Sciences, 2(3), 98–110.

Kimura, T., & Higaki, K. (2002). Gastrointestinal Transit and Drug Absorption. Biological and Pharmaceutical Bulletin, 25(2), 149–164. https://doi.org/10.1248/bpb.25.149

Kumar, S., Chohan, J. S., Kaur, H., Kasnia, R., Demiwal, S., & Nehra, B. (2024). An Updated Overview of Gastro-retentive Floating Drug Delivery Systems: Formulation Strategies and Application. Journal of Drug Delivery & Therapeutics, 14(8). https://search.ebscohost.com/login.aspx?direct=true&profile=ehost&scope=site&authtype=crawler&jrnl=22501177&AN=179582746&h=foFjyCHRVB5scUnDKubQwqxOZA%2BRgNQuHHWCxqMbNIxgNAYn3evvzouplbbAfRI61AHt2UKZH2e1WcoZ7u8Rmg%3D%3D&crl=c

Liang, Y.-K., Cheng, W.-T., Chen, L.-C., Sheu, M.-T., & Lin, H.-L. (2023). Development of a Swellable and Floating Gastroretentive Drug Delivery System (sfGRDDS) of Ciprofloxacin Hydrochloride. Pharmaceutics, 15(5), 1428. https://doi.org/10.3390/pharmaceutics15051428

Liu, J., Xu, Y. T., Kong, J. J., Yu, G. S., Li, G. B., Wang, J. P., & Zheng, Y. W. (2023). Risk factors for delayed gastric emptying after laparoscopic pancreaticoduodenectomy: A single-center experience of 1 000 cases. Zhonghua Wai Ke Za Zhi [Chinese Journal of Surgery], 61(10), 882–888.

Loke, Y. H., Jayakrishnan, A., Mod Razif, M. R. F., Yee, K. M., Kee, P. E., Goh, B. H., Helal Uddin, A. B. M., Lakshminarayanan, V., & Liew, K. B. (2024). A Comprehensive Review of Challenges in Oral Drug Delivery Systems and Recent Advancements in Innovative Design Strategies. Current Pharmaceutical Design, 31(5), 360–376. https://doi.org/10.2174/0113816128338560240923073357

Martău, G. A., Mihai, M., & Vodnar, D. C. (2019). The Use of Chitosan, Alginate, and Pectin in the Biomedical and Food Sector—Biocompatibility, Bioadhesiveness, and Biodegradability. Polymers, 11(11), 1837. https://doi.org/10.3390/polym11111837

Moussa, E., Siepmann, F., Flament, M. P., Benzine, Y., Penz, F., Siepmann, J., & Karrout, Y. (2019). Controlled release tablets based on HPMC:lactose blends. Journal of Drug Delivery Science and Technology, 52, 607–617. https://doi.org/10.1016/j.jddst.2019.05.028

Nyamweya, N. N. (2021). Applications of polymer blends in drug delivery. Future Journal of Pharmaceutical Sciences, 7(1), 18. https://doi.org/10.1186/s43094-020-00167-2

Olechno, K., & Winnicka, K. (2019). Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development. Materials, 12, 3386. https://doi.org/10.3390/ma12203386

Pan, P., Svirskis, D., Waterhouse, G. I. N., & Wu, Z. (2023). Hydroxypropyl Methylcellulose Bioadhesive Hydrogels for Topical Application and Sustained Drug Release: The Effect of Polyvinylpyrrolidone on the Physicomechanical Properties of Hydrogel. Pharmaceutics, 15(9), 2360. https://doi.org/10.3390/pharmaceutics15092360

Pandey, S., Pandey, T., Khan, S., & Wamankar, S. (2024). Enhancement of Low Solubility and Low Permeability Drug Azithromycin Using Crystallization Techniques. International Journal of Advanced Multidisciplinary Research and Studies, 4(6), 917–921. https://doi.org/10.62225/2583049x.2024.4.6.3532

Sahu, V. K., Sharma, N., Sahu, P. K., & Saraf, S. A. (2017). FORMULATION AND EVALUATION OF FLOATING-MUCOADHESIVE MICROSPHERES OF NOVEL NATURAL POLYSACCHARIDE FOR SITE SPECIFIC DELIVERY OF RANITIDINE HYDROCHLORIDE. International Journal of Applied Pharmaceutics, 15–19. https://doi.org/10.22159/ijap.2017v9i3.16137

Shree, D., Patra, C. N., & Sahoo, B. M. (2022). Fabrication and Applications of Raft-Forming System—An EmergingTrend in Gastro-retentive Drug Delivery System. Nanoscience & Nanotechnology-Asia, 12(3), e070722206711. https://doi.org/10.2174/2210681212666220707141136

Sivanathan, G., Rajagopal, S., Mahadevaswamy, G., Angamuthu, G., & Dhandapani, N. V. (2024). PHARMACEUTICAL NANOCRYSTALS: AN EXTENSIVE OVERVIEW. International Journal of Applied Pharmaceutics, 1–9. https://doi.org/10.22159/ijap.2024v16i6.52257

Spósito, L., Fonseca, D., Gonçalves Carvalho, S., Sábio, R. M., Marena, G. D., Bauab, T. M., Bagliotti Meneguin, A., Parreira, P., L. Martins, M. C., & Chorilli, M. (2024). Engineering resveratrol-loaded chitosan nanoparticles for potential use against Helicobacter pylori infection. European Journal of Pharmaceutics and Biopharmaceutics, 199, 114280. https://doi.org/10.1016/j.ejpb.2024.114280

Tripathi, J., Thapa, P., Maharjan, R., & Jeong, S. H. (2019). Current State and Future Perspectives on Gastroretentive Drug Delivery Systems. Pharmaceutics, 11(4), 193. https://doi.org/10.3390/pharmaceutics11040193

Viswanadha, L. S., Arcot, Y., Lin, Y.-T., & Akbulut, M. E. S. (2024). A comparative investigation of release kinetics of paclitaxel from natural protein and macromolecular nanocarriers in nanoscale drug delivery systems. JCIS Open, 15, 100120. https://doi.org/10.1016/j.jciso.2024.100120

Vrettos, N.-N., Roberts, C. J., & Zhu, Z. (2021). Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications. Pharmaceutics, 13(10), 1591. https://doi.org/10.3390/pharmaceutics13101591

Waknis, V., & Narang, A. S. (2023). Gastroretentive Drug Delivery Systems. In M. Hu & X. Li (Eds.), Oral Bioavailability and Drug Delivery (1st ed., pp. 637–656). Wiley. https://doi.org/10.1002/9781119660699.ch33

Wang, D., Jiang, Q., Dong, Z., Meng, T., Hu, F., Wang, J., & Yuan, H. (2023). Nanocarriers transport across the gastrointestinal barriers: The contribution to oral bioavailability via blood circulation and lymphatic pathway. Advanced Drug Delivery Reviews, 203, 115130.

Wang, S., Chen, X., Han, X., Hong, X., Li, X., Zhang, H., Li, M., Wang, Z., & Zheng, A. (2023). A Review of 3D Printing Technology in Pharmaceutics: Technology and Applications, Now and Future. Pharmaceutics, 15(2), 416. https://doi.org/10.3390/pharmaceutics15020416

Wiwattanapatapee, R., Klabklay, K., Raksajit, N., Siripruekpong, W., Leelakanok, N., & Petchsomrit, A. (2023). The development of an in-situ biopolymer-based floating gel for the oral delivery of metformin hydrochloride. Heliyon, 9(4), e14796. https://doi.org/10.1016/j.heliyon.2023.e14796

Yau, A. M., McLaughlin, J., Maughan, R. J., Gilmore, W., Ashworth, J. J., & Evans, G. H. (2018). A pilot study investigating the influence of glucagon-like peptide-1 receptor single nucleotide polymorphisms on gastric emptying rate in Caucasian men. Frontiers in Physiology, 9, 1331.

Zhang, A., Jung, K., Li, A., Liu, J., & Boyer, C. (2019). Recent advances in stimuli-responsive polymer systems for remotely controlled drug release. Progress in Polymer Science, 99, 101164. https://doi.org/10.1016/j.progpolymsci.2019.101164

Zheng, B., Wang, L., Yi, Y., Yin, J., & Liang, A. (2024). Design strategies, advances and future perspectives of colon-targeted delivery systems for the treatment of inflammatory bowel disease. Asian Journal of Pharmaceutical Sciences, 19(4), 100943. https://doi.org/10.1016/j.ajps.2024.100943

Zhi, H., Zhou, P., Chen, Y., Zhao, X., Hong, Y., Lin, M., & Yang, C. (2021). Buoyancy Regulation Strategy for Underwater Profiler Based on Adaptive Genetic Algorithm. Journal of Marine Science and Engineering, 9(1), 53. https://doi.org/10.3390/jmse9010053

Downloads

Published

2025-09-11

How to Cite

1.
Chasta P, Chandrul KK. Gastroretentive Drug Delivery Systems: Innovative Strategies for Enhanced Gastric Retention and Improved Oral Drug Absorption. J Neonatal Surg [Internet]. 2025Sep.11 [cited 2025Sep.20];13(1):1121-34. Available from: https://jneonatalsurg.com/index.php/jns/article/view/9132

Issue

Section

Original Article