• MANDAR J BHANDWALKAR Department of Pharmaceutics, YSPM’s Yashoda Technical Campus, Faculty of Pharmacy, Satara, Maharashtra, India.
  • PRASAD S DUBAL Department of Pharmaceutics, YSPM’s Yashoda Technical Campus, Faculty of Pharmacy, Satara, Maharashtra, India.
  • AKASH K.TUPE Department of Pharmaceutics, YSPM’s Yashoda Technical Campus, Faculty of Pharmacy, Satara, Maharashtra, India.
  • SUPRIYA N MANDRUPKAR KIMS Deemed to be University’s Krishna Institute of Pharmacy, Karad, India.


In recent years, gastroretentive drug delivery system (GRDDS) has gained researcher’s interest in the field of oral drug delivery. Various GRDDS approaches can be utilized to retain the dosage forms in the stomach and to release the drug slowly for an extended period of time. GRDDS can be used to prolong the residence time of delivery system in the stomach. This results in targeting of drug release at a specific site for the systemic or local effects. GRDDS can be used to overcome challenges associated with conventional oral dosage forms and to release the drug at a specific absorption site to improve bioavailability of particular drug substance. The challenges include fast gastric emptying of the dosage form which results in the poor bioavailability of the drug. Prolongation of the retention of drugs in stomach those having low solubility at high intestinal pH improves the solubility of drugs. GRDDS has proved to be effective in systemic actions as well as in local actions to treat gastric or duodenal ulcers. Local activity in the upper part of the small intestine can be obtained by improving the residence time of delivery system in the stomach. The system is useful for drugs which are unstable in the intestine or having a low solubility/permeability in the small intestine. Various GRDDS approaches include high density (sinking) systems, low-density (floating systems), mucoadhesive, expandable, unfoldable, superporous hydrogel systems, and magnetic systems.

Keywords: Gastroretentive drug delivery system, Gastric residence time, Migrating motor complex, Oral controlled release, Floating drug delivery, Gastrointestinal tract


1. Misra A, Singh B. Gastroretentive drug delivery systems. In: In Vitro in Vivo Tools Drug Delivery Research for Optimum Clinical Outcomes. United Kingdom: Taylor & Francis Group; 2018. p. 173-208.
2. Kesarla RS, Vora PA, Sridhar BK, Patel G, Omri A. Formulation and evaluation of floating tablet of H2-receptor antagonist. Drug Dev Ind Pharm 2015;41:1499-511.
3. Prinderre P, Sauzet C, Fuxen C. Advances in gastro retentive drug-delivery systems. Expert Opin Drug Deliv 2011;8:1189-203.
4. Aoki H, Iwao Y, Mizoguchi M, Noguchi S, Itai S. Clarithromycin highly-loaded gastro-floating fine granules prepared by high-shear melt granulation can enhance the efficacy of Helicobacter pylori eradication. Eur J Pharm Biopharm 2015;92:22-7.
5. Kim JY, Bae HJ, Choi J, Lim JR, Kim SW, Lee SH, et al. Efficacy of gastro-retentive forms of ecabet sodium in the treatment of gastric ulcer in rats. Arch Pharm Res 2014;37:1053-62.
6. Garg R, Gupta G. Progress in controlled gastroretentive delivery systems. Trop J Pharm Res 2008;7:1055-66.
7. Matharu RS, Sanghavi NM. Novel drug delivery system for captopril. Drug Dev Ind Pharm 1992;18:1567-74.
8. Rouge N, Allémann E, Gex-Fabry M, Balant L, Cole ET, Buri P, et al. Comparative pharmacokinetic study of a floating multiple-unit capsule, a high-density multiple-unit capsule and an immediate-release tablet containing 25 mg atenolol. Pharm Acta Helv 1998;73:81-7.
9. Sharma S, Pawar A. Low density multiparticulate system for pulsatile release of meloxicam. Int J Pharm 2006;313:150-8.
10. Goole J, Vanderbist F, Amighi K. Development and evaluation of new multiple-unit levodopa sustained-release floating dosage forms. Int J Pharm 2007;334:35-41.
11. Santus G, Lazzarini C, Bottoni G, Sandefer EP, Page RC, Doll WJ, et al. An in vitro-in vivo investigation of oral bioadhesive controlled release furosemide formulations. Eur J Pharm Biopharm 1997;44:39-52.
12. Klausner EA, Lavy E, Friedman M, Hoffman A. Expandable gastroretentive dosage forms. J Control Release 2003;90:143-62.
13. Park K. Enzyme-digestible swelling hydrogels as platforms for long-term oral drug delivery: Synthesis and characterization. Biomaterials 1988;9:435-41.
14. Prajapati VD, Jani GK, Khutliwala TA, Zala BS. Raft forming system-an upcoming approach of gastroretentive drug delivery system. J Control Release 2013;168:151-65.
15. Arora S, Ali J, Ahuja A, Khar RK, Baboota S. Floating drug delivery systems: A review. AAPS PharmSciTech 2005;6:372-90.
16. Pawar VK, Kansal S, Garg G, Awasthi R, Singodia D, Kulkarni GT. Gastroretentive dosage forms: A review with special emphasis on floating drug delivery systems. Drug Deliv 2011;18:97-110.
17. Streubel A, Siepmann J, Bodmeier R. Drug delivery to the upper small intestine window using gastroretentive technologies. Curr Opin Pharmacol 2006;6:501-8.
18. Laulicht B, Tripathi A, Schlageter V, Kucera P, Mathiowitz E. Understanding gastric forces calculated from high-resolution pill tracking. Proc Natl Acad Sci U S A 2010;107:8201-6.
19. Talukder R, Fassihi R. Gastroretentive delivery systems: A mini review. Drug Dev Ind Pharm 2004;30:1019-28.
20. Minami H, Mccallum RW. The physiology and pathophysiology of gastric emptying in humans. Gastroenterology 1984;86:1592-610.
21. Mandal UK, Chatterjee B, Senjoti FG. Gastro-retentive drug delivery systems and their in vivo success: A recent update. Asian J Pharm Sci 2016;11:575-84.
22. Wilson C, Washington N, Washington C, Physiological Pharmaceutics: Barriers to Drug Absorption. United States: CRC Press; 2000.
23. O’Reilly S, Wilson CG, Hardy JG. The influence of food on the gastric emptying of multiparticulate dosage forms. Int J Pharm 1987;34:213-6.
24. Khosla R, Feely LC, Davis SS. Gastrointestinal transit of non-disintegrating tablets in fed subjects. Int J Pharm 1989;53:107-17.
25. Khosla R, Davis SS. The effect of tablet size on the gastric emptying of non-disintegrating tablets. Int J Pharm 1990;62:R9.
26. Timmermans J, Moës AJ. Factors controlling the buoyancy and gastric retention capabilities of floating matrix capsules: New data for reconsidering the controversy. J Pharm Sci 1994;83:18-24.
27. Bennett CE, Hardy JG, Wilson CG. The influence of posture on the gastric emptying of antacids. Int J Pharm 1984;21:341-7.
28. Coupe AJ, Davis SS, Evans DF, Wilding IR. Nocturnal scintigraphic imaging to investigate the gastrointestinal transit of dosage forms. J Control Release 1992;20:155-62.
29. Nimmo J, Heading RC, Tothil P, Prescott LF. Pharmacological modification of gastric emptying: Effects of propantheline and metoclopromide on paracetamol absorption. Br Med J 1973;1:587-9.
30. Umamaheshwari RB, Ramteke S, Jain NK. Anti-Helicobacter pylori effect of mucoadhesive nanoparticles bearing amoxicilin in experimental gerbils model. AAPS PharmSciTech 2004;5:60-8.
31. Lopes CM, Bettencourt C, Rossi A, Buttini F, Barata P. Overview on gastroretentive drug delivery systems for improving drug bioavailability. Int J Pharm 2016;510:144-58.
32. El-Zahaby SA, Kassem AA, El-Kamel AH. Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori. Saudi Pharm J 2014;22:570-9.
33. Cvijic S, Ibric S, Parojcic J, Djuris J. An in vitro-in silico approach for the formulation and characterization of ranitidine gastroretentive delivery systems. J Drug Deliv Sci Technol 2018;45:1-10.
34. Diós P, Nagy S, Pál S, Pernecker T, Kocsis B, Budán F, et al. Preformulation studies and optimization of sodium alginate based floating drug delivery system for eradication of Helicobacter pylori. Eur J Pharm Biopharm 2015;96:196-206.
35. Fu J, Yin H, Yu X, Xie C, Jiang H, Jin Y, et al. Combination of 3D printing technologies and compressed tablets for preparation of riboflavin floating tablet-in-device (TiD) systems. Int J Pharm 2018;549:370-9.
36. Kagan L, Lapidot N, Afargan M, Kirmayer D, Moor E, Mardor Y, et al. Gastroretentive accordion pill: Enhancement of riboflavin bioavailability in humans. J Control Release 2006;113:208-15.
37. Sarkar D, Nandi G, Changder A, Hudati P, Sarkar S, Ghosh LK. Sustained release gastroretentive tablet of metformin hydrochloride based on poly (acrylic acid)-grafted-gellan. Int J Biol Macromol 2017;96:137-48.
38. Thapa P, Jeong SH. Effects of formulation and process variables on gastroretentive floating tablets with a high-dose soluble drug and experimental design approach. Pharmaceutics 2018;10:9-12.
39. Oh TO, Kim JY, Ha JM, Chi SC, Rhee YS, Park CW, et al. Preparation of highly porous gastroretentive metformin tablets using a sublimation method. Eur J Pharm Biopharm 2013;83:460-7.
40. He W, Li Y, Zhang R, Wu Z, Yin L. Gastro-floating bilayer tablets for the sustained release of metformin and immediate release of pioglitazone: Preparation and in vitro/in vivo evaluation. Int J Pharm 2014;476:223-31.
41. Hwang KM, Cho CH, Tung NT, Kim JY, Rhee YS, Park ES. Release kinetics of highly porous floating tablets containing cilostazol. Eur J Pharm Biopharm 2017;115:39-51.
42. Qin C, Wu M, Xu S, Wang X, Shi W, Dong Y, et al. Design and optimization of gastro-floating sustained-release tablet of pregabalin: In vitro and in vivo evaluation. Int J Pharm 2018;545:37-44.
43. Sawicki W. Pharmacokinetics of verapamil and norverapamil from controlled release floating pellets in humans. Eur J Pharm Biopharm 2002;53:29-35.
44. Jiménez-Martínez I, Quirino-Barreda T, Villafuerte-Robles L. Sustained delivery of captopril from floating matrix tablets. Int J Pharm 2008;362:37-43.
45. Chavanpatil MD, Jain P, Chaudhari S, Shear R, Vavia PR. Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin. Int J Pharm 2006;316:86-92.
46. Sethi S, Mangla B, Kamboj S, Rana V. A QbD approach for the fabrication of immediate and prolong buoyant cinnarizine tablet using polyacrylamide-g-corn fibre gum. Int J Biol Macromol 2018;117:350-61.
47. Kotreka UK, Adeyeye MC. Gastroretentive floating drug-delivery systems: A critical review. Crit Rev Ther Drug Carrier Syst 2011;28:47-99.
48. Singh BN, Kim KH. Floating drug delivery systems: An approach to oral controlled drug delivery via gastric retention. J Control Release 2000;63:235-59.
49. Clarke GM, Newton JM, Short MB. Comparative gastrointestinal transit of pellet systems of varying density. Int J Pharm 1995;114:1-11.
50. Whitehead L, Fell JT, Collett JH, Sharma HL, Smith AM. Floating dosage forms: An in vivo study demonstrating prolonged gastric retention. J Control Release 1998;55:3-12.
51. Rouge N, Buri P, Doelker E. Drug absorption sites in the gastrointestinal tract and dosage forms for site-specific delivery. Int J Pharm 1996;136:117-39.
52. Sato Y, Kawashima Y, Takeuchi H, Yamamoto H. Physicochemical properties to determine the buoyancy of hollow microspheres (microballoons) prepared by the emulsion solvent diffusion method. Eur J Pharm Biopharm 2003;55:297-304.
53. Cooreman MP, Krausgrill P, Hengels KJ. Local gastric and serum amoxicillin concentrations after different oral application forms. Antimicrob Agents Chemother 1993;37:1506-9.
54. Gajjar S, Mayavanshi AV. Floating drug delivery to increase gastric retension. J Pharm Educ Res 2008;1:55-61.
55. Krögel I, Bodmeier R. Development of a multifunctional matrix drug delivery system surrounded by an impermeable cylinder. J Control Release 1999;61:43-50.
56. Gröning R, Cloer C, Georgarakis M, Müller RS. Compressed collagen sponges as gastroretentive dosage forms: In vitro and in vivo studies. Eur J Pharm Sci 2007;30:1-6.
57. Sriamornsak P, Thirawong N, Puttipipatkhachorn S. Emulsion gel beads of calcium pectinate capable of floating on the gastric fluid: Effect of some additives, hardening agent or coating on release behavior of metronidazole. Eur J Pharm Sci 2005;24:363-73.
58. Streubel A, Siepmann J, Bodmeier R. Floating microparticles based on low density foam powder. Int J Pharm 2002;241:279-92.
59. Streubel A, Siepmann J, Bodmeier R. Floating matrix tablets based on low density foam powder: Effects of formulation and processing parameters on drug release. Eur J Pharm Sci 2003;18:37-45.
60. Bechgaard H, Nielsen GH. Controlled-release multiple-units and single-unit doses a literature review. Drug Dev Ind Pharm 1978;4:53-67.
61. Iannuccelli V, Coppi G, Sansone R, Ferolla G. Air compartment multiple-unit system for prolonged gastric residence. Part II. In vivo evaluation. Int J Pharm 1998;174:55-62.
62. Jain SK, Awasthi AM, Jain NK, Agrawal GP. Calcium silicate based microspheres of repaglinide for gastroretentive floating drug delivery: Preparation and in vitro characterization. J Control Release 2005;107:300-9.
63. Talukder R, Fassihi R. Gastroretentive delivery systems: Hollow beads. Drug Dev Ind Pharm 2004;30:405-12.
64. Tripathi J, Thapa P, Maharjan R, Jeong SH. Current state and future perspectives on gastroretentive drug delivery systems. Pharmaceutics 2019;11:1-22.
65. Stockwell AF, Davis SS, Walker SE. In vitro evaluation of alginate gel systems as sustained release drug delivery systems. J Control Release 1986;3:167-75.
66. Ingani HM, Timmermans J, Moës AJ. Conception and in vivo investigation of peroral sustained release floating dosage forms with enhanced gastrointestinal transit. Int J Pharm 1987;35:157-64.
67. Acharya S, Patra S, Pani NR. Optimization of HPMC and carbopol concentrations in non-effervescent floating tablet through factorial design. Carbohydr Polym 2014;102:360-8.
68. Bardonnet PL, Faivre V, Pugh WJ, Piffaretti JC, Falson F. Gastroretentive dosage forms: Overview and special case of Helicobacter pylori. J Control Release 2006;111:1-18.
69. Kawashima Y, Niwa T, Takeuchi H, Hino T, Itoh Y. Hollow microspheres for use as a floating controlled drug delivery system in the stomach. J Pharm Sci 1992;81:135-40.
70. Choi BY, Park HJ, Hwang SJ, Park JB. Preparation of alginate beads for floating drug delivery system: Effects of CO2 gas-forming agents. Int J Pharm 2002;239:81-91.
71. Park K, Robinson JR. Bioadhesive polymers as platforms for oral-controlled drug delivery: Method to study bioadhesion. Int J Pharm 1984;19:107-27.
72. Lehr CM, Bouwstra JA, Tukker JJ, Junginger HE. Intestinal transit of bioadhesive microspheres in an in situ loop in the rat-a comparative study with copolymers and blends based on poly(acrylic acid). J Control Release 1990;13:51-62.
73. Harris D, Fell JT, Sharma HL, Taylor DC. GI transit of potential bioadhesive formulations in man: A scintigraphic study. J Control Release 1990;12:45-53.
74. Huang Y, Leobandung W, Foss A, Peppas NA. Molecular aspects of muco-and bioadhesion: Tethered structures and site-specific surfaces. J Control Release 2000;65:63-71.
75. Arnold J, Hunkeler D. Gastro retention using polymer cocoons. Artif Cells Nanomedicine Biotechnol 2015;43:26-32.
76. Torrado S, Prada P, De La Torre PM, Torrado S. Chitosan-poly(acrylic) acid polyionic complex: In vivo study to demonstrate prolonged gastric retention. Biomaterials 2004;25:917-23.
77. Chen J, Park K. Synthesis and characterization of superporous hydrogel composites. J Control Release 2000;65:73-82.
78. Abouelatta SM, Aboelwafa AA, El-Gazayerly ON. Gastroretentive raft liquid delivery system as a new approach to release extension for carrier-mediated drug. Drug Deliv 2018;25:1161-74.
79. Hampson FC, Jolliffe IG, Bakhtyari A, Taylor G, Sykes J, Johnstone LM, et al. Alginate-antacid combinations: Raft formation and gastric retention studies. Drug Dev Ind Pharm 2010;36:614-23.
80. Abou Youssef NA, Kassem AA, El-Massik MA, Boraie NA. Development of gastroretentive metronidazole floating raft system for targeting Helicobacter pylori. Int J Pharm 2015;486:297-305.
81. Gröning R, Berntgen M, Georgarakis M. Acyclovir serum concentrations following peroral administration of magnetic depot tablets and the influence of extracorporal magnets to control gastrointestinal transit. Eur J Pharm Biopharm 1998;46:285-91.
82. Phuapradit W, Bolton S. The influence of tablet density on the human oral absorption of sustained release acetaminophen matrix tablets. Drug Dev Ind Pharma 1991;17:1097-107.
83. Nur AO, Zhang JS. Captopril floating and/or bioadhesive tablets: Design and release kinetics. Drug Dev Ind Pharm 2000;26:965-9.
84. Ichikawa M, Watanabe S, Miyake Y. A new multiple-unit oral floating dosage system. I: Preparation and in vitro evaluation of floating and sustained-release characteristics. J Pharm Sci 1991;80:1062-66.
85. Gangadharappa HV, Rahamath-Ulla M, Pramod-Kumar TM, Shakeel F. Floating drug delivery system of verapamil hydrochloride using karaya gum and HPMC. Clin Res Regul Aff 2010;27:13-20.
86. Garg R, Gupta G. Preparation and evaluation of gastroretentive floating tablets of acyclovir. Curr Drug Deliv 2009;6:437-43.
87. Hilton AK, Deasy PB. In vitro and in vivo evaluation of an oral sustained-release floating dosage form of amoxycillin trihydrate. Int J Pharm 1992;86:79-88.
88. Chen RN, Ho HO, Yu CY, Sheu MT. Development of swelling/ floating gastroretentive drug delivery system based on a combination of hydroxyethyl cellulose and sodium carboxymethyl cellulose for losartan and its clinical relevance in healthy volunteers with CYP2C9 polymorphism. Eur J Pharm Sci 2010;39:82-9.
89. Menon A, Ritschel WA, Sakr A. Development and evaluation of a monolithic floating dosage form for furosemide. J Pharm Sci 1994;83:239-45.
90. Thanoo BC, Sunny MC, Jayakrishnan A. Oral sustained-release drug delivery systems using polycarbonate microspheres capable of floating on the gastric fluid. J Pharm Pharmacol 1993;45:21-4.
91. Jain AK, Jain CP, Tanwar YS, Naruka PS. Formulation, characterization and in vitro evaluation of floating microspheres of famotidine as a gastro retentive dosage form. Asian J Pharm 2009;3:222-6.
92. Ramachandran S, Shaheedha S, Thirumurugan G, Dhanaraju M. Floating controlled drug delivery system of famotidine loaded hollow microspheres (microballoons) in the stomach. Curr Drug Deliv 2010;7:93-7.
93. Miyazaki S, Yamaguchi H, Yokouchi C, Takada M, Hou WM. Sustained-release and intragastric-floating granules of indomethacin using chitosan in rabbits. Chem Pharm Bull 1988;36:4033-8.
94. Pawar VK, Kansal S, Asthana S, Chourasia MK. Industrial perspective of gastroretentive drug delivery systems: Physicochemical, biopharmaceutical, technological and regulatory consideration. Expert Opin Drug Deliv 2012;9:551-65.
16 Views | 50 Downloads
How to Cite
J BHANDWALKAR, M., P. S DUBAL, A. K.TUPE, and S. N MANDRUPKAR. “REVIEW ON GASTRORETENTIVE DRUG DELIVERY SYSTEM”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 13, no. 12, Dec. 2020, pp. 38-45, doi:10.22159/ajpcr.2020.v13i12.37264.
Review Article(s)