GASTRORETENTIVE EFFERVESCENT FLOATING TABLETS (GREFT) OF DRUGS ACTING ON CARDIOVASCULAR DISEASES
DOI:
https://doi.org/10.22159/ijpps.2024v16i7.51296Keywords:
Bilayer tablet, Buoyancy, Cardiovascular diseases (CVDs), Effervescent floating, Floating lag time, Gastro retentive drug delivery systems (GRDDS), Gums, Hydroxypropylmethyl cellulose, Multi-particulate, etcAbstract
Incidences of Cardio Vascular Diseases (CVDs) are increasing in an alarming proportion in India. Conventional oral dosage forms cannot be retained in the stomach for long owing to gastric emptying. Moreover, drugs which are commonly employed in management of chronic CVDs either have reduced solubility at alkaline pH, undergo colonic degradation, exhibit site-specific absorption or varying bioavailability with combination therapy. Gastro-retentive drug delivery systems (GRDDS) are designed to overcome these challenges. Since 2006, Food and Drug Administration has approved only few GRDDS for treating CVDs. The aim of the present review is to summarize the outcomes of research carried on GRRDS with drugs for CVDs since last 15 y and comprehensive analysis of limitations of such studies due to which no product has been approved or commercialized in over last 18 y. Literature survey includes single unit, multi-particulate, monolayer and bilayer dosage forms with or without effervescence-inducing agents and made of natural and/or synthetic polymers like hydroxypropylmethyl cellulose, natural gums etc. Efforts have been made to compile in vitro buoyancy data such as floating lag time, total floating time, swelling index, release profile and release kinetics. Among various studies reported on monolayer and bilayer Gastro-Retentive Effervescent Floating Tablets, only 3 involved bioavailability studies in human volunteers. Toxicity studies in animals or stability studies are totally lacking. Observation with floating-type multi-particulate GRDDS is more disappointing. lack of safety, efficacy data, stability data, in vivo imaging studies and in vitro-in vivo correlation data might be actually responsible for lack of commercialization of any GRDDS for drugs acting on CVDs in 21st century.
Downloads
References
Prabhakaran D, Jeemon P, Roy A. Cardiovascular diseases in India: current epidemiology and future directions. Circulation. 2016;133(16):1605-20. doi: 10.1161/CIRCULATIONAHA.114.008729, PMID 27142605.
Vasan SK, Antonisamy B, Gowri M, Selliah HY, Geethanjali FS, Jebasingh FS. Prevalence, incidence and predictors of cardiovascular risk factors: longitudinal data from rural and urban South India and comparison with global data. BMJ Open Diabetes Res Care. 2020;8(1):1-9. doi: 10.1136/bmjdrc-2020-001782, PMID 33093130.
Ram S, Chandra R, Kundu A, Singh A, Singh S, Tanti A. Prevalence and determinants of self-reported heart disease among Indian men aged 15-54 y: evidence from NFHS-5. Clin Epidemiol Glob Health. 2023;23:1-8. doi: 10.1016/j.cegh.2023.101374.
Kundu J, Kundu S. Cardiovascular disease (CVD) and its associated risk factors among older adults in India: evidence from lasi wave. Clin Epidemiol Glob Health. 2022;13:1-5. doi: 10.1016/j.cegh.2021.100937.
Kalra A, Jose AP, Prabhakaran P, Kumar A, Agrawal A, Roy A. The burgeoning cardiovascular disease epidemic in Indians- perspectives on contextual factors and potential solutions. Lancet Reg Health Southeast Asia. 2023;12:100156. doi: 10.1016/j.lansea.2023.100156, PMID 37384064.
Muharram FR, Multazam CE, Mustofa A, Socha W, Andrianto MS, Martini S. The 30 years of shifting in the Indonesian cardiovascular burden-analysis of the global burden of disease study. J Epidemiol Glob Health. 2024;14(1):193-212. doi: 10.1007/s44197-024-00187-8, PMID 38324147.
Kundu J, James KS, Hossain B, Chakraborty R. Gender differences in premature mortality for cardiovascular disease in India, 2017-18. BMC Public Health. 2023;23(1):547. doi: 10.1186/s12889-023-15454-9, PMID 36949397.
Rehman S, Rehman E, Ikram M, Jianglin Z. Cardiovascular disease (CVD): assessment, prediction and policy implications. BMC Public Health. 2021;21(1):1299. doi: 10.1186/s12889-021-11334-2, PMID 34215234.
Porwal A, Dwivedi H, Pathak K. Decades of research in drug targeting using gastroretentive drug delivery systems for antihypertensive therapy. Braz J Pharm Sci. 2017;53(3):1-15. doi: 10.1590/s2175-97902017000300173.
Kumar M, Kaushik D. An overview on various approaches and recent patents on gastroretentive drug delivery systems. Recent Pat Drug Deliv Formul. 2018;12(2):84-92. doi: 10.2174/1872211312666180308150218, PMID 29521255.
Aslam R, Mehmood Y, Khan S, Yousaf H. Techniques and polymers used to design gastroretentive drug delivery systems-a review. World J Pharm Pharm Sci. 2014;12(3):97-110.
Mandal UK, Chatterjee B, Senjoti FG. Gastro-retentive drug delivery systems and their in vivo success: a recent update. Asian J Pharm Sci. 2016;9:575-84. doi: 10.1016/j.ajps.2016.04.007.
Ainurofi A, Daryati A, Murtadla FA, Salimah F, Akbar NM, Faizun RA. The use of natural and synthetic polymers in the formulation of gastroretentive drug delivery system. Int J Drug Deliv Technol. 2023;13(1):434-41. doi: 10.25258/ijddt.13.1.69.
https://www.accessdata.fda.gov/drugsatfda_docs/nda/ [Last accessed on 24 Feb 2024]
Nayak AK, Maji R, Das B. Gastroretentive drug delivery systems: a review. Asian J Pharm Res. 2010;3(1):2-10.
Badoni A, Ojha A, Gnanarajan G, Kothiyal P. Review on gastro retentive drug delivery system. J Pharm Innov. 2012;1(8):32-42.
Shinde S, Tadwee I, Shahi S. Gastro retentive drug delivery system: a review. Int J Pharm Res Allied Sci. 2011;1(1):1-13.
Pal R, Pandey P, Nogai L, Arushi A, Anand A, Suthar P. The future perspectives and novel approach on gastro retentive drug delivery system (grdds) with currrent state. J Popul Ther Clin Pharmacol. 2023;30(17):594-613. doi: 10.53555/jptcp.v30i17.2852.
Chandrakar S, Yadav C, Roy A, Gupta PP, Vaiswade R, Verma A. Gastro-retentive drug delivery system of antihypertensive drug. Eur J Pharm Sci. 2020;7(12):92-9.
Chawra HS, Tanwar YS, Gilhotra RM, Singh SK. Gastroretentive drug delivery systems a potential approach for antihypertensive drugs: an updated review. APJHS. 2018;5(2):217-23. doi: 10.21276/apjhs.2018.5.2.40.
Srikanth MV, Ram BJ, Sunil SA, Rao NS, Vandana KR. Gastroretentive drug delivery systems: novel approaches and its evaluation: a review. Int J Pharm Sci Rev Res. 2011;10:203-16.
Hoffman A, Stepensky D, lavy E, Eyal S, Klausner E, Friedman M. Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms. Int J Pharm. 2004;277(1-2):141-53. doi: 10.1016/j.ijpharm.2003.09.047, PMID 15158977.
Mohapatra PK, Satyavani CH, Sahoo S. The design and development of carvedilol gastroretentive floating drug delivery systems using hydrophilic polymers and in vitro characterization. Int J Pharm Pharm Sci. 2020;12(7):66-73. doi: 10.22159/ijpps.2020v12i7.38024.
Garg R, Gupta GD. Progress in controlled gastroretentive delivery systems. Trop J Pharm Res. 2008;7(3):1055-66. doi: 10.4314/tjpr.v7i3.14691.
Nasa P, Mahant S, Sharma D. Floating systems: a novel approach towards gastroretentive drug delivery systems. Int J Pharm Pharm Sci. 2010;2(3):2-7.
Talukder R, Fassihi R. Gastroretentive delivery systems: a mini review. Drug Dev Ind Pharm. 2004;30(10):1019-28. doi: 10.1081/ddc-200040239, PMID 15595568.
Suradkar P, Mishra R, Nandgude T. Overview on trends in development of gastroretentive drug delivery system. Res J Pharm Technol. 2019;12(11):5633-40. doi: 10.5958/0974-360X.2019.00975.2.
Gugulothu D, Choudhary SK. Design and in vitro evaluation of floating drug delivery system of glipizide using combination of natural mucilages and synthetic polymers. Int J Pharm Pharm Sci. 2021;13(7):40-8. doi: 10.22159/ijpps.2021v13i7.41644.
Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery systems. Expert Opin Drug Deliv. 2006;3(2):217-33. doi: 10.1517/17425247.3.2.217, PMID 16506949.
Sawanny R, Sharma A, Jain S, Mukherjee S, Khamkat P. Gastro retentive drug delivery system: latest approach towards novel drug delivery. Res J Pharm Technol. 2023;16(1):453-8. doi: 10.52711/0974-360X.2023.00077.
Landge P, Lavande J, Swami A, Dharashive V. A review on gastroretentive drug delivery system. RJPDFT. 2023:62-8. doi: 10.52711/0975-4377.2023.00011.
Raza M, Jayswal MG, Ahmed DA, Aejazuddin QM, Khan JG. Review on gastro retentive drug delivery system. World J Pharm Pharm Sci. 2022;11(9):624-40. doi: 10.20959/wjpps20229-23130.
Sourav M. Buccoadhesive drug delivery system-a review. WJPPS. 2017:378-403. doi: 10.20959/wjpps20174-8863.
Patil H, Tiwari RV, Repka MA. Recent advancements in mucoadhesive floating drug delivery systems: a mini-review. J Drug Deliv Sci Technol. 2016;31:65-71. doi: 10.1016/j.jddst.2015.12.002.
Pund AU, Shendge RS, Pote AK. Current approaches on gastroretentive drug delivery systems. J Drug Delivery Ther 2019;10(1):139-46. doi: 10.22270/jddt.v10i1.3803.
Niranjanbhai BD, Mahendrakumar VN, Surendran CS, Shah VH, Upadhyay UM. Advances in GRDDS: raft forming system: a review. J Drug Deliv Ther. 2012;2(5):123-8. doi: 10.22270/jddt.v2i5.228.
Mali AD, Bathe RS. Design and optimization of gastroretentive floating matrix tablets of an antihypertensive drug quinapril HCl. Int J Pharm Technol. 2015;7(2):9212-24.
More S, Gavali K, Doke O, Kasgawade P. Gastroretentive drug delivery system. J Drug Delivery Ther. 2018;8(4):24-5. doi: 10.22270/jddt.v8i4.1788.
Vinchurkar K, Sainy J, Khan MA, Mane S, Mishra DK, Dixit P. Features and facts of a gastroretentive drug delivery system-a review. Turk J Pharm Sci. 2022;19(4):476-87. doi: 10.4274/tjps.galenos.2021.44959, PMID 36047602.
J Bhandwalkar M, S Dubal P, K Tupe A, N Mandrupkar S. Review on gastroretentive drug delivery system. Asian J Pharm Clin Res. 2020;13:38-45. doi: 10.22159/ajpcr.2020.v13i12.37264.
Abraham S, Naufal M, Peter V, Raju S, Das C. Formulation and evaluation of gastro-retentive drug delivery system containing combination of glipizide and metformin hydrochloride. Asian J Pharm Clin Res. 2016;9(16):235-40. doi: 10.22159/ajpcr.2016.v9i6.14286.
CK, Seth N, Gill NS. Gastro retentive drug delivery system: a significant tool to increase the gastric residence time of drugs. Int J Curr Pharm Sci. 2021;13(1):7-11. doi: 10.22159/ijcpr.2021v13i1.40818.
Juweriya A, Ratnamala KV. Formulation and evaluation of sintered gastroretentive tablets of vildagliptin using design of experiment. Asian J Pharm Clin Res. 2023;16(6):46-52. doi: 10.22159/ajpcr.2023.v16i6.47150.
Pilaka SR, Addagala A, Srighakopalu V, Vegesna SP, Nekkalapu US, Vadapalli RR. Formulation and in vitro evaluation of enalapril maleate gastroretentive effervescent floating tablets with the combination of natural and synthetic polymers. Int J Chem Biol Sci. 2022;11(1):2286-97. doi: 10.21746/ijcls.2022.11.1.3.
Thulluru A, Basha SS, Singh UN, Jayasree T. Effect of combination of natural and synthetic polymers on the formulation of nifedipine gastroretentive floating tablets. Ind J Sci. 2022;13(73):45663-74.
Martha S. Development and in vitro evaluation of perindopril floating tablet. World J Pharm Res. 2015;4(4):1010-21.
Priya D, Padmapreetha J, Indrapriyadharshini C, Kumar P. Development and evaluation of gastroretentive floating tablets of atorvastatin calcium. World J Pharm Res. 2022;11(10):747-61. doi: 10.20959/wjpr202210-24511.
Karemore MN, Bali NR. Gellan gum based gastroretentive tablets for bioavailability enhancement of cilnidipine in human volunteers. Int J Biol Macromol. 2021;174:424-39. doi: 10.1016/j.ijbiomac.2021.01.199, PMID 33539955.
Jagdale SC, Agavekar AJ, Pandya SV, Kuchekar BS, Chabukswar AR. Formulation and evaluation of gastroretentive drug delivery system of propranolol hydrochloride. AAPS PharmSciTech. 2009;10(3):1071-9. doi: 10.1208/s12249-009-9300-8, PMID 19672719.
Saravanakumar K, Thulluru A, Samineni R, Ishwarya M, Nagaveni P, Mahammed N. Effect of sodium alginate in combination with natural and synthetic polymers on the release of verapamil HCl from its floating microspheres. J Pharm Sci Res. 2019;11(5):2028-35.
Srinivas L, Sagar S. Design, optimization, and evaluation of raft forming gastro retentive drug delivery system of lafutidine using box–behnken design. Int J App Pharm. 2022;14(1):266-74. doi: 10.22159/ijap.2022v14i1.43358.
Raza SN, Khan NA. Various formulation variables effecting floatation behaviour of single unit gastroretentive capsules of ofloxacin. Int J Pharm Pharm Sci. 2016;9(1):213-17. doi: 10.22159/ijpps.2017v9i1.13962.
Sundar WA, Vijayaragavan C, Purohit D. Formulation and evaluation of floating matrix tablets of clarithromycin using different grades of HPMC. Int J Pharm Pharm Sci. 2013;5(3):174-6.
Shankar KR, Aminabee S, lakshmi KC, Reddy GR, Shaik R, Tiyagura V. Effect of various sustained release polymers on floating tablets of carvedilol phosphate-a comparative study. Int J App Pharm. 2023;15(6):125-31. doi: 10.22159/ijap.2023v15i6.49170.
Kumar Goyal M, Dubey A, Kumar Yadav L. Formulation and evaluation of gastroretentive drug delivery system of telmisartan. Pharm Meth 2015;6(2):67-71. doi: 10.5530/phm.2015.6.9.
Pandiya H, Sharma CS. Development and characterization of gastroretentive drug delivery system of hydrochlorothiazide. Ann Rom Soc Cell Biol. 2021;25(3):5435-58.
Gaikwad SS, Avari JG. Improved bioavailability of Azelnidipine gastro retentive tablets-optimization and in vivo assessment. Mater Sci Eng C Mater Biol Appl. 2019;103:109800. doi: 10.1016/j.msec.2019.109800, PMID 31349458.
Wang S, Wen H, Li P, Cui M, Sun W, Wang H. Formulation and evaluation of gastric-floating controlled release tablets of Ginkgolides. J Drug Deliv Sci Technol. 2019;51:7-17. doi: 10.1016/j.jddst.2019.02.011.
Sanjana A, Ahmed MG. Development and in vitro evaluation of rosuvastatin tablets by floating drug delivery system. Asian J Pharm. 2017;11(2):1-5. doi: 10.22377/ajp.v11i02.1262.
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. 2010j;39(1-3):82-9. doi: 10.1016/j.ejps.2009.10.015, PMID 19903527.
Parveen MD, Wajid SK, Jat RK. Formulation and in vitro, in vivo evaluation of floating bi layer tablets of ezetimibe-nateglinide. Nat Volatiles Essent Oils. 2021;8(4):16586-606.
Porwal A, Dwivedi H, Pathak K. Gastroretentive bilayer film for sustained release of atorvastatin calcium and immediate release of amlodipine besylate: pharmaceutical, pharmacokinetic evaluation, and IVIVC. Pharm Dev Technol. 2020;25(4):416-31. doi: 10.1080/10837450.2019.1705486, PMID 31852330.
Charyulu NR, Bera D, Sakhia D, Manavadaria K, Shetty NG. Formulation and evaluation of bilayer floating tablets of diltiazem hydrochloride for bimodal release. Int Res Pharm Sci. 2012;3(2):301-6.
Leno Jenita J, Ramu MA, Sah P, Rathore SS. Optimization of parameters for the design and evaluation of fenofibrate loaded floating microspheres by taguchi method. JRP. 2023;27(1):130-45. doi: 10.29228/jrp.298.
Cheng HF, Feng Y, Duan QJ, Jiang DM, Tao KY. Floating microparticulate oral diltiazem hydrochloride delivery system for improved delivery to heart. Trop J Pharm Res. 2015;14(6):935-40. doi: 10.4314/tjpr.v14i6.1.
Garse H, Vij M, Yamgar M, Kadam V, Hirlekar R. Formulation and evaluation of a gastroretentive dosage form of labetalol hydrochloride. Arch Pharm Res. 2010;33(3):405-10. doi: 10.1007/s12272-010-0309-z, PMID 20361305.
Published
How to Cite
Issue
Section
Copyright (c) 2024 SUTAPA BISWAS MAJEE, TRISHA MISHRA, SOUVIK GUPTI
This work is licensed under a Creative Commons Attribution 4.0 International License.