A Recent Update on Formulation and Development of Gastro-Retentive Drug Delivery Systems

DOI:

https://doi.org/10.37285/ijpsn.2021.14.1.1

Authors

  • Abhishek Kumar
  • Meenakshi Bharkatiya

Abstract

Oral route has been the most convenient and accepted  route of drug delivery. Owing to tremendous curative  benefits of the oral controlled release dosage forms are  being preferred as the interesting topic in pharmaceutical  field to achieved improved therapeutics advantages.  Gastro retentive drug delivery system is novel drug  delivery systems which has an upper hand owing to its  ability of prolonged retaining ability in the stomach and  thereby increase gastric residence time of drugs and also  improves bioavailability of drugs. Concept of novel drug  delivery system arose to overcome the certain aspect  related to physicochemical properties of drug molecule  and the related formulations. In this context, various  gastro retentive drug delivery systems have been used to  improve the therapeutic efficacy of drugs that have a  narrow absorption window, are unstable at alkaline pH,  are soluble in acidic conditions, and are active locally in  the stomach. Concept of novel drug delivery system  arose to overcome the certain aspect related to  physicochemical properties of drug molecule and the  related formulations. Various approaches are currently  used including gastro retentive floating drug delivery  systems, swelling and expanding system, polymeric bio  adhesive systems, modified shape systems, high density  system and other delayed gastric emptying devices.  Moreover, future perspectives on this technology are  discussed to minimize the gastric emptying rate in both  the fasted and fed states. The present review briefly  addresses the physiology of the gastric emptying  process with respect to floating drug delivery systems.  The purpose of this review is to bring together the recent  literature with respect to the method of preparation, and  various parameters affecting the performance and  characterization of floating microspheres. Attempt has  been made to summarize important factors controlling  gastro retentive drug delivery systems. Overall, this  review may inform and guide formulation scientists in  designing the gastro retentive drug delivery system.

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Keywords:

Gastro retentive system, gastric residence time, bioavailability, narrow absorption window, polymeric bio adhesive systems, delayed gastric emptying devices

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Published

2021-01-01

How to Cite

1.
Kumar A, Bharkatiya M. A Recent Update on Formulation and Development of Gastro-Retentive Drug Delivery Systems. Scopus Indexed [Internet]. 2021 Jan. 1 [cited 2024 Apr. 29];14(1):5257-70. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/1270

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Review Articles

References

Abduljabbar NH, Badr-Eldin MS and Aldawsari MH (2015). Gastroretentive ranitidine hydrochloride tablets with combined floating and bioadhesive properties: Factorial design analysis, in vitro evaluation and in vivo abdominal X-ray imaging. Curr. Drug Deliv. 12: 578–590.

Adibkia K, Hamedeyazdan S and Javadzadeh Y (2011). Drug Release Kinetics and Physicochemical Characteristics of Floating Drug Delivery Systems. Expert Opin Drug Deliv 8(7): 891-903.

Airemwen, CO and Uhumwangho, MU (2016). Formulation and evaluation of floating matrix tablets of metformin using acrylate methacrylate copolymer and Irvingia gabonesis gum. JOPHAS 13(1): 2331 –2343.

Ali J, Arora S, Ahuja A, Babbar Ak, Sharma Rk and Khar Rk (2007). Formulation and Development of Hydrodynamically Balanced System for Metformin: In Vitro and In Vivo Evaluation. Eur J Pharm Biopharm 67(1): 196-201.

Amit Kumar Nayak, Jadupati Malakar and Kalyan Kumar Sen (2010). Gastroretentive drug delivery technologies: Current approaches and future potential. J Pharm Educ Res, 1(2): 1-10.

Amul mishra and Pinky gupta (2012). Gastro Retentive Drug Delivery System: A Review. Int. J. Drug Dev. Res. 4: 28-39. Anand S and Surana (2010). An overview on various approaches to Oral controlled drug delivery system via gastroretention, Int J Pharm Sci Rev Res., 2: 68-72.

Archana DK and Anil VC (2013). Recent advancement in gastro retentive drug delivery system – a review. Indo Am. j. pharm.. 3(7). 5221-32.

Arora S, Ali J, Ahuja A, Khar RK and Baboota S (2005). Floating Drug Delivery Systems: A Review. AAPS PharmSciTech, 6(3): E372-E90.

Badwan AA, Abumalooh A, Sallam E, Abukalaf A and Jawan O (1985). A sustained release drug delivery system using calcium alginate beads. Drug Dev Ind Pharm 11: 239‐256.

Bansal H, Kaur SP and Gupta AK (2011). Microspheres: methods of preparation and applications: A comparative study. Int J Pharm Sci Rev Res 10: 69‑78.

Bardonnet PL, Faivre V, Pugh WJ, Piffaretti JC and Falson F. (2006). Gastroretentive Dosage Forms: Overview and Special Case of Helicobacter Pylori. J Cont Rel 111(1-2): 1-18.

Baumgartner S, Kristl J, Vreˇcer F, Vodopivec P and Zorko, B (2000). Optimization of floating matrix tablets and evaluation of their gastric residence time. Int. J. Pharm 195: 125–135.

Catarina PR, Neufeld RJ, Ribeiro AJ and Veiga F (2006). Nanoencapsulation. Methods for preparation of drug-loaded polymeric nanoparticles, Nanomedicine: NBM 2: 8- 21.

Cedillo Ramirez E, Villafuerte Robles L and Hernandez Leon A (2006). Effect of Added Pharmatose DCL11 on the Sustained Release of Metronidazole from Methocel K4M and Carbopol 971P NF Floating Matrices. Drug Dev Ind Pharm 32(8): 955-65.

Chawla G and Bansal A (2003). A means to address regional variability in intestinal drug absorption. Pharm Tech 27(2): 50-68.

Chawla G, Gupta P, Koradia V and Bansal AK (2003). Gastroretention a Means to Address Regional Variability in Intestinal Drug Absorption. Pharm Technol, 7:52-68.

Choi B, Park H, Hwang S and Park J (2002). Preparation of alginate beads for floating drug delivery system: Effects of CO2 gas forming agents. Int. J. Pharm 239: 81–91.

Choy YB, Patel SR, Park JH, McCarey BE, Edelhauser HF, Mark R and Prausnitz MR (2011). Mucoadhesive microparticles in a rapidly dissolving tablet for sustained drug delivery to the eye. Invest. Ophthalmol. Vis. Sci. 52(5): 2627–2633.

Clarke G, Newton J and Short M (1993). Gastrointestinal transit of pellets of dyeing size and density. Int. J. Pharm. 100: 81–92. Despande AA and Shah NH (1987). Development of a Novel control release system for gastric retention. Pharm.Res. 14: 815-818. Dettmar PW, Dickson PA, Hampson FC, Jollife IG and Peers W

(2001). Mucoadhesive granules of carbomer suitable for oral administration of drugs. US Patent 6306789.

Devkant Sharma and Anjali Sharma (2014). Gastroretentive Drug Delivery System - a mini review. Asian Pac. J. Health Sci. 1(2): 80-89.

Dheeraj TB and Dinesh K (2012). Jain a textbook of “Novel Drug Delivery System” published by Nirali Prakashan, 1st ed. July, 11: 1-11.7

Dheeraj TB and Dinesh KJ (2012). Novel Drug Delivery System, 1st ed. july, published by Nirali prakashan, 11: 1-11.7.

Fabregas J, Claramunt J, Cucala J, Pous R and Siles A (1994). “In Vitro” Testing of an Antacid Formulation with Prolonged Gastric Residence Time (Almagate Flot-Coatfi). Drug Dev. Ind. Pharm. 20: 1199–1212.

Feldman M and Barnett C (1991). Fasting gastric pH and its relationship to true hypochlorhydria in humans. Dig. Dis. Sci. 36: 866–869.

Flake MM, Nguyen PK, Scott RA, Vandiver LR, Willits RK and Elbert DL (2011). Poly (ethylene glycol) microparticles produced by precipitation polymerization in aqueous solution. Biomacromolecules 12(3): 844–850.

Ganguly S and Dash AK (2004). A novel in situ gel for sustained drug delivery and targeting. Int J Pharm. 276(1-2): 83-92. Garg R and Gupta G (2008). Progress in controlled gastro retentive delivery systems. Trop. J. Pharm. Res 7: 1055–1066. Gaur PK, Mishra S, Bhardwaj S, Puri D and Kumar SS (2014). Ion Exchange Resins in Gastroretentive Drug Delivery: Characteristics, Selection, Formulation and Applications. J. Pharm. Sci. Pharmacol 1: 304–312.

Giovagnoli S, Blasi P, Ricci M and Rossi C (2004). Biodegradable microspheres as carriers for native superoxide dismutase and catalase delivery. AAPS Pharm Sci Tech. https ://doi.org/10.1208/pt050 451

Giunchedi P, Gavini E, Moretti MDL and Pirisino G (2000). Evaluation of alginate compressed matrices as prolonged drug delivery systems. AAPS Pharm Sci Tech 1: article19.

Guan J, Zhou L, Nie S, Yan T, Tang X and Pan W (2010). A Novel Gastric- Resident Osmotic Pump Tablet: In Vitro and In Vivo Evaluation. Int J Pharm 383(1-2): 30-6.

Guerrero S, Teijón C, Muñiz E, Teijón JM and Blanco MD (2010). Characterization and in vivo evaluation of ketotifen‑loaded chitosan microspheres. Carbohydr Polym 79: 1006‑13.

Gupta R, Tripathi P and Bhardwaj P (2008). Recent advances in gastro retentive drug delivery systems and its application on treatment of H. Pylori infections. J Anal Pharm Res., 7(4), 404- 410.

Hafeez A, Maurya A, Singh J, Mittal A and Rana L (2013). An overview on floating microsphere: Gastro Retention Floating drug delivery system (FDDS). J Phytopharmacol 2(3): 1-12

Halder A and Mukherjee (2005). Development and evaluation of polyethyleneimine treated calcium alginate beads for sustained release of diltiazem. J Microencapsul 22: 67‐80.

Hardenia SS, Jain A, Patel R and Kaushal A (2011). Floating drug delivery systems: a review. Asian J. Pharm 1(3): 284–93. Hoffman AA and Qadri BA (2006). Encyclopedia of Pharmaceutical Technology. 02 Oct. DOI: 10.1081/E-EPT-120041584. Huanbutta K, Limmatvapirat S, and Sungthongjeen S (2016). Novel Strategy to Fabricate Floating Drug Delivery System based on Submlimation Technique. AAPS Pharm Sci Tech. 17(2): 693-698. Iannuccelli V, oppi G, Sansone R and Ferolla G (1998). Air compartment Multipleunit System for Prolonged Gastric Residence, Part II. In-vivo Evaluation. Int. J. Pharma. 174 (1–2): 55–62.

Ito R, Machida Y, Sannan T and Nagai T (1990). Magnetic granules: A novel system for specific drug delivery to esophageal mucosa in oral administration. Int. J. Pharm. 61: 109–117.

Jain NK (2014). Progress in Controlled And Novel Drug Delivery System. New Delhi, CBS Publisher and Distributor. 1st ed. 76- 97.

Jain NK (2014). Progress in Controlled And Novel Drug Delivery System. New Delhi, CBS Publisher and Distributor. 1st ed. 84- 85.

Jalil R and Nixon JR (1990). Biodegradable poly (lactic acid) and poly (lactide-co-glycolide) microcapsules: problems associated with preparative techniques and release properties. J Microencapsul 7: 297–325.

Jamil F, Sunil K, Sharma S, Vishvakarma P and Singh L (2011). Review on Stomach Specific Drug Delivery Development and Evaluation IJRPBS, 2(4), 1427- 1433.

Jimenez-Castellanos NR, Zia H and Rhodes CT (1993). Mucoadhesive Drug Delivery Systems. Drug Deve. and Ind. Pharma. 19: 143-147.

Jimenez-Martinez I, Quirino-Barreda T and Villafuerte-Robles L (2008). Sustained Delivery of Captopril from Floating Matrix Tablets. Int J Pharm, 362(1-2): 37-43.

Joshi VK and Jaimini M (2013). Microballons drug delivery system: A review. AJPRD 1(1): 7 –17.

Kawashima Y, Niwa T, Takeuchi H, Hino T and Itoh Y (1992). Hollow microspheres for use as floating controlled drug delivery system in the stomach. J. Pharm. Sci. 81(2): 135-140.

Klausner EA, Lavy E and Friedman M (2003). Expandable gastroretentive dosage forms. J. Control. Release 90: 143–162. Krygowska-Wajs A, Cheshire WP, Wszolek ZK, Hubalewska Dydejczyk A, Jasinska-Myga B, Farrer M.J, Moskala M and Sowa-Staszczak, A (2009). Evaluation of gastric emptying in familial and sporadic Parkinson disease. Parkinsonism Relat. D. 15: 692–696.

Kumar R, Kamboj S, Chandra A, Gautam PK and Sharma VK (2016). Microballoons: An advance avenue for gastroretentive drug delivery system – A review. UK. J. Pharm. Biosci. 4(4): 29- 40.

Li LC and Tian YE (2002). Encyclopedia of Pharmaceutical Technology; James S; James CB. ed. Marcel Dekker Inc. NY. Lopes CM, Bettencourt C, Rossi A, Buttini F and Barata P (2016).

Overview on gastroretentive drug delivery systems for improving drug bioavailability. Int. J. Pharm 510: 144–158. Mandal UK, Chatterjee B and Senjoti FG (2016). Gastro-retentive drug delivery systems and their in vivo success: A recent update. Asian J. Pharm. Sci. 11: 575–584.

Moes (2003). A. Gastric retention systems for oral drug delivery. In Business Briefing: Pharmatech; Business Briefings Ltd.: Singapore, 157–159.

Moes AJ (2003). Gastric Retention Systems for Oral Drug Delivery. Business Briefing, Drug Delivery Oral, Pharmtech. 158-159. Mohamed HGD and Furquan NK (2009). Gastroretentive Drug

Delivery Systems: A Patent Perspective, Int. J. Health Res., 23-44.

Mohammed, Ahmed G, Satish K and Kiran KGB (2010). Formulation and evaluation of Gastric mucoadhesive drug delivery systems of captopril. J. Curr. Pharm. Res. 2(1): 26–32.

Moinard-Chécot D, Chevalier Y, Briançon S, Beney L and Fessi H (2008). Mechanism of nanocapsules formation by the emulsion diffusion process. J. Colloid. Interface. Sci 317: 458-468.

Mojaverian P, Vlasses PH, Kellner PE and Rocci ML (1988). Effects of gender, posture, and age on gastric residence time of an indigestible solid: Pharmaceutical considerations. Pharm. Res. 5: 639–644.

Motlekar N (2009). Optimization of experimental parameters for the production of LMWH‑loaded polymeric microspheres. Drug Des Devel Ther 2: 39‑47.

Murata Y, Kofuji K and Kawashima S (2003). Preparation of floating alginate beads for drug delivery to gastric mucosa. J Biomater Sci Polym Ed. 14: 581‐588.

Murata Y, Sasaki N, Miyamoto E and Kawashima S (2000). Use of floating alginate beads for stomach‐specific drug delivery. Eur J Pharm Biopharm 50: 221‐226.

Murphy CS, Pillay V, Choonara, YE and du Toit LC (2009). Gastroretentive drug delivery systems: Current developments in novel system design and evaluation. Curr. Drug Deliv. 6: 451– 460.

Naikwade S and Bajaj A (2009). Preparation and in vitro evaluation of budesonide spray dried microparticles for pulmonary delivery. Sci Pharm 77: 419‑41.

Oliveira BF, Santana MHA and Re MI (2005). Spray dried chitosan microspheres crosslinked with d, l-glutaraldehyde as a potential drug delivery system: preparation and characterization. Braz. J. Chem. Eng. 22(3): 353–360.

Omidian H, Rocca JG and Park K (2005). Advances in superporous hydrogels. J. Control. Release 102: 3–12.

Park K and Robinson JR. (1984). Bioadhesive polymers as platforms for oral-controlled drug delivery: Method to study bioadhesion. Int. J. Pharm. 19: 107–127.

Pawar Vk, Kansal S, Asthana S and Chourasia Mk (2012). Industrial Perspective of Gastroretentive Drug Delivery

Systems: Physicochemical, Biopharmaceutical, Technological and Regulatory Consideration. Expert Opin Drug Deliv 9(5): 551-65.

Pawar Vk, Kansal S, Garg G, Awasthi R, Singodia D and Kulkarni GT (2011). Gastroretentive Dosage Forms: A Review With Special Emphasis on Floating Drug Delivery Systems. Drug Delivery 18(2): 97-110.

Pawar VK, Kansal S, Garg G, Awasthi R, Singodia D and Kulkarni GT (2011). Gastroretentive dosage forms: a review with special emphasis on floating drug delivery systems. Drug Delivery 18(2): 97–110.

Permender Rathee (2011). Gastrointestinal mucoadhesive drug delivery system: A review J. Pharm. Res. 4(5): 1448-1453. Prajapati VD, Jani GK, Khutliwala TA and Zala BS (2013). Raft forming system—An upcoming approach of gastroretentive drug delivery system. J. Control. Release 168: 151–165.

Prasanth VV, Mathew ST, Parthasarathy G, Radhika PR, Pal TK and Siva KT (2009). Formulation and evaluation of sustained release matrix tablets of glipizide. Iran. J. Pharm. Sci. 5(4): 205– 214.

Rahim SA, Carter P and Elkordy AA (2017). Influence of calcium carbonate and sodium carbonate gassing agents on pentoxifylline floating tablets properties. Powder Technol. 322: 65–74.

Ramdas T (2004). Novel Sustained Release Gastroretentive Drug Delivery System: A Review. AJPRD (2)11: 26-41.

Reddy KA, Prathyusha P, Reddy KP, Kumar VN and Prashad NS (2011). Design and evaluation of floating drug delivery systems of cephalexin. J Pharm Biomed Sci 10: 1‑4.

Reddy LHV and Murthy R (2002). Floating dosage systems in drug delivery. Crit. Rev. Ther. Drug 19: 553–585.

Rossi A, Conti C, Colombo G, Castrati L, Scarpignato C, Barata P, Sandri G, Caramella C, Bettini R and Buttini F (2016). Floating modular drug delivery systems with buoyancy independent of release mechanisms to sustain amoxicillin and clarithromycin intra-gastric concentrations. Drug Dev. Ind. Pharm. 42: 332–

Salessiotis N (1972). Measurement of the diameter of the pylorus in man: Part I. Experimental project for clinical application. Am. J. Surg. 124: 331–333.

Saneshan GV and Krishna Kanth VS (2013). Preparation and in vitro evaluation of microballoon drug delivery system of Telmisartan. Int. J. Pharm. Sci. and Drug Res 5(4): 141-145.

Sathish D, Himabindu S, Shravan Kumar Y, Shayeda and Madhusudan Rao Y (2011). Floating Drug Delivery Systems for Prolonging Gastric Residence Time: A Review. Curr Drug Delivery 8(5): 494-510.

Schoubben A, Ricci M and Giovagnoli S (2019). Meeting the unmet: from traditional to cutting-edge techniques for poly lactide and poly lactide-co-glycolide microparticle manufacturing. J Pharm Investig. https ://doi.org/10.1007/s4000 5-019-00446 –y

Sharma and Khan (2014). Gastro retentive drug delivery system: an approach to enhance gastric retention for prolonged drug release. Int. J. Pharm. Sci. Res. 5(4): 1095-1106.

Shiraishi S, Imai T and Otagiri M (1993). Controlled release preparation of indomethacin using calcium alginate gel. Biol Pharm Bull 16: 1164‐1168.

Shiv HG, Vishakante D, Gwdaand T and Pramod M (2004). Floating controlled drug delivery systems for prolong gastric residence. Indian.J.Pharm.Educ. 38(4): 172-179.

Shweta S, Ankush P, Shivpoojan K and Rajat S (2016). PLGA-based nanoparticles: A new paradigm in biomedical applications, Trend. Anal. Chem, 80: 30-40.

Silva CM, Ribeiro AJ, Figueiredo M, Ferreira D and Veiga F (2006). Microencapsulation of hemoglobin in chitosan-coated alginate microspheres prepared by emulsification/internal gelation. AAPSJ 7(4): E903–E913.

Singh BN and Kim KH (2000). Floating Drug Delivery Systems: An Approach to Oral Controlled Drug Delivery via Gastric Retention. J Cont Rel 63(3): 235-59.

Sinha VR, Singla AK, Wadhawan S, Kaushik R, Kumria R, Bansal K and Dhawan S (2004). Chitosan microspheres as a potential carrier for drugs. Int. J. Pharm. 274(1–2): 1–33.

Stops F, Fell JT, Collett JH, Martini LG, Sharma HL and Smith AM (2006). Citric acid prolongs the gastro‐retention of a floating dosage form and increases bioavailability of riboflavin in the fasted state. Int J Pharm 308: 14‐24.

Streubel A, Siepmann J and Bodmeier R (2003). Multiple unit gastroretentive drug delivery systems: a new preparation method for low density microparticles. J Microencapsul 20: 329‐347.

Sultana S, Bhavna, Iqbal Z and Panda BP, Talegaonkar S, Bhatnagar A and Ahmad FJ (2009). Lacidipine encapsulated gastroretentive microspheres prepared by chemical denaturation for pylorospasm. J. Microencapsul. 26(5): 385–393.

Sun R, Lu Y and Chen K (2009). Preparation and characterization of hollow hydroxyapatite microspheres by spray drying method. Mater Sci Eng C 29: 1088‑92.

Sunil K, Faraz J, Meenu R and Saurabh S (2012). Gastro Retentive Drug Delivery System: Features and Facts Int. J. Res. Pharm. Biomed. Sci. 3(1): 125-130.

Swetha S, Allena RT and Gowda DV (2012). A comprehensive review on gastro retentive drug delivery systems. Int. J. Pharm. Biomed. Res.3: 1285-1293.

Talukder R and Fassihi R (2004). Gastroretentive delivery systems: A mini review. Drug Dev. Ind. Pharm. 30: 1019–1028. Timmermans J and Moes AJ (1990). How well floating dosages do forms float? Int. J. Pharm. 62: 207–216.

Tokumitsu H, Ichikawa H, Fukumori Y and Block LH (1999). Preparation of gadopentetic acid-loaded chitosan microparticles for gadolinium neutron-capture therapy of cancer by a novel emulsion-droplet coalescence technique. Chem. Pharm. Bull.

(Tokyo) 47(6): 838–842.

Tonnesen HH and Karlsen J (2002). Alginate in drug delivery systems. Drug Dev Ind Pharm. 28: 621‐630.

Triantafyllou K, Kalantzis C, Papadopoulos A, Apostolopoulos P, Rokkas T, Kalantzis N and Ladas S (2007). Video-capsule endoscopy gastric and small bowel transit time and completeness of the examination in patients with diabetes mellitus. Dig. Liver Dis. 39: 575–580.

Trivedi P, Verma AML and Garud N (2008). Preparation and characterization of aceclofenac microspheres. Asian J. Pharm. 2: 110–115.

Vivek KP, Shaswat K, Shalini A and Chourasia MK (2012). Industrial Perspective of Gastroretentive Drug Delivery Systems: Physiochemical, Biopharmaceutical, Technological and Regulatory Consideration. Expert opinion on drug delivery 9(5): 551-565.

Wang A, Lu Y and Sun R (2007). Recent progress on the fabrication of hollow microspheres. Mater. Sci. Eng. A. 460(1): 1‑6. Wang YT, Mohammed SD, Farmer AD, Wang D, Zarate N and Hobson AR (2015). Regional gastrointestinal transit and pH studied in 215 healthy volunteers using the wireless motility capsule: Influence of age, gender, study country and testing protocol. Aliment. Pharmacol. Ther. 42: 761–772.

Whitehead L, Fell JT and Collett JH (1996). Development of a Gastroretentive Dosage Form. Eur J Pharm Sci. 4(1): S182.