IN VIVO MONITORING STRATEGIES FOR EVALUATION OF FLOATING DRUG DELIVERY SYSTEMS
DOI:
https://doi.org/10.22159/ijap.2022v14i6.45906Keywords:
Gastroretentive technologies, Floating drug delivery systems, Gastric retention, In vivo imaging, Salient advantagesAbstract
In recent years, various advancements have been introduced in the development of controlled drug release devices for resolving different physiological problems for example, gastric retention inconsistency along with erratic gastric emptying time. Gastroretentive delivery formulations receive considerable attention to overcome these drawbacks and in optimizing the absorption of different medicaments. Gastroretentive technologies considerably extend the stomach retention time of dosage forms with increased bioavailability as well as therapeutic efficacy. Gastroretention can be successfully achieved utilizing gastric floating system. The rationale of the present manuscript focuses on current advancements of gastric floating systems so as to accomplish appropriate drug bioavailability and, subsequently drug targeting to the stomach. In vivo evaluation parameters, especially pivotal imaging techniques including roentgenography, gamma scintigraphy, gastroscopy, magnetic marker monitoring, magnetic resonance imaging, ultrasonography, 13C octanoic acid breath test etc. have been emphasized in this manuscript for monitoring drug formulation behavior which extensively revolutionized thorough understanding in the avenue of improved bioavailability of gastroretentive systems.
Downloads
References
Kanupriya C, Nirmata S, Gill NS. Gastro retentive drug delivery system: a significant tool to increase the gastric residence time of drugs. Int J Curr Pharm Res. 2021;13(1):7-11.
Adibkia K, Hamedeyazdan S, Javadzadeh Y. Drug release kinetics and physicochemical characteristics of floating drug delivery systems. Expert Opin Drug Deliv. 2011;8(7):891-903. doi: 10.1517/17425247.2011.574124, PMID 21506906.
Wu Y, Zhang W, Huang J, Luo Z, Li J, Wang L. Mucoadhesive improvement of alginate microspheres as potential gastroretentive delivery carrier by blending with Bletilla striata polysaccharide. Int J Biol Macromol. 2020;156:1191-201. doi: 10.1016/j.ijbiomac.2019.11.156, PMID 31756485.
Prajapati VD, Jani GK, Khutliwala TA, Zala BS. Raft forming system-an upcoming approach of gastroretentive drug delivery system. J Control Release. 2013;168(2):151-65. doi: 10.1016/j.jconrel.2013.02.028, PMID 23500062.
Shashank C, Kumari P, Singh S, Agarwal VK. Approaches to increase the gastric residence time: floating drug delivery system-a review. Asian J Pharm Clin Res. 2013;6(3):1-9.
Schneider F, Koziolek M, Weitschies W. In vitro and in vivo test methods for the evaluation of gastroretentive dosage forms. Pharmaceutics. 2019;11(8):416-45. doi: 10.3390/ pharmaceutics11080416, PMID 31426417.
Kotreka UK, Adeyeye MC. Gastroretentive floating drug-delivery systems: A critical review. Crit Rev Ther Drug Carrier Syst. 2011;28(1):47-99. doi: 10.1615/critrevtherdrugcarriersyst.v28.i1.20. PMID 21395515.
Mohapatra PK, Satayavani CH, Satajit S. Design and development of carvedil of gastroretentive floating drug delivery system using hydrophilic polymers and in vitro characterization. Int J Pharm Pharm Sci. 2020;12(7):66-73.
Pahwa R, Bisht S, Kumar V, Kohli K. Recent advances in gastric floating drug delivery technology: a review. Curr Drug Deliv. 2013;10(3):286-98. doi: 10.2174/1567201811310030005, PMID 23808593.
Pahwa R, Singh M, Kumar V, Kohli K. Recent advances and patent perspectives in gastroretentive technology. Recent Pat Drug Deliv Formul. 2012;6(3):278-90. doi: 10.2174/187221112802652660, PMID 22563754.
Tripathi J, Thapa P, Maharjan R, Jeong SH. Current state and future perspectives on gastroretentive drug delivery systems. Pharmaceutics. 2019;11(4):1-22. doi: 10.3390/ pharmaceutics11040193, PMID 31010054.
Adebisi AO, Conway BR. Modification of drug delivery to improve antibiotic targeting to the stomach. Ther Deliv. 2015;6(6):741-62. doi: 10.4155/tde.15.35, PMID 26149788.
Arora S, Ali J, Ahuja A, Khar RK, Baboota S. Floating drug delivery systems: a review. AAPS PharmSciTech. 2005;6(3):E372-90. doi: 10.1208/pt060347, PMID 16353995.
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.
Pahwa R, Bhardwaj BY, Sharma A, Piplani M, Kumar M. Gastroretentive floating technology for eradication of Helicobacter pylori: an insight view. Int J App Pharm. 2021;13(3):5-10. doi: 10.22159/ijap.2021v13i3.39369.
Shah HP, Prajapati ST, Patel CN. Gastroretentive drug delivery systems: from conception to commercial success. J Crit Rev. 2017;4(2):10-21. doi: 10.22159/jcr.2017v4i2.16717.
Awasthi R, Kulkarni GT. Decades of research in drug targeting to the upper gastrointestinal tract using gastro retention technologies: where do we stand? Drug Deliv. 2016;23(2):378-94. doi: 10.3109/10717544.2014.936535, PMID 25026414.
Singh BN, Kim KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release. 2000;63(3):235-59. doi: 10.1016/S0168-3659(99)00204-7, PMID 10601721.
Nayak V, Somu K, Thomson SR, Bs S. Ceftriaxone-induced periorbital edema. Asian J Pharm Clin Res 2019;12(1). doi: 10.22159/ajpcr.2019.v12i1.25293.
Naseem F, Shah SU, Rashid SA, Farid A, Almehmadi M, Alghamdi S. Metronidazole based floating bioadhesive drug delivery system for potential eradication of H. pylori: preparation and in vitro characterization. Polymers. 2022;14(3):519. doi: 10.3390/polym14030519, PMID 35160508.
Hwang KM, Byun W, Cho CH, Park ES. Preparation and optimization of glyceryl behenate-based highly porous pellets containing cilostazol. Pharm Dev Technol. 2018;23(5):540-51. doi: 10.1080/10837450.2016.1245743, PMID 27718780.
Chen R, Guo X, Liu X, Cui H, Wang R, Han J. Formulation and statistical optimization of gastric floating alginate/oil/chitosan capsules loading procyanidins: in vitro and in vivo evaluations. Int J Biol Macromol. 2018;108:1082-91. doi: 10.1016/j.ijbiomac.2017.11.032, PMID 29128589.
Vasvari G, Haimhoffer A, Horvath L, Budai I, Trencsenyi G, Beresova M. Development and characterization of gastroretentive solid dosage form based on melt foaming. AAPS PharmSciTech. 2019;20(7):290. doi: 10.1208/s12249-019-1500-2, PMID 31428895.
Simons FJ, Wagner KG. Modeling, design and manufacture of innovative floating gastroretentive drug delivery systems based on hot-melt extruded tubes. Eur J Pharm Biopharm. 2019;137:196-208. doi: 10.1016/j.ejpb.2019.02.022, PMID 30826475.
Sopyan I, Sriwidodo, Wahyuningrum R, P NA. A review: floating drug delivery system as a tool to improve dissolution rate in gastric. Int J App Pharm 2020;12(4):51-4. doi: 10.22159/ ijap.2020v12i4.38415.
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.
Sathish D, Himabindu S, Kumar YS, Shayeda MR Y, Rao YM. Floating drug delivery systems for prolonging gastric residence time: a review. Curr Drug Deliv. 2011;8(5):494-510. doi: 10.2174/156720111796642273, PMID 21696354.
Parikh DC, Amin AF. In vitro and in vivo techniques to assess the performance of gastro-retentive drug delivery systems: a review. Expert Opin Drug Deliv. 2008;5(9):951-65. doi: 10.1517/17425247.5.9.951, PMID 18754747.
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(5):575-84. doi: 10.1016/j.ajps.2016.04.007.
Ishak RAH. Buoyancy-generating agents for stomach-specific drug delivery: an overview with special emphasis on floating behavior. J Pharm Pharm Sci. 2015;18(1):77-100. doi: 10.18433/J3602K, PMID 25877444.
Klausner EA, Lavy E, Friedman M, Hoffman A. Expandable gastroretentive dosage forms. J Control Release. 2003;90(2):143-62. doi: 10.1016/S0168-3659(03)00203-7, PMID 12810298.
Pahwa R, Dutt H, Kumar V, Kohli K. Pharmacoscintigraphy: an emerging technique for evaluation of various drug delivery systems. Arch Appl Sci Res. 2010;2(5):92-105.
Wilson CG. In vivo monitoring of dosage forms. J Pharm Pharmacol. 1998;50(4):383-6. doi: 10.1111/j.2042-7158.1998.tb06877.x. PMID 9625482.
Billa N, Yuen KH, Khader MA, Omar A. Gamma-scintigraphic study of the gastrointestinal transit and in vivo dissolution of a controlled release diclofenac sodium formulation in xanthan gum matrices. Int J Pharm. 2000;201(1):109-20. doi: 10.1016/S0378-5173(00)00399-9, PMID 10867269.
Feinle C, Kunz P, Boesiger P, Fried M, Schwizer W. Scintigraphic validation of a magnetic resonance imaging method to study gastric emptying of a solid meal in humans. Gut. 1999;44(1):106-11. doi: 10.1136/gut.44.1.106, PMID 9862835.
Wilding IR, Coupe AJ, Davis SS. The role of γ-scintigraphy in oral drug delivery. Adv Drug Deliv Rev. 2001;46(1-3):103-24. doi: 10.1016/S0169-409X(00)00135-6, PMID 11259836.
Kedzierewicz F, Thouvenot P, Lemut J, Etienne A, Hoffman M, Maincent P. Evaluation of peroral silicone dosage forms in humans by gamma-scintigraphy. J Control Release. 1999;58(2):195-205. doi: 10.1016/S0168-3659(98)00154-0, PMID 10053192.
Davis SS, Hardy JG, Newman SP, Wilding IR. Gamma scintigraphy in the evaluation of pharmaceutical dosage forms. Eur J Nucl Med. 1992;19(11):971-86. doi: 10.1007/ BF00175865, PMID 1425786.
Pahwa R, Dutt H, Kumar V, Sharma CP. In vivo evaluation using gamma scintigraphy. Pharm Technol. 2010;34(11).
Khalaf A, Hoad CL, Blackshaw E, Alyami J, Spiller RC, Gowland PA. Simultaneous measurement of gastric emptying of a soup test meal using MRI and gamma scintigraphy. Diagnostics (Basel). 2020;10(3). doi: 10.3390/diagnostics10030170, PMID 32235742.
Weitschies W, Blume H, Monnikes H. Magnetic marker monitoring: high-resolution real-time tracking of oral solid dosage forms in the gastrointestinal tract. Eur J Pharm Biopharm. 2010;74(1):93-101. doi: 10.1016/ j.ejpb.2009.07.007. PMID 19619649.
Steingoetter A, Weishaupt D, Kunz P, Mader K, Lengsfeld H, Thumshirn M. Magnetic resonance imaging for the in vivo evaluation of gastric-retentive tablets. Pharm Res. 2003;20(12):2001-7. doi: 10.1023/b:pham.0000008049.40370.5a. PMID 14725366.
Rauya E, Sha O, Darwazeh R, Zhang BQ. Efficacy and safety of magnetic guided capsule gastroscopy in gastric diseases. Acta Gastroenterol Belg. 2019;82(4):507-13. PMID 31950806.
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(2):97-110. doi: 10.3109/10717544.2010.520354. PMID 20958237.
Faas H, Schwizer W, Feinle C, Lengsfeld H, de Smidt C, Boesiger P. Monitoring the intragastric distribution of a colloidal drug carrier model by magnetic resonance imaging460. Pharm Res. 2001;18(4):460-6. doi: 10.1023/a:1011098125916. PMID 11451032.
Schwizer W, Fraser R, Maecke H, Siebold K, Funck R, Fried M. Gd-DOTA as a gastrointestinal contrast agent for gastric emptying measurements with MRI. Magn Reson Med. 1994;31(4):388-93. doi: 10.1002/mrm.1910310407, PMID 8208114.
Malpure PS, Chavan BR, Maru AD, Bhadhane JS, Thakare EB, Sonawane PS. Gastroretentive drug delivery system: a review. World J Pharm Pharm Sci. 2019;8(3):506-28.
Lee J. Toward office-based measurement of gastric emptying in symptomatic diabetics using 13Coctanoic acid breath test. American Journal of Gastroenterology. 2000;95(10):2751-61. doi: 10.1016/S0002-9270(00)01976-6.
Benna Kumari, Khansili A, Manish K. Development and optimization of vildagliptin loaded floating microspheres using central composite design: in vitro and in vivo evaluations. Ann Rom Soc Cell Biol. 2021;25(4):12742-55.
Sheikh FA, Hussain MA, Ashraf MU, Haseeb MT, Farid-ul-Haq M. Linseed hydrogel based floating drug delivery system for fluoroquinolone antibiotics: design, in vitro drug release and in vivo real-time floating detection. Saudi Pharm J. 2020;28(5):538-49. doi: 10.1016/j.jsps.2020.03.005. PMID 32435134.
Rahamathulla M, Saisivam S, Gangadharappa HV. Development of valsartan floating matrix tablets using low density polypropylene foam powder: in vitro and in vivo evaluation. AAPS PharmSciTech. 2019;20(1):35. doi: 10.1208/s12249-018-1265-z, PMID 30604045.
Gokbulut E, Vural I, Aşıkoglu M, Ozdemir N. Floating drug delivery system of itraconazole: formulation, in vitro and in vivo studies. J Drug Deliv Sci Technol. 2019;49:491-501. doi: 10.1016/j.jddst.2018.12.019.
Sharma BG, Khanna K, Kumar N, Nishad DK, Basu M, Bhatnagar A. Development and gamma scintigraphy evaluation of gastro retentive calcium ion-based oral formulation: an innovative approach for the management of gastro-esophageal reflux disease (GERD). Drug Dev Ind Pharm. 2017;43(11):1759-69. doi: 10.1080/03639045.2017.1339080, PMID 28581835.
Razavi M, Karimian H, Yeong CH, Sarji SA, Chung LY, Nyamathulla S. Gamma scintigraphic study of the hydrodynamically balanced matrix tablets of Metformin HCl in rabbits. Drug Des Devel Ther. 2015;9:3125-39. doi: 10.2147/DDDT.S82935. PMID 26124637.
Razavi M, Karimian H, Yeong CH, Chung LY, Nyamathulla S, Noordin MI. Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits. Drug Des Devel Ther. 2015;9:4373-86. doi: 10.2147/DDDT.S86263. PMID 26273196.
Zhao Q, Gao B, Ma L, Lian J, Deng L, Chen J. Innovative intragastric ascaridole floating tablets: development, optimization, and in vitro-in vivo evaluation. Int J Pharm. 2015;496(2):432-9. doi: 10.1016/j.ijpharm.2015.10.007. PMID 26453784.
He S, Li F, Zhou D, Du J, Huang Y. Formulation and evaluation of novel coated floating tablets of bergenin and cetirizine dihydrochloride for gastric delivery. Drug Dev Ind Pharm. 2012;38(10):1280-8. doi: 10.3109/03639045.2011.645836. PMID 22206469.
Yao H, Yao H, Zhu J, Yu J, Zhang L. Preparation and evaluation of a novel gastric floating alginate/poloxamer inner-porous beads using foam solution. Int J Pharm. 2012;422(1-2):211-9. doi: 10.1016/j.ijpharm.2011.10.054, PMID 22093955.
Tadros MI. Controlled-release effervescent floating matrix tablets of ciprofloxacin hydrochloride: development, optimization and in vitro-in vivo evaluation in healthy human volunteers. Eur J Pharm Biopharm. 2010;74(2):332-9. doi: 10.1016/j.ejpb.2009.11.010, PMID 19932750.
Kulkarni A, Bhatia M. Development and evaluation of regioselective bilayer floating tablets of atenolol and lovastatin for biphasic release profile. Iran J Pharm Res. 2009;8(1):15-25.
Goole J, Van Gansbeke BV, Pilcer G, Deleuze P, Blocklet D, Goldman S. Pharmacoscintigraphic and pharmacokinetic evaluation on healthy human volunteers of sustained-release floating minitablets containing levodopa and carbidopa. Int J Pharm. 2008;364(1):54-63. doi: 10.1016/ j.ijpharm.2008.08.016, PMID 18778758.
Ma N, Xu L, Wang Q, Zhang X, Zhang W, Li Y. Development and evaluation of new sustained-release floating microspheres. Int J Pharm. 2008;358(1-2):82-90. doi: 10.1016/ j.ijpharm.2008.02.024, PMID 18407442.
Strubing S, Abboud T, Contri RV, Metz H, Mader K. New insights on poly(vinyl acetate)-based coated floating tablets: characterization of hydration and CO2 generation by benchtop MRI and its relation to drug release and floating strength. Eur J Pharm Biopharm. 2008;69(2):708-17. doi: 10.1016/j.ejpb.2007.12.009. PMID 18249530.
Nama M, Gonugunta CSR, Reddy Veerareddy PR. Formulation and evaluation of gastroretentive dosage forms of clarithromycin. AAPS PharmSciTech. 2008;9(1):231-7. doi: 10.1208/s12249-008-9038-8, PMID 18446486.
Ali J, Arora S, Ahuja A, Babbar AK, Sharma RK, Khar RK. Formulation and development of hydrodynamically balanced system for metformin: in vitro and in vivo evaluation. Eur J Pharm Biopharm. 2007;67(1):196-201. doi: 10.1016/j.ejpb.2006.12.015, PMID 17270409.
Ali J, Arora S, Ahuja A, Babbar AK, Sharma RK, Khar RK. Formulation and development of floating capsules of celecoxib: in vitro and in vivo evaluation. AAPS PharmSciTech. 2007;8(4):E119. doi: 10.1208/pt0804119, PMID 18181540.
Zou H, Jiang X, Kong L, Gao S. Design and gamma-scintigraphic evaluation of a floating and pulsatile drug delivery system based on an impermeable cylinder. Chem Pharm Bull (Tokyo). 2007;55(4):580-5. doi: 10.1248/cpb.55.580, PMID 17409552.
Jain SK, Agrawal GP, Jain NK. A novel calcium silicate-based microspheres of repaglinide: in vivo investigations. Journal of Controlled Release. 2006;113(2):111-6. doi: 10.1016/ j.jconrel.2006.04.005.
Jain SK, Agrawal GP, Jain NK. Evaluation of porous carrier-based floating orlistat microspheres for gastric delivery. AAPS PharmSciTech. 2006;7(4):90. doi: 10.1208/pt070490, PMID 17233542.
Stops F, Fell JT, Collett JH, Martini LG, Sharma HL, Smith AM. The use of citric acid to prolong the in vivo gastro-retention of a floating dosage form in the fasted state. Int J Pharm. 2006;308(1-2):8-13. doi: 10.1016/j.ijpharm.2005.09.036, PMID 16338108.
Stops F, Fell JT, Collett JH, Martini LG, Sharma HL, Smith AM. Citric acid prolongs the gastro-retention of a floating dosage form and increases the bioavailability of riboflavin in the fasted state. Int J Pharm. 2006;308(1-2):14-24. doi: 10.1016/j.ijpharm.2005.09.039, PMID 16343829.
Sato Y, Kawashima Y, Takeuchi H, Yamamoto H, Fujibayashi Y. Pharmacoscintigraphic evaluation of riboflavin-containing microballoons for a floating controlled drug delivery system in healthy humans. J Control Release. 2004;98(1):75-85. doi: 10.1016/j.jconrel.2004.04.021, PMID 15245891.
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(5):917-23. doi: 10.1016/S0142-9612(03)00579-9, PMID 14609680.
Sato Y, Kawashima Y, Takeuchi H, Yamamoto H. In vivo evaluation of riboflavin-containing microballoons for floating controlled drug delivery system in healthy human volunteers. J Control Release. 2003;93(1):39-47. doi: 10.1016/S0168-3659(03)00370-5, PMID 14602420.
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(1):3-12. doi: 10.1016/S0168-3659(97)00266-6, PMID 9795000.
Atyabi F, Sharma HL, Mohammad HAH, Fell JT. In vivo evaluation of a novel gastric retentive formulation based on ion exchange resins. J Control Release. 1996;42(2):105-13. doi: 10.1016/0168-3659(96)01344-2.
Desai S, Bolton S. A floating controlled-release drug delivery system: in vitro-in vivo evaluation. Pharm Res. 1993;10(9):1321-5. doi: 10.1023/a:1018921830385. PMID 8234170.
Khattar D, Ahuja A, Khar RK. Hydrodynamically balanced systems as sustained release dosage forms for propranolol hydrochloride. Pharmazie. 1990;45(5):356-8. PMID 2395898.
Davis SS, Stockwell AF, Taylor MJ, Hardy JG, Bechgaard H, Christensen FN. The effect of density on gastric emptying time of single and multiple unit dosage form. Pharm Res 1986;3(4):208-13.https://doi.org/10.1023/A:1016334629169.
Published
How to Cite
Issue
Section
Copyright (c) 2022 SWATI SAINI, BIGUL YOGESHVER BHARDWAJ, JATIN CHHABRA, MANISH KUMAR, RAKESH PAHWA
This work is licensed under a Creative Commons Attribution 4.0 International License.