Polymers in Medicine

Polim. Med.
Scopus CiteScore: 3.5 (CiteScore Tracker 3.6)
Index Copernicus (ICV 2023) – 121.14
MEiN – 70
ISSN 0370-0747 (print)
ISSN 2451-2699 (online) 
Periodicity – biannual

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Polymers in Medicine

2019, vol. 49, nr 2, July-December, p. 71–79

doi: 10.17219/pim/122016

Publication type: review article

Language: English

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Creative Commons BY-NC-ND 3.0 Open Access

Comprehensive review of the role of acrylic acid derivative polymers in floating drug delivery system

Beena Kumari1,2,A,B,C, Aparna Khansili2,B,D,E, Parmita Phougat3,B,D, Manish Kumar4,D,F

1 Department of Pharmaceutical Sciences, Indira Gandhi University, Rewari, India

2 Department of Pharmacy, School of Medical and Allied Sciences, GD Goenka University, Gurugram, India

3 Pandit Bhagwat Dayal Sharma Post Graduate Institute of Medical Sciences, Rohtak, India

4 MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana-Ambala, India

Abstract

In the development of drug delivery systems, an oral drug delivery system is the preferred route of drug administration. Many components play an important role in developing a drug delivery system. Amongst those components, polymers have evolved with these systems. Macromolecule compounds consisting of many monomer units which are joined to each other by different bonds are known as polymers. For drugs that are absorbed primarily in the upper gastrointestinal tract, floating drug delivery systems offer an additional advantage. The purpose behind this review was to focus on different types of floating drug delivery systems and different types of polymers used in floating drug delivery systems, focusing on acrylic acid derivatives and their applications. In this review, the main emphasis is on acrylic acid derivative polymers, their formulation and grades, and various patents on these types of polymers. Based on the literature survey, mainly 2 types of polymers are used in this drug delivery system; i.e., natural and synthetic. Examples of natural polymers are xanthan gum, guar gum or chitosan, and synthetic polymers include acrylic acid derivatives and hydroxylpropyl methylcellulose (HPMC). Eudragit and Carbopol are the most widely used acrylic acid derivatives.

Key words

acrylic polymers, Eudragit, floating drug delivery system, acrylic acid derivatives, carbomer

References (78)

  1. Avinash Y, Kaushik A, Tiwari K, Gaur A. Role of excipients and polymeric advancements in preparation of floating drug delivery systems. Int J Pharm Investig. 2015;5(1):1–12.
  2. Nayak AK, Maji R, Das B. Gastro-retentive drug delivery systems: A review. Asian J Pharma Clin Res. 2010;3(1):2–9.
  3. Lee JH, Park TG, Choi HK. Development of oral drug delivery system using floating microspheres. J Microencapsul. 1999;16:715–729.
  4. Bansal AK, Chawla G, Gupta P, Koradia V. Gastro-retention: A means to address regional variability in intestinal absorption. Pharma Tech. 2003;2(1):50–68.
  5. Zubedi SS, Mohammed S. Floating tablets and its polymers. J Drug Deliv Therapeutics. 2018;8(5):16–24.
  6. Jain SK, Jain NK, Agrawal GP. Gastro-retentive floating drug delivery: An overview. Drug Deliv Technol. 2005;5:7–15.
  7. Kumar G. Natural polymers in the development of floating drug delivery systems: A review. Int J Pharm Life Sci. 2013;2(4):165–178.
  8. Darekar D. An overview on natural gum and its pharmaceutical application. Int J Uni Pharmacy Biosci. 2013;2:535–547.
  9. Darekar D, Gupta P. An overview on natural gum and its pharmaceutical application. Int J Uni Pharmacy Biosci. 2014; 2: 432–447.
  10. Joshi M. Role of Eudragit in targeted drug delivery. Int J Curr Pharm Res. 2013;5:58–62.
  11. Sonje A, Chandra A. Comprehensive review on eudragit polymers. Int Res J Pharm. 2013;4:71–74.
  12. Rowe R, Paul S. Pharmaceutical Press. Handbook of Pharmaceutical Excipient. 6th ed., 2009.
  13. Stam JJ, Vink J, Lecessies S, Bruijin JA, Bregman W. Topical tretinoin under occlusion on a typical navei. Melanoma Res. 1988;8:539–548.
  14. Rieger MM, Lachman & Lieberman HA, Kanig JL. The Theory and Practice of Industrial Pharmacy. 3rd ed. 1986.
  15. Gupta P, Kumar M, Sachan N. An overview on polymethacrylate polymers in gastro-retentive dosage forms. Open Pharmaceutical Sciences J. 2015;2:31–42.
  16. Joshi M. Role of eudragit in targeted drug delivery. Int J Current Pharma Res. 2013;5(2):202.
  17. Rayehe TR, Zahra JA, Seyed AM. Formulation and evaluation of captopril floating matrix tablets based on gas formation. Afr J Pharm Pharmacol. 2013;6:2438–2444.
  18. Padma PS, Vandana P, Nisha V, Kausalya J, Vaijayanthi V, Ravichandiran V. Formulation and evaluation of gastro-retentive floating tablets of atenolol. J Pharm Res. 2011;4:3709–3711.
  19. Tripathi GK, Singh S, Nath G. Formulation and in-vitro evaluation of pH-sensitive oil entrapped polymeric blend amoxicillin beads for the eradication of Helicobacter pylori. Iran J Pharm Res. 2012;11:447–455.
  20. Kumar S, Chand T. Formulation and development of floating and mucoadhesive microspheres of clarithromycin. Pharm Innov J. 2013;2:19–26.
  21. Gangdharappa HV, Biswas S, Getyala A, Gupta V, Kumar PT. Development, in-vitro and in-vivo evaluation of novel floating hollow microspheres of Rosiglitazone Maleate. Der Pharm Lett. 2011;3:299–316.
  22. Wang J, Cui F, Shi K, Yang L, Wang S, Zhang L. In vivo evaluation of a sustained-release multiple-unit floating system containing nitrendipine. Asian J Pharm Sci. 2008;3:1517.
  23. Samala ML, Sridevi G. Role of polymers as gelling agents in the formulation of emulgels. Polym Sci. 2016;1:21–32.
  24. Prusty A, Gupta BK. Role of chitosan and eudragit in polymerbased extended release matrix tablets: A review. Int J Pharm Sci Res. 2017;8(12):4973–4982.
  25. Chein YW. Novel Drug Delivery Systems. 2nd ed. New York, NY: Marcel Dekker; 2009.
  26. Gokbulut E, Vural I, Aşıkoğlu ON. Floating drug delivery system of itraconazole: Formulation, in vitro and in vivo studies. J Drug Delivery Sci Tech. 2019;49:491–501.
  27. Zhang C, Xu MA. Floating multiparticulate system for ofloxacin based on a multilayer structure: In vitro and in vivo evaluation. Int J Pharm. 2012;430:141–150.
  28. Parida P, Mishra SC, Sahoo S, Behera A, Nayak BP. Development and characterization of ethyl cellulose based microsphere for sustained release of Nifedipine. J Pharma Analysis. 2016;6:341–344.
  29. Chaturvedi AK, Verma A, Singh A, Kumar A. Formulation and characterization of microballoons of norfloxacin. J Drug Deliv Therapeutics. 2011;1(2):21–26.
  30. Gupta R, Prajapati SK, Pattnaik S, Bhardwaj P. Asian Pac J Trop Biomed. 2014;4(9):729–735.
  31. Ehab H, Myron CG, Ronald WM, Adel S. A study of the pharmacodynamics differences between immediate and extended release bumetanide formulation. Int J Pharm. 2003;267:129–140.
  32. Khare B, Dubey N, Sharma A. Antiulcer activity of controlled release formulation containing aqueous extract of acacia catechu wild on rodent models. Int J Curr Pharm Res. 2018;10(5):25–31.
  33. Gupta P, Kumar M, Kaushik D. Pantoprazole sodium loaded microballoons for the systemic approach: In vitro and in vivo evaluation. Adv Pharm Bull. 2017;7(3):461–467.
  34. Giulia A, Andrea C, Francesca S, Aldo P, Silvana M, Rita P. Polysaccharides based gastro-retentive system to sustain piroxicam release: Development and in vivo prolonged anti-inflammatory effect. Biomac. 2018;6:213–219.
  35. Atyabi F, Sharma HL, Mohammad, HA, Fell JT. In vivo evaluation of a novel gastro-retentive formulation based on ion exchange resins. J Control Release. 1996;42:105–113.
  36. Radhakrishnan P, Verma P, Jayachandran V, et al. In vitro and in vivo evaluation of gastro-retentive carvedilol loaded chitosan beads using Gastroplus TM. Int J Biol Macromol. 2017;10:1016.
  37. Jijun F, Xiaoli W, Lishuang X, Jia M. Preparation and in vitro in vivo evaluation of double layer coated and matrix sustained release pellet formulations of Diclofenac Potassium. Int J Pharm. 2011;406:84–90.
  38. Huang Yu, Yumeng Wei, Hongru Y, et al. A 5-fluorouracil-loaded floating gastro-retentive hollow microsphere: Development, pharmacokinetic in rabbits, and biodistribution in tumor-bearing mice. Drug Des Devel Ther. 2016;10:997–1008.
  39. Colo G, Falchi S, Zambito Y. In vitro evaluation of a system for pH-controlled peroral delivery of metformin. J Control Release. 2002;80:119–128.
  40. 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. 2017;108:219–229.
  41. Goole J, Deleuze P, Vanderbist F, Amighi K. New levodapa sustained release floating mini tablets coated with insoluble acrylic polymer. Eur J Pharm Sci. 2008;68:310–318.
  42. Giovana B, Celli, Amyl G, Marianne S. Development and evaluation of floating alginate microspheres for oral delivery of anthocyanins: A preliminary investigation. Food Sci Nutr. 2017;5(3):713–721.
  43. Kagan L, Lapidot N, Afargan M, Kirmayer D. Gastro-retentive accordion pill: Enhancement of riboflavin bioavailability in humans. J Control Release. 2006;113:208–215.
  44. Nashar NN, Donia AA, Mady OY, Maghraby GM. Formulation of clarithromycin floating microspheres for eradication of Helicobacter pylori. J Drug Delivery Sci Tech. 2017;10:101–106.
  45. Ninan M, Xu L, Wang Q, Zhang X. Development and evaluation of new sustained-release floating microspheres. Int J Pharm. 2008;358:82–90.
  46. Jain A, Pandey V, Ganeshpurkar A, Dubey N, Bansal D. Formulation and characterization of floating microballoons of Nizatidine for effective treatment of gastric ulcers in murine model. Drug Deliv. 2015;22(3):306–311.
  47. Strubing, S, Metz H, Mader K. Characterization of poly (vinyl acetate) based floating matrix tablets. J Control Release. 2008;126:149–155.
  48. Yadav A, Jain DK. Gastro-retentive microballoons of metformin: Formulation development and characterization. J Adv Pharm Technol Res. 2011;2(1):51–55.
  49. Sato Y, Kawashima Y, Takeuchi H, Yamamoto H. In vivo evaluation of riboflavin-containing microballoons for controlled drug delivery system in healthy human volunteers. J Control Release. 2003;93:39–47.
  50. Husseiny RA, Abu Lila, Abdallah MH, Hamed EE, El-Ghamry. Design, in vitro/in vivo evaluation of meclizine HCl-loaded floating microspheres targeting pregnancy related nausea and vomiting. J Drug Delivery Sci Tech. 2018;5:135–142.
  51. El-Kamel AH, Sokar MS, Al-Gamal SS, Naggar VF. Preparation and evaluation of ketoprofen floating oral delivery system. Int J Pharm. 2001;220:13–21.
  52. Kumaraswamy S, Thangasundaralingam SR, Sekar R, Jayakrishnan A. A floating-type dosage form of repaglinide in polycarbonate microspheres. J Drug Delivery Sci Tech. 2017;10:201–213.
  53. Sato Y, Kawashima Y, Takeuchi H, Yamamoto H. In vitro and in vivo evaluation of riboflavin-containing microballoons for a floating controlled drug delivery system in healthy humans. Int J Pharm. 2004;275:97–107.
  54. Chao Pi, Jiyuan Yuan, Hao Liu, et al. In vitro and in vivo evaluation of curcumin loaded hollow microspheres prepared with ethyl cellulose and citric acid. Biomac. 2017;45:17–425.
  55. Pi C, Feng T, Liang J, et al. Polymer blends used to develop felodipine loaded hollow microspheres for improved oral bioavailability. Int J Biol Macromol. 2018;112:1038–1047.
  56. 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.
  57. Jain SK, Awasthi AM, Jain NK, Agrawal GP. Calcium silicate based microspheres of repaglinide for gastro-retentive floating drug delivery: Preparation and in vitro characterization. J Control Release. 2005;107:300–309.
  58. 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;81:135–140.
  59. Patra CN, Priya R, Swain S, et al. Pharmaceutical significance of Eudragit: A review. Future J Pharm Sci. 2017;2:789–796.
  60. Piao H, Liu S. Development of an osmotically-driven pellet coated with acrylic copolymers (Eudragit® RS 30D) for the sustained release of oxymatrine, a freely water soluble drug used to treat stress ulcers (I): In vitro and in vivo evaluation in rabbits. Drug Dev Ind Pharm. 2013;39:1230–1237.
  61. Sahoo SK, Dhal S, Mohapatro P, Behera BC, Barik BB. Effect of processing temperature on Eudragit RS PO microsphere characteristics in the solvent evaporation process. Pharmazie. 2007;62:638–639.
  62. Kibria G, Roni MA, Absar MS, Jalil RU. Effect of plasticizer on release kinetics of diclofenac sodium pellets coated with Eudragit RS30D. AAPS Pharm Sci Tech. 2008;9:1240–1246.
  63. Boza A, Caraballo I, Alvarez JF, Rabasco AM. Evaluation of Eudragit RS-PO and Ethocel 100 matrices for the controlled release of lobenzarit disodium. Drug Dev Ind Pharm. 1999;25:229–233.
  64. Kibria G, Islam KM, Jalil RU. Stability study of ambroxol hydrochloride sustained release pellets coated with acrylic polymer. Pak J Pharm Sci. 2009;22:36–43.
  65. Mathur V, Nagpal K, Singh SK, Mishra DN. Comparative release profile of sustained release matrix tablets of verapamil HCl. Int J Pharm Investig. 2013;3:60–65.
  66. Krejcová K, Rabisková M, Vetchý D, Tomásek V, Prokopová A. The effect of polymeric dispersion type on the release of diclofenac sodium from coated pellets. Ceska Slov Farm. 2007;56:190–199.
  67. Tayel SA, El-Nabarawi MA, Tadros MI, Abd-Elsalam WH. Positively charged polymeric nanoparticle reservoirs of terbinafine hydrochloride: preclinical implications for controlled drug delivery in the aqueous humor of rabbits. AAPS Pharm Sci Tech. 2013;14:782–793.
  68. Roni MA, Kibria G, Jalil RF. Formulation and in vitro evaluation of alfuzosin extended release tablets using directly compressible eudragit. Indian J Pharm Sci. 2009;71:252–258.
  69. Gupta NV, Natasha S, Getyala A, Bhat RS. Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal candidiasis. Acta Pharm. 2013;63:359–372.
  70. Rey H, Wagner KG, Wehrlé P, Schmidt PC. Development of matrixbased theophylline sustained-release microtablets. Drug Dev Ind Pharm. 2000;26:21–26.
  71. Zhang W, Li X, Ye T, et al. Nanostructured lipid carrier surface modified with Eudragit RS 100 and its potential ophthalmic functions. Int J Nanomed. 2014;9:4305–4315.
  72. Kibria G, Islam KM, Jalil RU. Stability study of ambroxol hydrochloride sustained release pellets coated with acrylic polymer. Pak J Pharm Sci. 2009;22:36–43.
  73. Antoine A, Hélène, H. Colonic delivery using zn/pectin beads with a eudragit coating. US Patent: 20080124279. 2008.
  74. Shojaei AH, Melissa EC. Modified release tablet formulations with enhanced mechanical properties. US Patent: 20070104782. 2007.
  75. David C, Rong-jen T, Hue-in L. Improved stabilization of misoprostol. European Patent: 0896823. 2002.
  76. Choy J, Choi GE, Park MC. Ursodeoxycholic acid-synthetic hydrotalcite Eudragit hybrid, pharmaceutical composition containing the same and method for preparing the same.US Patent: 20120156263. 2012.
  77. Isa O. Oral drug delivery formulations. US Patent: 20150250733. 2015;September 10.
  78. Jorge PH. Coated senna extract granules. WO/2011/014976. 2011; October 02.