Volume : 09, Issue : 06, June – 2022
44.A REVIEW ON SOURCE, PHYSICOCHEMICAL PROPERTIES, GRADES, PREPARATION, EVALUATION, APPLICATIONS AND PATENTS OF CARBOPOL IN VARIOUS FORMULATIONS
Mr. Niranjan D. Bachewad, Mr. Nandan C. Jadhav, Dr. R. O. Sonawane*
The current review was prepared with the objectives of complying source, grades, properties, preparation, evaluation, applications and patents of carbopol. Carbopol are polyacrylic acid polymers which may be used as bio adhesive vehicles for drug delivery. carbopols crosslinked with ally1 sucrose. Materials are available in a number of grades, depending largely on the molecular weight of the polymer chains. Carbopols are thought to be highly polydisperse, with significant differences in the molecular weight of supposedly identical grades reported. Carbopol is widely used in the pharmaceutical industry due to its high viscosity at low concentrations, good patient acceptability, and low toxicity profile. Initially, they were used as an alternative thickening agent to natural gums. Polyacrylic acid (PAA) is a large-scale commercial polymer that is widely used in a variety of industries, agriculture, and medicine. Controlled release in tablets, bioadhesion in buccal, ophthalmic, intestinal, nasal, vaginal, and rectal applications are all made possible by the readily water swellable carbopol polymers. Thickening at extremely low concentrations to produce a wide range of viscosities and flow properties in topical, lotions, creams, and gels, oral suspensions, and transdermal gel reservoirs. The prepared carbopol were further characterized for yield FTIR, DSC, XRPD, TGA, SEM, Raman Spectroscopy, Charge density and Zeta Potential.
Keywords: Carbopol, sustained release, controlled release, polyacrylic acid,
Cite This Article:
Please cite this article in press Niranjan D. Bachewad et al, A Review On Source, Physiochemical Properties, Grades, Preparation, Evaluation, Applications And Patents Of Carbopol In Various Formulations., Indo Am. J. P. Sci, 2022; 09(6).,
Number of Downloads : 10
1. Priyanka R, Prabhu RS. Magna Scientia Advanced Research and Reviews.
2. Craig DQ, Tamburic S, Buckton G, Newton JM. An investigation into the structure and properties of Carbopol 934 gels using dielectric spectroscopy and oscillatory rheometry. Journal of controlled release. 1994 Jul 1;30(3):213-23.
3. Bonacucina G, Martelli S, Palmieri GF. Rheological, mucoadhesive and release properties of Carbopol gels in hydrophilic cosolvents. International journal of pharmaceutics. 2004 Sep 10;282(1-2):115-30.
4. Lu G, Jun HW. Diffusion studies of methotrexate in Carbopol and Poloxamer gels. International journal of pharmaceutics. 1998 Jan 12;160(1):1-9
5. Ceulemans J, Ludwig A. Optimisation of carbomer viscous eye drops: an in vitro experimental design approach using rheological techniques. European Journal of Pharmaceutics and Biopharmaceutics. 2002 Jul 1;54(1):41-50.
6. Kumar K, Dhawan N, Sharma H, Vaidya S, Vaidya B. Bioadhesive polymers: Novel tool for drug delivery. Artificial cells, nanomedicine, and biotechnology. 2014 Aug 1;42(4):274-83.
7. R Varges P, M Costa C, S Fonseca B, F Naccache M, de Souza Mendes PR. Rheological characterization of carbopol® dispersions in water and in water/glycerol solutions. Fluids. 2019 Mar;4(1):3.
8. Park SH, Chun MK, Choi HK. Preparation of an extended-release matrix tablet using chitosan/Carbopol interpolymer complex. International journal of pharmaceutics. 2008 Jan 22;347(1-2):39-44.
9. Gutowski IA, Lee D, de Bruyn JR, Frisken BJ. Scaling and mesostructure of Carbopol dispersions. Rheologica acta. 2012 May;51(5):441-50.
10. Taberner TS, Martın-Villodre A, Pla-Delfina JM, Herráez JV. Consistency of Carbopol 971-P NF gels and influence of soluble and cross-linked PVP. International journal of pharmaceutics. 2002 Feb 21;233(1-2):43-50.
11. Goskonda VR, Reddy IK, Durrani MJ, Wilber W, Khan MA. Solid-state stability assessment of controlled release tablets containing Carbopol® 971P. Journal of controlled release. 1998 Jun 1;54(1):87-93.
12. Schoenfeld FK. Organizing for Profit with New Products. Carbopol Polymers: A Case History. Research Management. 1958 Sep 1;1(3):143-54.
13. Warda J, Brückle I, Bezúr A, Kushel D. Analysis of agarose, carbopol, and laponite gel poultices in paper conservation. Journal of the American Institute for Conservation. 2007 Jan 1;46(3):263-79.
14. Shafiei M, Balhoff M, Hayman NW. Chemical and microstructural controls on viscoplasticity in Carbopol hydrogel. Polymer. 2018 Mar .14; 139:44-51.
15. Loiseau J, Doerr N, Suau JM, Egraz JB, Llauro MF, Ladavière C, Claverie J. Synthesis and characterization of poly (acrylic acid) produced by RAFT polymerization. Application as a very efficient dispersant of CaCO3, kaolin, and TiO2. Macromolecules. 2003 May 6;36(9):3066-77.
16. Abdelaal MY, Makki MS, Sobahi TR. Modification and characterization of polyacrylic acid for metal ion recovery. Am. J. Polym. Sci. 2012;2(4):73-8.
17. Ohara, Takashi; Sato, Takahisa; Shimizu, Noboru; Prescher, Günter; Schwind, Helmut; Weiberg, Otto; Marten, Klaus; Greim, Helmut (2003). “Acrylic Acid and Derivatives”. Ullmann’s Encyclopedia of Industrial Chemistry. Weinheim: Wiley- VCH. doi:10.1002/14356007.a01_161.pub2
18. Khutoryanskiy VV, Staikos G. Hydrogen-bonded interpolymer complexes: formation, structure and applications. World Scientific; 2009.
19. Fahmy A, Mix R, Schönhals A, Friedrich JF. Structure of Plasma‐Deposited Poly (acrylic acid) Films. Plasma processes and polymers. 2011 Feb 22;8(2):147-59.
20. Panzade P, Puranik PK. Carbopol Polymers:s A Versatile Polymer for Pharmaceutical Applications. Research Journal of Pharmacy and Technology. 2010;3(3):672-5.
21. Park A, Shlepr J. Carbopol® Aqua CC Polymer: The Premier Cationic Compatible Rheology Modifier for Low pH Formulations. Cosmetic Science Technology. 2006 Jul:241-8.
23. https://www.lubrizol.com/-/media/Lubrizol/Health/TDS/TDS- 730_Viscosity_Carbopol_in_Aqueous-Systems.pdf)
24. Lefrançois P, Ibarboure E, Payré B, Gontier E, Le Meins JF, Schatz C. Insights into C arbopol gel formulations: Microscopy analysis of the microstructure and the influence of polyol additives. Journal of Applied Polymer Science. 2015 Dec 10;132(46).
25. Maslii Y, Ruban O, Kasparaviciene G, Kalveniene Z, Materiienko A, Ivanauskas L, Mazurkeviciute A, Kopustinskiene DM, Bernatoniene J. The Influence of pH Values on the Rheological, Textural and Release Properties of Carbomer Polacril® 40P-Based Dental Gel Formulation with Plant-Derived and Synthetic Active Components. Molecules. 2020 Jan;25(21):5018.
26. Sahoo S, Chakrabarti CK, Mishra SC. Qualitative analysis of controlled release ciprofloxacin/carbopol 934 mucoadhesive suspension. Journal of advanced pharmaceutical technology & research. 2011 Jul;2(3):195.
27. Suhail M, Wu PC, Minhas MU. Using carbomer-based hydrogels for control the release rate of diclofenac sodium: Preparation and in vitro evaluation. Pharmaceuticals. 2020 Nov;13(11):399 Craig D.Q.M. Pharmaceutical applications of DSC in Thermal analysis of pharmaceuticals. Boca Raton, CRC Press; 53-99, 2007.
28. Hosmani AH, Yogesh S, Thorat ID, Karmarkar AB. Formation and characterization of carbopol 971P-PVP interpolymer complex and its application for sustained delivery of acyclovir. Journal of Advanced Pharmacy Education & Research Apr-Jun. 2013;3(2).
29. Ismail SH, Hamdy A, Ismail TA, Mahboub HH, Mahmoud WH, Daoush WM. Synthesis and Characterization of Antibacterial Carbopol/ZnO Hybrid Nanoparticles Gel. Crystals. 2021 Sep;11(9):1092.
30. Andonova V, Georgiev G, Toncheva V, Karashanova D, Katsarov P, Kassarova M. Carbopol® and chitosan coated nanoparticles with in-situ loaded indomethacin. AJPTR. 2014;4(1):664-78.
31. Kaur DA, Raina AP, Singh NI. Formulation and evaluation of carbopol 940 based glibenclamide transdermal gel. Int J Pharm Pharm Sci. 2014;6:434-0.
32. Baek G, Kim C. Rheological properties of Carbopol containing nanoparticles. Journal of Rheology. 2011 Mar 24;55(2):313-30.
33. Sahoo S, Chakraborti CK, Mishra SC, Nanda UN. Qualitative analysis of environmentally responsive Biodegradable smart carbopol polymer.
34. ISHIKAWA S, KOBAYASHI M, SAMEJIMA M. Evaluation of the rheological properties of various kinds of carboxyvinylpolymer gels. Chemical and pharmaceutical bulletin. 1988 Jun 25;36(6):2118-27.
35. Lu MY, Borodkin S, Woodward L, Li P, Diesner C, Hernandez L, Vadnere M. A polymer carrier system for taste masking of macrolide antibiotics. Pharmaceutical research. 1991 Jun;8(6):706-12.
36. Delgado A, Gallardo V, Parera A, González-Caballero F. A study of the electrokinetic and stability properties of nitrofurantoin suspensions. II: Flocculation and redispersion properties as compared with theoretical interaction energy curves. Journal of pharmaceutical sciences. 1990 Aug 1;79(8):709-15.
37. Anlar S, Capan Y, Hincal AA. Physico-chemical and bioadhesive properties of polyacrylic acid polymers. Die Pharmazie. 1993 Apr 1;48(4):285-7.
38. Gumma A. Mesure de la bio-disponibilité d’un principe actif appliqué par voie topique [Measurement of the biologic-availability of an active principle applied topically]. Pharm Acta Helv. 1971 Dec;46(12):730-6. French. PMID: 5143004.
39. Laba D, editor. Rheological properties of cosmetics and toiletries. CRC Press; 1993 Sep 16.
40. Berney BM, Deasy PB. Evaluation of carbopol 934 as a suspending agent for sulphaoimidine suspensions. International Journal of Pharmaceutics. 1979 Aug 1;3(2- 3):73-80.
41. Pérez-Marcos B, Gutiérrez C, Gómez-Amoza J, Martínez-Pacheco R, Souto C, Concheiro A. Usefulness of certain varieties of Carbomer in the formulation of hydrophilic furosemide matrices. International journal of pharmaceutics. 1991 Jan 15;67(2):11321.
42. Orwoll, Robert A.; Yong, Chong S. (1999). “Poly(acrylic acid)”. In Mark, James E. (ed.). Polymer Data Handbook. Oxford University Press, Inc. pp. 252–253. ISBN 978- 0195107890.
43. Kaiser, Nancy; Klein, Dan; Karanja, Peter; Greten, Zachariah; Newman, Jerry (2009). “Inactivation of chlorhexidine gluconate on skin by incompatible alcohol hand sanitizing gels”. American Journal of Infection Control. 37 (7): 569– 73. doi:10.1016/j.ajic.2008.12.008. PMID 19398245
45. Mogoşanu, George Dan; Grumezescu, Alexandru Mihai (2014). “Natural and synthetic polymers for wounds and burns dressing”. International Journal of Pharmaceutics. 463 (2):127– 136. doi:10.1016/j.ijpharm.2013.12.015. PMID 24368109
46. Ruiz-Rubio L, Alonso ML, Pérez-Álvarez L, Alonso RM, Vilas JL, Khutoryanskiy VV. Formulation of Carbopol®/Poly (2-ethyl-2-oxazoline) s mucoadhesive tablets for buccal delivery of hydrocortisone. Polymers. 2018 Feb;10(2):175.
47. Vaithiyalingam SR, Tuliani P, Wilber W, Reddy IK, Khan MA. Formulation and stability evaluation of ketoprofen sustained-release tablets prepared by fluid bed granulation with Carbopol® 971P solution. Drug development and industrial pharmacy. 2002 Jan 1;28(10):1231-40.
48. Gupta S, Vyas SP. Carbopol/ chitosan-based pH triggered in situ gelling system for ocular delivery of timolol maleate. Scientia pharmaceutica. 2010 Dec;78(4):959-76.
49. Nandgude T, Thube R, Jaiswal N, Deshmukh P, Chatap V, Hire N. Formulation and evaluation of pH induced in-situ nasal gel of salbutamol sulphate. International journal of pharmaceutical sciences and nanotechnology. 2008;1(2):177-83.
50. Singh VK, Anis A, Banerjee I, Pramanik K, Bhattacharya MK, Pal K. Preparation and characterization of novel carbopol based bigels for topical delivery of metronidazole for the treatment of bacterial vaginosis. Materials Science and Engineering: C. 2014 Nov 1; 44:151-8.
51. Garud N, Garud A. Preparation and in-vitro evaluation of metformin microspheres using non-aqueous solvent evaporation technique. Tropical Journal of Pharmaceutical Research. 2012;11(4):577-83.
52. Sultana Y, Aqil M, Ali A, Zafar S. Evaluation of carbopol-methyl cellulose based sustained-release ocular delivery system for pefloxacin mesylate using rabbit eye model. Pharmaceutical development and technology. 2006 Jan 1;11(3):313-9.
53. Kumar JR, Muralidharan S. Formulation and in vitro evalution of gellan gum/carbopol and sodium alginate-based solution to gel depot of ketotifen fumarate system. Journal of Pharmaceutical Sciences and Research. 2012 Nov 1;4(11):1973.
54. Ubaid M, Ilyas S, Mir S, Khan AK, Rashid R, Khan MZ, Kanwal ZG, Nawaz A, Shah A, Murtaza G. Formulation and in vitro evaluation of carbopol 934-based modified clotrimazole gel for topical application. Anais da Academia Brasileira de Ciências. 2016 Dec 1; 88:2303-17.
55. Mortazavi SA, Jaffariazar Z, Damercheli E. Formulation and in-vitro evaluation of ocular ciprofloxacin-containing minitablets prepared with different combinations of carbopol 974P and various cellulose derivatives. Iranian journal of pharmaceutical research: IJPR. 2010;9(2):107.
56. Sheshala R, Ming NJ, Kok YY, Singh TR, Dua K. Formulation and characterization of pH induced in situ gels containing sulfacetamide sodium for ocular drug delivery: A combination of Carbopol®/HPMC polymer. Indian Journal of Pharmaceutical Education and Research. 2019 Oct 1.
57. Goskonda VR, Reddy IK, Durrani MJ, Wilber W, Khan MA. Solid-state stability assessment of controlled release tablets containing Carbopol® 971P. Journal of controlled release. 1998 Jun 1;54(1):87-93.
58. Al-Suwayeh SA, Taha EI, Al-Qahtani FM, Ahmed MO, Badran MM. Evaluation of skin permeation and analgesic activity effects of carbopol lornoxicam topical gels containing penetration enhancer. The Scientific World Journal. 2014 Jan 1;2014.
59. Kesharwani R, Sachan A, Singh S, Patel D. Formulation and evaluation of solid lipid nanoparticle (SLN) based topical gel of etoricoxib. Journal of Applied Pharmaceutical Science. 2016 Oct;6(10):124-31.
60. Jana S, Manna S, Nayak AK, Sen KK, Basu SK. Carbopol gel containing chitosan-egg albumin nanoparticles for transdermal aceclofenac delivery. Colloids and surfaces B: Biointerfaces. 2014 Feb 1; 114:36-44.
61. Ed Kisak Jagat Singh (2020) Diclofenac topical formulation [U.S. Patent No. 20200237919A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US20200237919A1/en
62. Ayca Yildiz Peköz Yildiz Özsoy Erginer Derya Arslan (2018) Mucoadhesive buccal in situ gel formulation [E.P. Patent No. 3173067A1] E.P. Patent and Trademark Office. https://patents.google.com/patent/EP3173067A1/en
63. Narayana KALA Aurora Sundeep(2012) Carrier based nanogel formulation for skin targeting [W.O. Patent No. 2012176212A1] W.O. Patent and Trademark Office. https://patents.google.com/patent/WO2012176212A1/en
64. Yunik Chang Gordon J. Dow Radhakrishnan Pillai (2020) Topical pharmaceutical formulations containing a low concentration of benzoyl peroxide in suspension in water and a water-miscible organic solvent [U.S. Patent No. 20200276218A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US20200276218A1/en
65. Andreas Sommer Chengzhi Zhang John Carter John Arthur Margaret Bradbury (2021) Novel pharmaceutical formulations [U.S. Patent No. 20210205214A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US20210205214A1/en
66. Hyder Aliyar Robert Huber Gary Loubert Gerald Schalau (2015) Topical Formulation Compositions Containing Silicone Based Excipients To Deliver Actives To A Substrate [U.S. Patent No. 20150141389A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US20150141389A1/en
67. Emre Sefik Caglar Hatice Yesim Karasulu Muhammed Davut Arpa Neslihan Ustudag Okur (2018) Formulations of benzocaine loaded microemulsion based hydrogels for therapeutic purposes and their production method [E.P. Patent No. 3344230A1] E.P. Patent and Trademark Office. https://patents.google.com/patent/EP3344230A1/en
68. Dennis Joseph Church Anthony Nichols (2017) Topical compositions comprising carbomer for the treatment and prevention of viral infections and allergic conditions [W.O. Patent No. 2017212422A1] W.O. Patent and Trademark Office. https://patents.google.com/patent/WO2017212422A1/en
69. Anders Pettersson Christer Nyström Susanne Bredenberg (2018) New Medicinal Preparations Useful In Health Care [C.Y. Patent No. 1119580T1] C.Y. Patent and Trademark Office. https://patents.google.com/patent/CY1119580T1/en
70. Michael T. Nordsiek Kodumudi S. Balaji (2020) Aqueous-based metronidazole gel formulations [U.S. Patent No. 10596155B2] U.S. Patent and Trademark Office. https://patents.google.com/patent/US10596155B2/en
71. Andreas Sommer Chengzhi Zhang John Carter John Charles Arthur Margaret Bradbury Thomas George Gant Manouchehr Shahbaz (2021) Formulations and Pharmacokinetics of Deuterated Benzoquinoline Inhibitors of Vesicular Monoamine Transporter 2 [U.S. Patent No. 20210244723A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US20210244723A1/en
72. Kenneth Shaw Mingbao Zhang (2021) Method of treatment using nanoparticulate ganaxolone formulations [U.S. Patent No. 11071740B2] U.S. Patent and Trademark Office. https://patents.google.com/patent/US11071740B2/en
73. Carla Marcella Caramella Silvia Rossi Giuseppina Sandri Giovanni Gennari (2014) Antiviral topical formulations in the form of a bio-adhesive gel [U.S. Patent No. 20100249156A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US20100249156A1/en
74. John A. Garruto Elizabeth Tsin Ho Makino Rahul C. Mehta Sujatha D. Sonti (2020) Melanin modification compositions and methods of use [A.U. Patent No. 2019261739B2] A.U. Patent and Trademark Office.https://patents.google.com/patent/AU2019261739B2/en
75. David K. Hood Karyn B. Visscher Surya Kamin Sounak Sarkar (2018) Lactamic polymer containing an acetoacetate moiety [U.S. Patent No.10118981B2] U.S. Patent and Trademark Office. https://patents.google.com/patent/US10118981B2/en
76. Hong-Ru Lin Kuo-Chun Sung (2003) Ophthalmic drug delivery formulations and method for preparing the same [U.S. Patent No. 6511660B1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US6511660B1/en
77. Youn Woong CHOI Byung Hwan RYOO Yong Mi JEONG Jae Sang JANG (2009)Novel controlled release-niacin formulation [U.S. Patent No. 20090069389A1 U.S.PatentandTrademarkOffice. https://patents.google.com/patent/US20090069389A1/en
78. Shen Gao Daniel Moros Maxine Moldenhauer (2003) Ibuprofen suspension [W.O. Patent No. 2003105804A1] W.O. Patent and Trademark Office. https://patents.google.com/patent/WO2003105804A1/en
79. Veerappa Subramanian Muthusamy Shanmugam (2003) Sustained release tablets containing bupropion hydrochloride [U.S. Patent No. 20030044462A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US20030044462A1/en
80. Jiansheng Wan, Xiaoming Chen, Pranav Gupta, David Monteith (2008) Ph sensitive matrix formulation[C.A. Patent No.2673111A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/CA2673111A1/en
81. Andreas Supersaxo (2002) topically applied pharmaceutical formulation [U.S. Patent No. 6420394B1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US6420394B1/en
82. Audra Lynn Stinchcomb Stan Lee Banks (2010) Formulations of cannabidiol and prodrugs of cannabidiol and methods of using the same [U.S. Patent No. 20100273895A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US20100273895A1/en
83. Hardeep Wadhwa (2003) Tasteless, directly compressible, fast-dissolving complexes and pharmaceutical formulations thereof [U.S. Patent No. 20030170310A1] U.S. Patent and Trademark Office. https://patents.google.com/patent/US20030170310A1/en
84. Lorraine Elisabeth Pena Maw-Sheng Wu New composition of minoxidil [J.P. Patent No. 2010006829A]J.P.Patent and Trademark Office. https://patents.google.com/patent/JP2010006829A/en
85. Foster M. FDA panel recommends more research on motavizumab; against marketing approval. Infectious Diseases in Children. 2010 Jul 1;23(7):28.
86. McNAMARA DA. New Oral and Topical Agents Fill Acne Toolbox. Family Practice News. 2009 May 15;39(10):28-.
88. Rahmi F, Sopyan I. pH Triggered In-situ Gelling Ophthalmic Drug Delivery System.
89. Gaynes BI, Onyekwuluje A. Topical ophthalmic NSAIDs: a discussion with focus on nepafenac ophthalmic suspension. Clinical ophthalmology (Auckland, NZ). 2008 Jun;2(2):355.
90. Nagra U, Adnan S, Shafqat S, Shabbir M, Ali S, Zafar A. Effect of Sustained Release Polymers on Drug Release Profile of Aceclofenac Tablets Physicochemical Properties, Analysis of Kinetics and Fit Factor.
91. Seshadri VC, Manohari PJ, Kunchithapatham J, Kulathingal J. TOPICAL GEL FORMULATION OF DIAMINODIPHENYL SULFONE FOR ACNE VULGARIS.
92. Sivakumar A. Formulation and Evaluation Studies of Acyclovir Topical Gels for Antiviral Activity (Doctoral dissertation, Periyar College of Pharmaceutical Sciences for Girls, Tiruchirapalli).
93. Das MK, Ahmed AB. Formulation and ex vivo evaluation of rofecoxib gel for topical application. Acta Pol Pharm. 2007 Sep 1;64(5):461-7.
94. Shelke O, Kulkarni A. Formulation, Development and Evaluation of Nifedipine Emulgel for Treatment of Anal Fissures using Polymeric Emulsifiers. Indian Journal of Pharmaceutical Education and Research. 2019 Apr 1;53(2s): s76-83.