COMPARATIVE PHYSICOCHEMICAL EVALUATION OF DIFFERENT POLYMERS AS A MATRIX FOR THE FORMULATION OF SUSTAINED RELEASE TABLET USING FACTORIAL DESIGN

Authors

  • ALAA BUR Department of Pharmaceutics, Faculty of Pharmacy, University of Khartoum, Khartoum, Sudan
  • ABDULLAH H. MAAD Department of Pharmaceutics, College of Pharmacy, University of Al-Ameed, Karbala, Iraq. Department of Pharmacy Practice, College of Clinical Pharmacy, Hodeidah University, Al-Hodeidah, Yemen https://orcid.org/0000-0002-6009-5166
  • YUSRA AHMED Department of Pharmaceutics, Faculty of Pharmacy, University of Khartoum, Khartoum, Sudan https://orcid.org/0000-0001-9668-3069
  • MALAZ YOUSEF Department of Pharmaceutics, Faculty of Pharmacy, University of Khartoum, Khartoum, Sudan
  • ZUHEIR OSMAN Department of Pharmaceutics, Faculty of Pharmacy, University of Khartoum, Khartoum, Sudan

DOI:

https://doi.org/10.22159/ijap.2025v17i4.54169

Keywords:

Sustained release matrix tablet, Metronidazole, Guar gum, Hydroxypropyl Methylcellulose (HPMC)

Abstract

Objective: This research aims to evaluate and compare the physicochemical properties of various naturally occurring biocompatible polymers used as matrix materials in sustained-release tablet formulations. Metronidazole serves as the model drug in these formulations.

Methods: This study contributes to ongoing efforts to investigate the potential of natural polymers in developing drug delivery systems. Nine batches of Metronidazole matrix tablets were formulated using the wet granulation technique, incorporating varying concentrations of guar gum and Hydroxypropyl Methylcellulose (HPMC) polymers, as well as their combination in a 4:1 ratio. A 3² full factorial statistical design was employed to assess the impact of both polymer type and concentration on the physical properties of the granules and tablets, including drug release percentage, half-life of drug release(T₅₀%), and dissolution efficiency after 8 h.

Results: The designed factors showed a significant influence (p<0.05) on most of the responses studied, except for the polymer type, which exhibited no significant effect on the dissolution efficiency after 8 h. HPMC-based granules exhibited the best flow properties, with an angle of repose of 32.0° in F8 (HPMC 55%), the lowest Carr’s Index of 11.8, and the best Hausner ratio of 1.12, indicating superior flowability compared to Guar-based formulations. HPMC-based tablets showed the highest hardness, with F8 (HPMC 55%) achieving 7.5 kg/cm². The highest swelling index was observed in the blended formulation F9 (Guar/HPMC 55%), reaching 2.93 at 7 h, compared to 2.62 in F1 (Guar 45%) and 1.86 in F2 (HPMC 45%). F1 (Guar 45%) exhibited the highest cumulative drug release, with 89.4% released at 24 h, compared to 85.4% in F9 (Guar/HPMC 55%). The combination of Guar gum and HPMC (F9, 55%) resulted in significant release retardation compared to individual polymers. The combination of Guar gum and HPMC (F9, 55%) resulted in the longest half-life (T₅₀%) of drug release, at 6.93 h, compared to 3.75 h in F1 (Guar 45%) and 5.27 h in F2 (HPMC 45%). Dissolution efficiency was highest in F5 (HPMC 50%), with 78.8% after 8 h, compared to 69.7% in F9 (Guar/HPMC 55%), showing that the combination of Guar gum and HPMC results in a slower release, reflected by the lower dissolution efficiency.

Conclusion: The blend of guar gum and HPMC in a 4:1 ratio provides a more effective release-retardation profile compared to guar gum alone. The formulation (F9), comprising a blend of guar gum and HPMC polymer at a higher concentration of 55%, was identified as the optimal formulation. It demonstrated favorable granule flow properties and exhibited the most effective sustained release profile.

References

Alam S, Bishal A, Bandyopadhyay B. Formulation and evaluation of metformin hydrochloride sustained release matrix tablets. Int J Curr Pharm Sci. 2021;13(5):82-8. doi: 10.22159/ijcpr.2021v13i5.1899.

Vroman I, Tighzert L. Biodegradable polymers. Materials. 2009;2(2):307-44. doi: 10.3390/ma2020307.

Ngwuluka NC, Ochekpe NA, Aruoma OI. Naturapolyceutics: the science of utilizing natural polymers for drug delivery. Polymers. 2014;6(5):1312-32. doi: 10.3390/polym6051312.

Majee SB, Mishra T, Gupti S. Gastroretentive effervescent floating tablets (GREFT) of drugs acting on cardiovascular diseases. Int J Pharm Pharm Sci. 2024;16(7):21-7. doi: 10.22159/ijpps.2024v16i7.51296.

Al Kamarany MA, Maad AH, Mohajab AA, Isra’a Al-masrafi I. Impact monitoring of low and high dexamethasone doses on COVID-19 outcomes in Hodeidah Yemen: a pharmacoepidemiological study. Asian J Pharm Clin Res. 2025;18(1):52-5. doi: 10.22159/ajpcr.2025v18i1.53226.

Siepmann J, Peppas NA. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv Drug Deliv Rev. 2001;48(2-3):139-57. doi: 10.1016/s0169-409x(01)00112-0, PMID 11369079.

Guarve K, Kriplani P. HPMC-A marvel polymer for pharmaceutical industry patent review. Recent Adv Drug Deliv Formul. 2021;15(1):46-58. doi: 10.2174/1872211314666210604120619, PMID 34086557.

Khudhur ZO, Maad AH, Ghanimi H, Abdolmaleki A. Fullerene nanoparticle as new therapeutic agent for the nervous system disorders. Nanomed J. 2024;11(4):342-59. doi: 10.22038/nmj.2024.78043.1903.

Bhatt P, Patel D, Patel A, Patel A, Nagarsheth A. Oral controlled release systems: current strategies and challenges misra a shahiwala a editors. Novel drug delivery technologies: innovative strategies for drug re-positioning. Singapore: Springer Singapore; 2019. p. 73-120. doi: 10.1007/978-981-13-3642-3_4.

Naeem A, Yu C, Wang X. Highly swellable cytocompatible and biodegradeable guar gum based hydrogel system for controlled release of bioactive components of liquorice (Glycyrrhiza glabra L.): synthesis and evaluation. Int J Biol Macromol. 2024;273(Pt1):132825. doi: 10.1016/j.ijbiomac.2024.132825.

Verma D, Sharma SK. Recent advances in guar gum based drug delivery systems and their administrative routes. Int J Biol Macromol. 2021 Jun 30;181:653-71. doi: 10.1016/j.ijbiomac.2021.03.087, PMID 33766594.

Azhar M, Mishra A. Review of nanoemulgel for treatment of fungal infections. Int J Pharm Pharm Sci. 2024;16(9):8-17. doi: 10.22159/ijpps.2024v16i9.51528.

Medina Lopez JR, Gomez Vargas YJ, Mendez Hernandez HR, Reyes Ramirez FD, Ruiz Segura JC, Hurtado M. Estimation of in vitro and in vivo performance of metronidazole oral dosage forms. Int J App Pharm. 2023;15(4):291-5. doi: 10.22159/ijap.2023v15i4.48137.

Bayor MT, Tuffour E, Lambon PS. Evaluation of starch from new sweet potato genotypes for use as a pharmaceutical diluent binder or disintegrant. J App Pharm Sci. 2013;3(8 Suppl 1):S17-S23. doi: 10.7324/JAPS.2013.38.S4.

Stationery Office British Pharmacopoeia. London, UK: The Stationery Office; 2008.

Gangurde HH, Chordiya MA, Tamizharasi S, Senthilkumaran K, Sivakumar T. Formulation and evaluation of sustained release bioadhesive tablets of ofloxacin using 32 factorial design. Int J Pharm Investig. 2011;1(3):148-56. doi: 10.4103/2230-973X.85964, PMID 23071937.

Singh J, Garg R, Gupta GD. Enhancement of solubility of lamotrigine by solid dispersion and development of orally disintegrating tablets using 32 full factorial design. J Pharm (Cairo). 2015;2015:828453. doi: 10.1155/2015/828453, PMID 26634173.

Kassaye L, Genete G. Evaluation and comparison of in-vitro dissolution profiles for different brands of amoxicillin capsules. Afr Health Sci. 2013;13(2):369-75. doi: 10.4314/ahs.v13i2.25, PMID 24235938.

Shah RB, Tawakkul MA, Khan MA. Comparative evaluation of flow for pharmaceutical powders and granules. AAPS PharmSciTech. 2008;9(1):250-8. doi: 10.1208/s12249-008-9046-8, PMID 18446489.

Rao YM, Veni JK, Jayasagar G. Formulation and evaluation of diclofenac sodium using hydrophilic matrices. Drug Dev Ind Pharm. 2001;27(8):759-66. doi: 10.1081/DDC-100107239, PMID 11699827.

Ahmed Y, Maad AH, Hassan HA, Abdallah DB, Yousef M, Kadhum AA. Evaluation of carboxymethyl millet starch and pregelatinized millet starch as pharmaceutical excipients using factorial experimental designs. Int J App Pharm. 2025;17(2):321-8. doi: 10.22159/ijap.2025v17i2.52161.

Naga Durga DH, Lohithasu D, Ramana Murthy KV. Development and evaluation of diclofenac sodium controlled release dosage forms using natural hydrophilic and hydrophobic polymers and its comparative studies. Indian J Pharm Educ Res. 2017;51(1):116-27. doi: 10.5530/ijper.51.1.16.

Dahma Z, Torrado Salmeron C, Alvarez Alvarez C, Guarnizo Herrero V, Martinez Alonso B, Torrado G. Topical meloxicam hydroxypropyl guar hydrogels based on low substituted hydroxypropyl cellulose solid dispersions. Gels. 2024;10(3):207. doi: 10.3390/gels10030207, PMID 38534625.

Sriamornsak P, Thirawong N, Korkerd K. Swelling erosion and release behavior of alginate based matrix tablets. Eur J Pharm Biopharm. 2007;66(3):435-50. doi: 10.1016/j.ejpb.2006.12.003, PMID 17267187.

El Nabarawi MA, Teaima MH, Abd El Monem RA, El Nabarawy NA, Gaber DA. Formulation release characteristics and bioavailability study of gastroretentive floating matrix tablet and floating raft system of mebeverine HCl. Drug Des Devel Ther. 2017 Apr 3;11:1081-93. doi: 10.2147/DDDT.S131936, PMID 28435220.

Berradi A, Aziz F, Achaby ME, Ouazzani N, Mandi L. A comprehensive review of polysaccharide based hydrogels as promising biomaterials. Polymers. 2023;15(13):2908. doi: 10.3390/polym15132908, PMID 37447553.

Shah U, Patel B, Patel M. Formulation and evaluation of controlled release matrix tablet of diltiazem HCl by using HPMC and guar gum as polymeric matrix material. Ars Pharm. 2012;53(4):16-20.

Maad AH, Al Gamli AH, Shamarekh KS, Refat M, Shayoub ME. Antiproliferative and apoptotic effects of Solenostemma Argel leaf extracts on colon cancer cell line HCT-116. Biomed Pharmacol J. 2024;17(3):1987-96. doi: 10.13005/bpj/3001.

Yavari N, Azizian S. Mixed diffusion and relaxation kinetics model for hydrogels swelling. J Mol Liq. 2022 Oct 1;363:119861. doi: 10.1016/j.molliq.2022.119861.

Ritger PL, Peppas NA. A simple equation for description of solute release II. fickian and anomalous release from swellable devices. J Control Release. 1987;5(1):37-42. doi: 10.1016/0168-3659(87)90035-6.

Colombo P, Bettini R, Santi P, Peppas NA. Swellable matrices for controlled drug delivery: gel layer behaviour mechanisms and optimal performance. Pharm Sci Technol Today. 2000;3(6):198-204. doi: 10.1016/S1461-5347(00)00269-8, PMID 10840390.

Published

07-07-2025

How to Cite

BUR, A., MAAD, A. H., AHMED, Y., YOUSEF, . M., & OSMAN, . Z. (2025). COMPARATIVE PHYSICOCHEMICAL EVALUATION OF DIFFERENT POLYMERS AS A MATRIX FOR THE FORMULATION OF SUSTAINED RELEASE TABLET USING FACTORIAL DESIGN. International Journal of Applied Pharmaceutics, 17(4), 201–209. https://doi.org/10.22159/ijap.2025v17i4.54169

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Original Article(s)

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