The effect of polymer amount and crosslinker ratio in polymeric hydrogel beads on characterization

Rukiye Sevinç Özakar; Emrah Özakar

The effect of polymer amount and crosslinker ratio in polymeric hydrogel beads on characterization

Abstract

Today, treating diseases requires increasing the patient's living standard rather than just applying a classical treatment protocol. In this study, it was aimed at facilitating drug intake, reduce the dose of the active substance, reduce the number of daily doses to be taken, reduce or eliminate possible side and/or toxic effects, transport the active substance to the target area and make as much bioavailability from the active substance as possible too. For this purpose, in our study, hydrogel bead formulations with ionotropic gelation technique were developed using ampicillin sodium as a model drug and sodium alginate and HPMC K100 as polymer. CaCl2 was used as a crosslinking agent. While developing a new drug delivery system formulation, size, morphology with SEM, in vitro release profiles, release kinetics, encapsulation efficiencies, drug loading capacities, yields, and swelling capacities, FT-IR and XRD analysis were evaluated in the hydrogel beads depending on the amount of the polymer and crosslinking agent. It has been made possible to extend the duration of drug action by changing the amount of polymer and crosslinker ratios in oral drug delivery of ampicillin sodium with alginate beads. Thus, it is likely to increase patient compliance as well as to reduce drug-related side and/or toxic effects with less dosing.

Keywords

References

[1] Uhrich KE, Cannizzaro SM, Langer RS, Shakesheff KM. Polymeric systems for controlled drug release. Chem Rev. 1999; 99 (11): 3181-3198.
[2] McGinity JW, DiNunzio JC, Keen JM. Oral Controlled-release polymeric drug delivery systems. In Bader RA, Putman DA. (Eds). Engineering Polymer Systems for Improved Drug Delivery. John Wiley & Sons, Inc., 2014, pp.285-318.
[3] Nokhodchi A, Raja S, Patel P, Asare-Addo K. The role of oral controlled release matrix tablets in drug delivery systems. Bioimpacts. 2012; 2 (4): 175-87.
[4] Saikia C, Gogoi P, Maji TK. Chitosan: A promising biopolymer in drug delivery applications. J Mol Genet Med. 2015; S4 (006): 1-10.
[5] Veronovski A, Tkalec G, Knez Ž, Novak Z. Characterisation of biodegradable pectin aerogels and their potential use as drug carriers. Carbohydr Polym. 2014. 113: 272-278.
[6] Gandhi KJ, Deshmane SV, Biyani KR. Polymers in pharmaceutical drug delivery system: A review. Int J Pharm Sci Rev Res. 2012; 14 (2): 57-66.
[7]Ibrahim M, Naguib YW, Sarhan HA, Abdelkader H. Gastro-retentive oral drug delivery systems: A promising approach for narrow absorption window drugs. J Adv Biomed & Pharm Sci. 2019; 2 (3): 98-110. Research Article [8] Chowdary KPR, Chaitanya CKL. Recent research on floating drug delivery systems-A review. J Glob Trends Pharm Sci. 2014; 5 (1): 1361-1373.
[9] Choi BY, Park HJ, Hwang SJ, Park JB. Preparation of alginate beads for floating drug delivery system: Effects of CO(2) gas-forming agents. Int J Pharm. 2002; 239(1-2): 81-91.

[10] Zubedi SS, Mohammed S. Formulation and in-vitro evaluation of chlorzoxazone floating tablets. Pharma Innov. 2018; 7 (8): 348-356.
[11] Racoviţă Ş, Vasiliu S, Popa M, Luca C. Polysaccharides based on micro- and nanoparticles obtained by ionic gelation and their applications as drug delivery systems. Rev Roum Chim. 2009; 54 (9): 709-718.
[12] Patil P, Chavanke D, Wagh MA. A review on ionotropic gelation method: Novel approach for controlled gastroretentive gelispheres. Int J Pharm Pharm Sci. 2012; 4 (4): 27-32. [13] Ibrahim SM, Abou El Fadl FI, El-Naggar AA. Preparation and characterization of crosslinked alginate–CMC beads for controlled release of nitrate salt. J Radioanal Nucl Chem. 2014; 299 (3): 1531-1537.
[14] Patil H, Tiwari RV, Repka MA. Recent advancements in mucoadhesive floating drug delivery systems: A mini- review. J Drug Deliv Sci Technol. 2016; 31: 65-71.
[15] [16] Dixit N. Floating drug delivery system J Curr Pharm Res. 2011; 7 (1): 6-20. Sevinç Özakar R, Aktaş Y, Bilici D, Ayyıldız A. Physicochemical characterization and microbiological evaluation of tetracycline hcl loaded chitosan beads for periodontitis treatment: A preliminary study. J Allied Pharm Sci. 2017: 28- 34.
[17] Unagolla JM, Jayasuriya AC. Drug transport mechanisms and in vitro release kinetics of vancomycin encapsulated chitosan-alginate polyelectrolyte microparticles as a controlled drug delivery system. Eur J Pharm Sci. 2018; 114: 199- 209.
[18] El-Kamel A, Al-Gohary OMN, Hosny EA. Alginate-diltiazem hydrochloride beads: optimization of formulation factors, in vitro and in vivo availability. J Microencapsul. 2003; 20 (2): 211-225.
[19] Mandal S, Kumar SS, Krishnamoorthy B, Basu SK. Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods. Braz J Pharm Sci. 2010; 46 (4): 785-793.
[20] Smrdel P, Bogataj M, Mrhar A. The influence of selected parameters on the size and shape of alginate beads prepared by ionotropic gelation. Sci Pharm. 2008; 76 (1): 77-90.
[21] Ramteke KH, Jadhav VB, Kulkarni NS, Kharat AR, Diwate SB. Preparation, evaluation and optimization of multiparticulate system of mebendazole for colon targeted drug delivery by using natural polysaccharides. Adv Pharm Bull. 2015; 5 (3): 361-371.
[22] Ahmed OAA, Badr-Eldin SM, Ahmed TA. Kinetic study of the in vitro release and stability of theophylline floating beads. Int J Pharm Pharm Sci. 2013; 5 (1): 179-184.
[23] Cojocaru V, Ranetti AE, Hinescu LG, Ionescu M, Cosmescu C, Poştoarcă AG, Cinteza OL. Formulation and evaluation of in vitro release kinetics of Na(3)CaDTPA decorporation agent embedded in microemulsion-based gel formulation for topical delivery. Farmacia, 2015. 63 (5): p. 656-664.
[24] Maver T, Mohan T, Gradišnik L, Finšgar M, Stana Kleinschek K, Maver, U. Polysaccharide thin solid films for analgesic drug delivery and growth of human skin cells. Frontiers in chemistry, 2019. 7 (217): 1-13.
[25] Patel N, Lalwani D, Gollmer S, Injeti E, Sari Y, Nesamony J. Development and evaluation of a calcium alginate based oral ceftriaxone sodium formulation. Prog Biomater. 2016; 5 (2): 117-133.
[26] Shivakumara LR, Demappa T. Synthesis and swelling behavior of sodium alginate/poly(vinyl alcohol) hydrogels. Turk J Pharm Sci. 2019; 16 (3): 252-260.
[27] Tavakol M, Vasheghani-Farahani E, Hashemi-Najafabadi S. The effect of polymer and CaCl2 concentrations on the sulfasalazine release from alginate-N,O-carboxymethyl chitosan beads. Prog Biomater. 2013; 2 (1): 1-8.
[28] Tótoli EG, Salgado HRN. Development and validation of the quantitative analysis of ampicillin sodium in powder for injection by Fourier-transform infrared spectroscopy (FT-IR). Physical Chemistry. 2012; 2 (6): 103-108.
[29] Abdelmalek I, Svahn I, Mesli S, Simonneaux G, Mesli A. Formulation, evaluation and microbiological activity of ampicillin and amoxicillin microspheres. J Mater Environ Sci. 2014; 5 (6): 1799-1807.
[30] Verma A, Sharma M, Verma N, Pandit J. Floating alginate beads: Studies on formulation factors for improved drug entrapment efficiency and in vitro release. Farmacia. 2013; 61 (1): 143-161.
[31] Onyido I, Sha’Ato R, Nnamonu LA. Environmentally friendly formulations of trifluralin based on alginate modified starch. J Environ Prot. 2012; 3 (9): 1085-1093.
[32] Sekharan TR, Palanichamy S, Tamilvanan S, Shanmuganathan S, Thirupathi AT. Formulation and evaluation of hydroxypropyl methylcellulose-based controlled release matrix tablets for theophylline. Indian J Pharm Sci. 2011; 73 (4): 451-456.
[33] Huei GOS, Muniyandy S, Sathasivam T, Veeramachineni AK, Janarthanan P. Iron cross-linked carboxymethyl cellulose-gelatin complex coacervate beads for sustained drug delivery. Chemical Papers. 2016; 70 (2): 243-252.
[34] Del Gaudio P, Russo P, Lauro MR, Colombo P, Aquino RP. Encapsulation of ketoprofen and ketoprofen lysinate by prilling for controlled drug release. AAPS PharmSciTech. 2009; 10 (4): 1178-1185.
[35] Iswandana R, Putri KSS, Dwiputra R, Yanuari T, Sari SP, Djajadisastra J. Formulation of chitosan tripolyphosphate- tetrandrine beads using ionic gelation method: In vitro and in vivo evaluation. Int J App Pharm. 2017; 9 (5): 109-115.
[36] Larosa C, Salerno M, de Lima JS, Meri RM, da Silva MF, de Carvalho LB, Converti A. Characterisation of bare and tannase-loaded calcium alginate beads by microscopic, thermogravimetric, FTIR and XRD analyses. Int J Biol Macromol. 2018; 115: 900-906.
[37] Patil JS, Kamalapur MV, Marapur SC, Shiralshetti SS, Kadam DV. Ionotropically gelled chitosan-alginate complex hydrogel beads: Preparation, characterization and in-vitro evaluation. Indian J Pharm Edu Res. 2012; 46 (1): 248-52. [38] Mokale V, Jitendra N, Yogesh S, Gokul K. Chitosan reinforced alginate controlled release beads of losartan potassium: Design, formulation and in vitro evaluation. J Pharm Investig. 2014; 44 (4): 243-252.
[39] Bagyalakshmi J, Arun Raj R, Ravi TK. Fomulation, physical charecterisation and in-vitro release studies of prednisolone alginate beads for colon targeting by ionotropic gelation. Pharmacie Globale. 2011; 2(3): 1-4.
[40] Kim J-Y, Seo J-W, Rhee Y-S, Park C-W, Park E-S. Freeze-dried highly porous matrix as a new gastroretentive dosage form for ecabet sodium: in vitro and in vivo characterizations. J Pharm Sci. 2014; 103 (1): 262-273.
[41] Prasanth AG, Kumar AS, Shruthi BS, Subramanian S. Kinetic study and in vitro drug release studies of nitrendipine loaded arylamide grafted chitosan blend microspheres. Mater Res Express. 2019; 6 (12).
[42] Pudjiastuti P, Wafiroh S, Hendrad E, Darmokoesoemo H, Harsini M, Fauzi MARD, Nahar L, Sarker SD. Disintegration, in vitro dissolution, and drug release kinetics profiles of kappa-carrageenan-based nutraceutical had- shell capsules containing salicylamide. Open Chem. 2020; 18 (1): 226-231.
[43] Kowalczuk D, Pitucha M. Application of FTIR method for the assessment of immobilization of active substances in the matrix of biomedical materials. Materials. 2019; 12 (18): 2972.
[44] Mourdikoudis S, Pallares RM, Thanh NTK. Characterization techniques for nanoparticles: Comparison and complementarity upon studying nanoparticle properties. Nanoscale. 2018; 10 (27): 12871-12934.

Details

Primary Language

English

Subjects

Pharmaceutical Delivery Technologies

Journal Section

Research Article

Authors

Rukiye Sevinç Özakar ^*
Türkiye

Emrah Özakar
Türkiye

Publication Date

June 28, 2025

Submission Date

April 11, 2021

Acceptance Date

June 28, 2025

Published in Issue

Year 2021 Volume: 25 Number: 5

IZ

https://izlik.org/JA69RZ56BD

Cite

RIS / Bibtex

APA

Sevinç Özakar, R., & Özakar, E. (2025). The effect of polymer amount and crosslinker ratio in polymeric hydrogel beads on characterization. Journal of Research in Pharmacy, 25(5), 653-666. https://izlik.org/JA69RZ56BD

AMA

1.Sevinç Özakar R, Özakar E. The effect of polymer amount and crosslinker ratio in polymeric hydrogel beads on characterization. J. Res. Pharm. 2025;25(5):653-666. https://izlik.org/JA69RZ56BD

Chicago

Sevinç Özakar, Rukiye, and Emrah Özakar. 2025. “The Effect of Polymer Amount and Crosslinker Ratio in Polymeric Hydrogel Beads on Characterization”. Journal of Research in Pharmacy 25 (5): 653-66. https://izlik.org/JA69RZ56BD.

EndNote

Sevinç Özakar R, Özakar E (July 1, 2025) The effect of polymer amount and crosslinker ratio in polymeric hydrogel beads on characterization. Journal of Research in Pharmacy 25 5 653–666.

IEEE

[1]R. Sevinç Özakar and E. Özakar, “The effect of polymer amount and crosslinker ratio in polymeric hydrogel beads on characterization”, J. Res. Pharm., vol. 25, no. 5, pp. 653–666, July 2025, [Online]. Available: https://izlik.org/JA69RZ56BD

ISNAD

Sevinç Özakar, Rukiye - Özakar, Emrah. “The Effect of Polymer Amount and Crosslinker Ratio in Polymeric Hydrogel Beads on Characterization”. Journal of Research in Pharmacy 25/5 (July 1, 2025): 653-666. https://izlik.org/JA69RZ56BD.

JAMA

1.Sevinç Özakar R, Özakar E. The effect of polymer amount and crosslinker ratio in polymeric hydrogel beads on characterization. J. Res. Pharm. 2025;25:653–666.

MLA

Sevinç Özakar, Rukiye, and Emrah Özakar. “The Effect of Polymer Amount and Crosslinker Ratio in Polymeric Hydrogel Beads on Characterization”. Journal of Research in Pharmacy, vol. 25, no. 5, July 2025, pp. 653-66, https://izlik.org/JA69RZ56BD.

Vancouver

1.Rukiye Sevinç Özakar, Emrah Özakar. The effect of polymer amount and crosslinker ratio in polymeric hydrogel beads on characterization. J. Res. Pharm. [Internet]. 2025 Jul. 1;25(5):653-66. Available from: https://izlik.org/JA69RZ56BD