Skip to main content

Advertisement

Log in

Pluronic F127-co-poly (2 acrylamido-2-methylpropane sulphonic acid) crosslinked matrices as potential controlled release carrier for an anti-depressant drug: in vitro and in vivo attributes

  • Original Paper
  • Published:
Chemical Papers Aims and scope Submit manuscript

Abstract

The principal goal of the study was to orchestrate synthetically cross-connected pluronic-co-poly (AMPS) hydrogels by free radical copolymerization technique for the controlled conveyance of Venlafaxine HCl. Pluronic-based hydrogels were developed by blending different proportions of pluronic F127, AMPS, and EGDMA while venlafaxine HCl was selected as an experimental drug. FTIR, TGA, DSC, SEM, and XRD demonstrated the effective grafting of reactants into the crosslinked network. The fabricated hydrogel gave more than 90% drug entrapment efficiency. The swelling pattern represents more than 34% swelling at pH 6.8 whereas, at pH 1.2 it gives up to 17% swelling indicating pH-responsive hydrogel. Similarly, drug release analysis also gave more drug release at pH 6.8 as compared to pH 1.2, that is 98% and 42%, respectively. Kinetics modeling revealed the controlled release trend of venlafaxine in a fabricated gel. Cytotoxicity and compatibility of developed gel to the biological system were examined by conducting a toxicity study on rabbits, which confirmed that the developed gel was non-toxic. Supported with pharmacokinetic evaluations, a stable copolymeric network of pluronic F127 was developed with AMPS as a likely possibility for the controlled delivery of venlafaxine HCl.

Graphical abstract

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7
Fig. 8
Fig. 9
Fig. 10

Similar content being viewed by others

References

  • Abdullah O, Minhas MU, Ahmad M, Ahmad S, Ahmad A (2018) Synthesis of hydrogels for combinatorial delivery of 5-fluorouracil and leucovorin calcium in colon cancer: optimization, in vitro characterization and its toxicological evaluation. Polym Bull:1–21.

  • Ahmed EM (2015) Hydrogel: preparation, characterization, and applications: a review. J Adv Res 6(2):105–121

    Article  CAS  PubMed  Google Scholar 

  • Akash MSH, Rehman K, Li N, Gao J-Q, Sun H, Chen S (2012) Sustained delivery of IL-1Ra from pluronic F127-based thermosensitive gel prolongs its therapeutic potentials. Pharm Res 29(12):3475–3485

    Article  CAS  PubMed  Google Scholar 

  • Akhlaq M, Maryam F, Elaissari A, Ullah H, Adeel M, Hussain A, Ramzan M, Ullah O, Zeeshan Danish M, Iftikhar S (2018) Pharmacokinetic evaluation of quetiapine fumarate controlled release hybrid hydrogel: a healthier treatment of schizophrenia. Drug Deliv 25(1):916–927

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Ali L, Ahmad M, Usman M, Yousuf M (2014) Controlled release of highly water-soluble antidepressant from hybrid copolymer poly vinyl alcohol hydrogels. Polym Bull 71(1):31–46

    Article  CAS  Google Scholar 

  • Ali L, Ahmad M, Aamir MN, Minhas MU, Rasul A, Yousuf M, Hussain H, Khan JA, Sohail M (2019) Venlafaxine-loaded sustained-release poly (hydroxyethyl methacrylate-co-itaconic acid) hydrogel composites: their synthesis and in vitro/in vivo attributes. Iran Poly J 28(3):251–258

    Article  CAS  Google Scholar 

  • Asghar S, Akhtar N, Minhas MU, Khan KU (2021) Bi-polymeric spongy matrices through cross-linking polymerization: synthesized and evaluated for solubility enhancement of acyclovir. AAPS PharmSciTech 22(5):1–16

    Article  Google Scholar 

  • Asghar S, Minhas MU, Ahmad M, Khan KU, Sohail M, Khalid I (2018) Hydrophobic–hydrophilic cross‐linked matrices for controlled release formulation of highly water‐soluble drug venlafaxine: synthesis and evaluation studies. Adv Polym Tech :1–13.

  • Azmeera, V.; Adhikary, P.; Krishnamoorthi, S (2012). Synthesis and characterization of graft copolymer of dextran and 2-acrylamido-2-methylpropane sulphonic acid. Int J Carbohydr Chem [cited 2020 Nov 11]:[8 p.]. https://doi.org/10.1155/2012/209085

  • Babu M, Yadav HK, Moin A, Shivakumar HG (2011) In vitro–in vivo evaluation of poly (2-hydroxyethyl methacrylate-co-methyl methacrylate) hydrogel implants containing cisplatin. Acta Pharm Sin B 1(4):261–267

    Article  CAS  Google Scholar 

  • Barhate S, Husain M (2016) Comparative in vitro dissolution testing of hydrophilic controlled-release venlafaxine matrix tablets and effexor XR using QbD. Dissolut Technol 23:40–44

    Article  CAS  Google Scholar 

  • Barkat K, Ahmad M, Minhas MU, Khalid I (2017) Oxaliplatin-loaded crosslinked polymeric network of chondroitin sulfate-co-poly (methacrylic acid) for colorectal cancer: its toxicological evaluation. J Appl Polym Sci 134(38):45312

    Article  Google Scholar 

  • Barlow A, Landolf KM, Barlow B, Yeung SYA, Heavner JJ, Claassen CW, Heavner MS (2020) Review of emerging pharmacotherapy for the treatment of coronavirus disease 2019 Pharmacotherapy: Pharmacotherapy, 40(5):416–37.

  • Beuermann S, Buback M, Hesse P, Junkers T, Lacík I (2006) Free-radical polymerization kinetics of 2-acrylamido-2-methylpropanesulfonic acid in aqueous solution. Macromolecules 39(2):509–516

    Article  CAS  Google Scholar 

  • Bukhari SMH, Khan S, Rehanullah M, Ranjha NM (2015) Synthesis and characterization of chemically cross-linked acrylic acid/gelatin hydrogels: effect of pH and composition on swelling and drug release. Int J Polym Sci [cited 2020 Nov 11]:[16 p.]. https://doi.org/10.1155/2015/187961

  • Bymaster FP, Dreshfield-Ahmad LJ, Threlkeld PG, Shaw JL, Thompson L, Nelson DL, Hemrick-Luecke SK, Wong DT (2001) Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacol 25(6):871–880

    Article  CAS  Google Scholar 

  • Chun KW, Lee JB, Kim SH, Park TG (2005) Controlled release of plasmid DNA from photo-cross-linked pluronic hydrogels. Biomaterials 26(16):3319–3326

    Article  CAS  PubMed  Google Scholar 

  • Devane CL (2003) Immediate-release versus controlled-release formulations: pharmacokinetics of newer antidepressants in relation to nausea. J Clin Psychiatry 64:14–19

    CAS  PubMed  Google Scholar 

  • Escobar-Chávez J, López-Cervantes M, Naik A, Kalia Y, Quintanar-Guerrero D, Ganem-Quintanar A (2006) Applications of thermo-reversible pluronic F-127 gels in pharmaceutical formulations. J Pharm Pharm Sci 9(3):339–358

    PubMed  Google Scholar 

  • Freiberg S, Zhu X (2004) Polymer microspheres for controlled drug release. Int J Pharm 282(1–2):1–18

    Article  CAS  PubMed  Google Scholar 

  • Ganji F, Vasheghani-Farahani E (2009) Hydrogels in controlled drug delivery systems. Iran Polym J 18(1):63–88

    CAS  Google Scholar 

  • Gioffredi E, Boffito M, Calzone S, Giannitelli SM, Rainer A, Trombetta M, Mozetic P, Chiono V (2016) Pluronic F127 hydrogel characterization and biofabrication in cellularized constructs for tissue engineering applications. Procedia Cirp 49:125–132

    Article  Google Scholar 

  • Gohel MC, Bariya SH (2009) Fabrication of triple-layer matrix tablets of venlafaxine hydrochloride using xanthan gum. AAPS PharmSciTech 10(2):624–630

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Gohel M, Soni C, Nagori S, Sarvaiya K (2008) Modulation of venlafaxine hydrochloride release from press coated matrix tablet. Indian J Pharm Sci 70(3):292

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Gong CY, Shi S, Dong PW, Zheng XL, Fu SZ, Guo G, Yang JL, Wei YQ, Qian ZY (2009) In vitro drug release behavior from a novel thermosensitive composite hydrogel based on Pluronic f127 and poly (ethylene glycol)-poly (ε-caprolactone)-poly (ethylene glycol) copolymer. BMC Biotechnol 9(1):1–13

    Article  Google Scholar 

  • Gulrez SK, Al-Assaf S, Phillips GO (2011) Hydrogels: methods of preparation, characterisation and applications. In: Carpi A (ed) Progress in molecular and environmental bioengineering, 1st edn. IntechOpen, London, pp 117–150

    Google Scholar 

  • Gupta P, Vermani K, Garg S (2002) Hydrogels: from controlled release to pH-responsive drug delivery. Drug Discov Today 7(10):569–579

    Article  CAS  PubMed  Google Scholar 

  • Hamidi M, Azadi A, Rafiei P (2008) Hydrogel nanoparticles in drug delivery. Adv Drug Deliv Rev 60(15):1638–1649

    Article  CAS  PubMed  Google Scholar 

  • Hanif M, Ranjha NM, Shoaib MH, Mudasser J, Yousuf RI, Khan A, Zia-ul-Haq M (2011) Preparation, characterization and release of verapmil hydrochloride from polycaprolactone/acrylic acid (PCL/AA) hydrogels. Pak J Pharm Sci 24(4):503–511

    CAS  PubMed  Google Scholar 

  • Hazer O, Soykan C, Kartal Ş (2007) Synthesis and swelling behavior analysis of poly (acrylamidoxime-co-2-acrylamido-2-methylpropane sulfonic Acid) hydrogels. J Macromol Sci A 45(1):45–51

    Article  Google Scholar 

  • Hennink WE, van Nostrum CF (2012) Novel crosslinking methods to design hydrogels. Adv Drug Deliv Rev 64:223–236

    Article  Google Scholar 

  • Hu H, Yu J, Li Y, Zhao J, Dong H (2012) Engineering of a novel pluronic F127/graphene nanohybrid for pH responsive drug delivery. J Biomed Mater Res A 100(1):141

    Article  PubMed  Google Scholar 

  • Hussain T, Ranjha NM, Shahzad Y (2011) Swelling and controlled release of tramadol hydrochloride from a pH-sensitive hydrogel. Des Monomers Polym 14(3):233–249

    Article  CAS  Google Scholar 

  • Innocenzi P, Malfatti L, Piccinini M, Marcelli A (2010) Evaporation-induced crystallization of pluronic F127 studied in situ by time-resolved infrared spectroscopy. J Phys Chem A 114(1):304–308

    Article  CAS  PubMed  Google Scholar 

  • Jakab K, Damon B, Neagu A, Kachurin A, Forgacs G (2006) Three-dimensional tissue constructs built by bioprinting. Biorheology, 43(3,4): 509–13

  • Jin J, Mitome T, Egashira Y, Nishiyama N (2011) Phase control of ordered mesoporous carbon synthesized by a soft-templating method. Colloids Surf A Physicochem Eng Asp 384(1–3):58–61

    Article  CAS  Google Scholar 

  • Kabiri K, Azizi A, Zohuriaan MMJ, Bagheri MG, Bouhendi H, Jamshidi A (2011) Super-alcogels based on 2-acrylamido-2-methylpropane sulphonic acid and poly (ethylene glycol) macromer. Iran Polym J 20(3):175–183

    CAS  Google Scholar 

  • Khalid I, Ahmad M, Minhas MU, Barkat K, Sohail M (2018) Cross-linked sodium alginate-g-poly (Acrylic Acid) structure: a potential hydrogel network for controlled delivery of loxoprofen sodium. Adv Polym Tech 37(4):985–995

    Article  CAS  Google Scholar 

  • Khan S, Ranjha NM (2014) Effect of degree of cross-linking on swelling and on drug release of low viscous chitosan/poly (vinyl alcohol) hydrogels. Polym Bull 71(8):2133–2158

    Article  CAS  Google Scholar 

  • Khattak SF, Bhatia SR, Roberts SC (2005) Pluronic F127 as a cell encapsulation material: utilization of membrane-stabilizing agents. Tissue Eng 11(5–6):974–983

    Article  CAS  PubMed  Google Scholar 

  • Kim SJ, Lee CK, Kim SI (2004) Electrical/pH responsive properties of poly (2-acrylamido-2-methylpropane sulfonic acid)/hyaluronic acid hydrogels. J Appl Polym Sci 92(3):1731–1736

    Article  CAS  Google Scholar 

  • Kolesky DB, Truby RL, Gladman AS, Busbee TA, Homan KA, Lewis JA (2014) 3D bioprinting of vascularized, heterogeneous cell-laden tissue constructs. J Adv Mater 26(19):3124–3130

    Article  CAS  Google Scholar 

  • Mahmood A, Ahmad M, Sarfraz RM, Minhas MU (2016) β-CD based hydrogel microparticulate system to improve the solubility of acyclovir: optimization through in-vitro, in-vivo and toxicological evaluation. J Drug Deliv Sci Technol 36:75–88

    Article  CAS  Google Scholar 

  • Malana MA, Zafar ZI, Zuhra R (2012) Effect of cross linker concentration on swelling kinetics of a synthesized ternary co-polymer system. J Chem Soc Pak 34(4):793–801

    CAS  Google Scholar 

  • Malaterre V, Metz H, Ogorka J, Gurny R, Loggia N, Mäder K (2009) Benchtop-magnetic resonance imaging (BT-MRI) characterization of push–pull osmotic controlled release systems. J Control Release 133(1):31–36

    Article  CAS  PubMed  Google Scholar 

  • Malik NS, Ahmad M, Minhas MU (2017) Cross-linked β-cyclodextrin and carboxymethyl cellulose hydrogels for controlled drug delivery of acyclovir. PLoS ONE 12(2):e0172727

    Article  PubMed  PubMed Central  Google Scholar 

  • Matthew JE, Nazario YL, Roberts SC, Bhatia SR (2002) Effect of mammalian cell culture medium on the gelation properties of Pluronic® F127. Biomaterials 23(23):4615–4619

    Article  CAS  PubMed  Google Scholar 

  • Mawad D, Foster JL, Lauto A (2008) Drug-delivery study and estimation of polymer–solvent interaction parameter for bisacrylate ester-modified Pluronic hydrogels. Int J Pharm 360(1–2):231–235

    Article  CAS  PubMed  Google Scholar 

  • Muth EA, Haskins JT, Moyer JA, Husbands GE, Nielsen ST, Sigg EB (1986) Antidepressant biochemical profile of the novel bicyclic compound Wy-45,030, an ethyl cyclohexanol derivative. Biochem Pharmacol 35(24):4493–4497

    Article  CAS  PubMed  Google Scholar 

  • Nart Z, Kayaman-Apohan N (2011) Preparation, characterization and drug release behavior of poly (acrylic acid–co-2-hydroxyethyl methacrylate-co-2-acrylamido-2-methyl-1-propanesulfonic acid) microgels. J Polym Res 18(5):869–874

    Article  CAS  Google Scholar 

  • Nerkar PP, Gattani S (2011) In vivo, in vitro evaluation of linseed mucilage based buccal mucoadhesive microspheres of venlafaxine. Drug Deliv 18(2):111–121

    Article  CAS  PubMed  Google Scholar 

  • Nerkar PP, Gattani SG (2012) Cress seed mucilage based buccal mucoadhesive gel of venlafaxine: in vivo, in vitro evaluation. J Mater Sci Mater Med 23(3):771–779

    Article  CAS  PubMed  Google Scholar 

  • Peppas N (1985) Analysis of fickian and non-fickian drug release from polymers. Pharm Acta Helv 60:110–111

    CAS  PubMed  Google Scholar 

  • Quan H, Xie L, Su X, Feng Y (2019) The thermoviscosifying behavior of water-soluble polymer based on graft polymerization of pluronic F127 with acrylamide and 2-acrylamido-2-methylpropane sulfonic acid sodium salt. Polymers 11(10):1702

    Article  CAS  PubMed Central  Google Scholar 

  • Ranjha NM, Ayub G, Naseem S, Ansari MT (2010) Preparation and characterization of hybrid pH-sensitive hydrogels of chitosan-co-acrylic acid for controlled release of verapamil. J Mater Sci Mater Med 21(10):2805–2816

    Article  CAS  PubMed  Google Scholar 

  • Ranjha NM, Mudassir J, Majeed S (2011) Synthesis and characterization of polycaprolactone/acrylic acid (PCL/AA) hydrogel for controlled drug delivery. B Mater Sci 34(7):1537–1547

    Article  CAS  Google Scholar 

  • Rastogi PK, Krishnamoorthi S, Ganesan V (2012) Synthesis, characterization, and ion exchange voltammetry study on 2-acrylamido-2-methylpropane sulphonic acid and N-(hydroxymethyl) acrylamide-based copolymer. J Appl Polym Sci 123(2):929–935

    Article  CAS  Google Scholar 

  • Rehman S, Ranjha NM, Shoukat H, Madni A, Ahmad F, Raza MR, Jameel QA, Majeed A, Ramzan N (2021) Fabrication, evaluation, in vivo pharmacokinetic and toxicological analysis of pH-sensitive eudragit S-100-coated hydrogel beads: a promising strategy for colon targeting. AAPS PharmSciTech 22(6):1–17

    Article  Google Scholar 

  • Ribeiro LS, Falcão AC, Patrício JA, Ferreira DC, Veiga FJ (2007) Cyclodextrin multicomponent complexation and controlled release delivery strategies to optimize the oral bioavailability of vinpocetine. J Pharm Sci 96(8):2018–2028

    Article  CAS  PubMed  Google Scholar 

  • Rokhade AP, Shelke NB, Patil SA, Aminabhavi TM (2007) Novel hydrogel microspheres of chitosan and pluronic F-127 for controlled release of 5-fluorouracil. J Microencapsul 24(3):274–288

    Article  CAS  PubMed  Google Scholar 

  • Sadeghi M, Yarahmadi M (2011) Synthesis and properties of biopolymer based on carboxymethyl cellulose-g-poly (N-vinylpyrollidin-co-2-acrylamido-2-methyl propan sulfonic acid as superabsorbent hydrogels. Orient J Chem 27(1):13–21

    CAS  Google Scholar 

  • Saikia A, Aggarwal S, Mandal U (2013) Preparation and controlled drug release characteristics of thermoresponsive PEG/poly (NIPAM-co-AMPS) hydrogels. Int J Polym Mater 62(1):39–44

    Article  CAS  Google Scholar 

  • Sairam M, Babu VR, Naidu BVK, Aminabhavi TM (2006) Encapsulation efficiency and controlled release characteristics of crosslinked polyacrylamide particles. Int J Pharm 320(1–2):131–136

    Article  CAS  PubMed  Google Scholar 

  • Şen M, Yakar A (2005) Enhancement of copolymerization of itaconic acid with N-vinyl 2-pyrrolidone by radiation in the presence of cross-linking agent. Nucl Instrum Meth B 234(3):226–234

    Article  Google Scholar 

  • Shoukat H, Pervaiz F, Noreen S, Nawaz M, Qaiser R, Anwar M (2020) Fabrication and evaluation studies of novel polyvinylpyrrolidone and 2-acrylamido-2-methylpropane sulphonic acid-based crosslinked matrices for controlled release of acyclovir. Polym Bull 77(4):1869–1891

    Article  CAS  Google Scholar 

  • Soares GA, de Castro AD, Cury BS, Evangelista RC (2013) Blends of cross-linked high amylose starch/pectin loaded with diclofenac. Carbohydr Polym 91(1):135–142

    Article  CAS  PubMed  Google Scholar 

  • Solhi S, Jashni E, Hosseini S, Van der Bruggen B, Solhi H, Khodabakhshi A (2018) Adapting the release characteristics of aluminum phosphide from membrane-coated rice tablets by using activated carbon nanoparticles. J Ind Eng Chem 58:202–207

    Article  CAS  Google Scholar 

  • Tanaka S, Doi A, Nakatani N, Katayama Y, Miyake Y (2009) Synthesis of ordered mesoporous carbon films, powders, and fibers by direct triblock-copolymer-templating method using an ethanol/water system. Carbon 47(11):2688–2698

    Article  CAS  Google Scholar 

  • Teijon J, Trigo R, Garcia O, Blanco M (1997) Cytarabine trapping in poly (2-hydroxyethyl methacrylate) hydrogels: drug delivery studies. Biomaterials 18(5):383–388

    Article  CAS  PubMed  Google Scholar 

  • Teijón C, Olmo R, Blanco MD, Teijón JM, Romero A (2006) Effect of the crosslinking degree and the nickel salt load on the thermal decomposition of poly (2-hydroxyethyl methacrylate) hydrogels and on the metal release from them. J Colloid Interface Sci 295(2):393–400

    Article  PubMed  Google Scholar 

  • Turabee MH, Jeong TH, Ramalingam P, Kang JH, Ko YT (2019) N, N, N-trimethyl chitosan embedded in situ Pluronic F127 hydrogel for the treatment of brain tumor. Carbohydr Polym 203:302–309

    Article  CAS  PubMed  Google Scholar 

  • Varaprasad K, Ravindra S, Reddy NN, Vimala K, Raju KM (2010) Design and development of temperature sensitive porous poly (NIPAAm-AMPS) hydrogels for drug release of doxorubicin-a cancer chemotherapy drug. J Appl Polym Sci 116(6):3593–3602

    CAS  Google Scholar 

  • Varaprasad K, Reddy NN, Ravindra S, Vimala K, Raju KM (2011) Synthesis and characterizations of macroporous poly (acrylamide-2-acrylamido-2-methyl-1-propanesulfonic acid) hydrogels for in vitro drug release of ranitidine hydrochloride. Int J Polym Mater 60(7):490–503

    Article  CAS  Google Scholar 

  • Wichterle O, Lim D (1960) Hydrophilic gels for biological use. Nature 185(4706):117

    Article  Google Scholar 

  • Yin L, Fei L, Cui F, Tang C, Yin C (2007) Superporous hydrogels containing poly (acrylic acid-co-acrylamide)/O-carboxymethyl chitosan interpenetrating polymer networks. Biomaterials 28(6):1258–1266

    Article  CAS  PubMed  Google Scholar 

  • Zarzycki R, Modrzejewska Z, Nawrotek K (2017) Drug release from hydrogel matrices. Ecol Chem Enginer S 17:117–136

    Google Scholar 

  • Zhang C, Easteal AJ (2003) Study of free-radical copolymerization of N-isopropylacrylamide with 2-acrylamido-2-methyl-1-propanesulphonic acid. J Appl Polym Sci 88(11):2563–2569

    Article  CAS  Google Scholar 

Download references

Funding

No funding was obtained.

Author information

Authors and Affiliations

Authors

Contributions

HS Writing–original draft; Writing–review & editing. Conception and design of data, Acquisition of data, acquisition of interpretation of data, revising the manuscript critically for important intellectual content. FP Approval of the version of the manuscript to be published and supervised the findings of this work. revising the manuscript critically for important intellectual content. SR Data analysis, drafting the manuscript.

Corresponding author

Correspondence to Fahad Pervaiz.

Ethics declarations

Conflict of interest

The authors declare no conflict of interest.

Additional information

Publisher's Note

Springer Nature remains neutral with regard to jurisdictional claims in published maps and institutional affiliations.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Shoukat, H., Pervaiz, F. & Rehman, S. Pluronic F127-co-poly (2 acrylamido-2-methylpropane sulphonic acid) crosslinked matrices as potential controlled release carrier for an anti-depressant drug: in vitro and in vivo attributes. Chem. Pap. 76, 2917–2933 (2022). https://doi.org/10.1007/s11696-022-02077-4

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s11696-022-02077-4

Keywords

Navigation