Skip to main content

Advertisement

SpringerLink
Log in

Physicochemical and in Vitro Antibacterial Evaluation of Metronidazole Loaded Eudragit S-100 Nanofibrous Mats for the Intestinal Drug Delivery

  • Research Article
  • Published:
Advanced Fiber Materials Aims and scope Submit manuscript

Abstract

Metronidazole (MTZ) loaded Eudragit S-100 (ES-100) nonwoven nanofibrous mats were successfully electrospun and evaluated for intestinal drug delivery. MTZ was varied in the range of 1–15% (w/w) in ES-100 nanofibrous mats, the morphological characterization of nanofibrous mats was carried out using FE-SEM and the average diameter of nanofiber was found in the range 150–600 nm. WAXD and DSC demonstrated the amorphous nature of MTZ in ES-100 nanofibrous mats. Their contact angle analysis confirmed the hydrophobic nature. The mechanical strength of ES-100 nanofibrous mats decreased with increasing MTZ concentration. The drug release profiles showed 74% MTZ release from ES-100d within 2 h at pH 6.8 which is the colonic environment. Antibacterial activities against gram-positive bacteria (Staphylococcus aureus) and gram-negative bacteria (Escherichia coli) showed that the ES-100 nanofibrous mats loaded with MTZ exhibited good activity.

Graphic abstract

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

Access this article

Log in via an institution

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

Instant access to the full article PDF.

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

  1. Patel M, Shah T, Amin A. Therapeutic opportunities in colon-specific drug-delivery systems. Crit Rev Ther Drug Carr Syst. 2007;24:147.

    Article  CAS  Google Scholar 

  2. Asghar LF, Chandran S. Design and evaluation of pH modulated controlled release matrix systems for colon specific delivery of indomethacin. Pharmazie. 2008;63:736.

    CAS  Google Scholar 

  3. Beloqui A, Coco R, Memvanga PB, Ucakar B, des Rieux A, Préat V. pH-sensitive nanoparticles for colonic delivery of curcumin in inflammatory bowel disease. Int J Pharm. 2014;473:203.

  4. Canavan C, Abrams KR, Mayberry JF. Meta-analysis: mortality in Crohn’s disease. Aliment Pharmacol Ther. 2007;25:861.

    Article  CAS  Google Scholar 

  5. Bonadiesa I, Maglione L, Ambrogi V, Paccez JD, Zerbini LF, Luiz F, Rocha e silva LF, Picanço NS, Wanderli PT, Grafova I, Grafov A, Carfagna C. Electrospun core/shell nanofibers as designed devices for efficient Artemisinin delivery. Eur Poly J. 2017;89:211.

    Article  Google Scholar 

  6. Moreno I, González-González V, Romero-García J. Control release of lactate dehydrogenase encapsulated in poly (vinyl alcohol) nanofibers via electrospinning. Eur Polym J. 2011;47:1264.

    Article  CAS  Google Scholar 

  7. Zamani M, Morshed M, Varshosaz J, Jannesari M. Controlled release of metronidazole benzoate from poly e-caprolactone electrospun nanofibers for periodontal diseases. Eur J Pharm Biopharm. 2010;75:179.

    Article  CAS  Google Scholar 

  8. Kim K, Luu YK, Chang C, Fang D, Hsiao BS, Chu B, Hadjiargyrou M. Incorporation and controlled release of a hydrophilic antibiotic using poly(lactide-co-glycolide)-based electrospun nanofibrous scaffolds. J Control Release. 2004;98:47.

    Article  CAS  Google Scholar 

  9. Huang ZM, He CL, Yang A, Zhang Y, Han XJ, Yin J, Wu Q. Encapsulating drugs in biodegradable ultrafine fibers through co-axial electrospinning. J Biomed Mater Res A. 2006;77:169.

    Article  Google Scholar 

  10. Verreck G, Chun I, Rosenblatt J, Peeters J, Dijck AV, Mensch J, Noppe M, Brewster ME. Incorporation of drugs in an amorphous state into electrospun nanofibers composed of a water-insoluble, nonbiodegradable polymer. J Control Release. 2003;92:349.

    Article  CAS  Google Scholar 

  11. Reda RI, Wen MM, El-Kamel AH. Ketoprofen-loaded Eudragit electrospun nanofibers for the treatment of oral mucositis. Int J Nanomed. 2017;12:2335.

    Article  CAS  Google Scholar 

  12. Laha A, Sharma CS, Majumdar S. Sustained drug release from multi-layered sequentially crosslinked electrospun gelatin nanofiber mesh. Mater Sci Eng C. 2017;76:782.

    Article  CAS  Google Scholar 

  13. Lee H, Xu G, Kharaghani D, Nishino M, Song KH, Lee JS, Kim IS. Electrospun tri-layered zein/PVP-GO/zein nanofiber mats for providing biphasic drug release profiles. Int J Pharm. 2017;531:101.

    Article  CAS  Google Scholar 

  14. Hamori M, Nagano K, Kakimoto S, Naruhashi K, Kiriyama A, Nishimura A, Shibata N. Preparation and pharmaceutical evaluation of acetaminophen nano-fiber tablets: application of a solvent-based electrospinning method for tableting. Biomed Pharmacother. 2016;78:14.

    Article  CAS  Google Scholar 

  15. https://healthcare.evonik.com/en/products/pharmaceutical-excipients/solubility-enhancement

  16. Hita V, Singh R, Jain SK. Colonic targeting of metronidazole using azo aromatic polymers: development and characterization. Drug Del. 1997;4:19.

    Article  CAS  Google Scholar 

  17. Chacko M, Bhide SV. Carcinogenicity, perinatal carcinogenicity and teratogenicity of low dose metronidazole (MTZ) in Swiss mice. J Cancer Res Clin Oncol. 1986;112:135.

    Article  CAS  Google Scholar 

  18. Chaber A. Okołooperacyjna profilaktyka antybiotykowa w chirurgii przewodu pokarmowego Antibiotic prophylaxis in alimentary tract surgery, w chirurgii przewodu pokarmowego. Wspó³czesna Onkologia. 1999;2:86.

  19. Sadowska A, Krętowski R, Szynaka B, Cechowska-Pasko M, Car H. Metronidazole decreases viability of DLD-1 colorectal cancer cell line. Cancer Biother Radiopharm. 2013;28:615.

    Article  CAS  Google Scholar 

  20. Turanli Y, Tort S, Acartürk F. Development and characterization of methylprednisolone loaded delayed release nanofibers. J Drug Del Sci Tech. 2019;49:58.

    Article  CAS  Google Scholar 

  21. Ho MH, Chang HC, Chang YC, Claudia J, Lin TC, Chang PC. PDGF-metronidazole-encapsulated nanofibrous functional layers on collagen membrane promote alveolar ridge regeneration. Int J Nanomedicine. 2017;12:5525.

    Article  CAS  Google Scholar 

  22. Schkarpetkin D, Reise M, Wyrwa R, Völpel A, Berg A, Schweder M, Schnabelrauch M, Watts DC, Sigusch BW. Development of novel electrospun dual-drug fiber mats loaded with a combination of ampicillin and metronidazole. Dent Mater. 2016;32:951.

    Article  CAS  Google Scholar 

  23. Giram PS, Shitole A, Nande SS, Sharma N, Garnaik B. Fast dissolving moxifloxacin hydrochloride antibiotic drug from electrospun Eudragit L-100 nonwoven nanofibrous Mats. Mat Sci Eng C. 2018;92:526.

    Article  CAS  Google Scholar 

  24. Shitole AA, Giram PS, Raut PW, Rade PP, Khandwekar AP, Sharma N, Garnaik B. Clopidrogel eluting electrospun Polyurethane/Polyethylene glycol thromboresistant, hemocompatible nanofibrous scaffolds. J Bio Appl. 2019;33:1327.

    Article  CAS  Google Scholar 

  25. Zhang L, Yan J, Yin Z, Tang C, Guo Y, Li D, Wei B, Xu Y, GU Q, Wang L. Electrospun vancomycin-loaded coating on titanium implants for the prevention of implant associated infections. Int J Nanomedicine. 2014;9:3027.

    CAS  Google Scholar 

  26. Shen X, Yu D, Zhu L, Branford-White C, White K, Chatterton NP. Electrospun diclofenac sodium loaded Eudragit® L 100–55 nanofibers for colon-targeted drug delivery. Int J Pharm. 2011;408:200.

    Article  CAS  Google Scholar 

  27. Yang DJ, Xiong CD, Govender T, Wang YZ. Preparation and drug-delivery potential of metronidazole-loaded PELA triblock co-polymeric electrospun membranes. J Biomater Sci Polym Ed. 2009;20:1321.

    Article  CAS  Google Scholar 

  28. Dewan I, Islam MM,  Al-Hasan M,  Nath J,  Sultana S,  Rana MS. Surface deposition and coalescence and coacervation phase separation methods: In Vitro Study and Compatibility Analysis of Eudragit RS30D, Eudragit RL30D, and Carbopol-PLA Loaded Metronidazole Microspheres. J Pharm (Cairo). 2015;2015:254930.

  29. Mehta R, Chawla A, Sharma P, Pawar P. Formulation and in vitro evaluation of Eudragit S-100 coated naproxen matrix tablets for colon-targeted drug delivery system. J Adv Pharm Technol Res. 2013;4:31.

    Article  CAS  Google Scholar 

  30. Payab S, Davaran S, Tanhaei A, Fayyazi B, Jahangiri A, Farzaneh A, Adibkia K. Triamcinolone acetonide–Eudragit® RS100 nanofibers and nanobeads: morphological and physicochemical characterization. Artif Cells Nanomed Biotechnol. 2016;44:362.

    Article  CAS  Google Scholar 

  31. Chou SF, Woodrow KA. Relationships between mechanical properties and drug release from electrospun fibers of PCL and PLGA blends. J Mech Behav Biomed Mater. 2017;65:724.

    Article  CAS  Google Scholar 

  32. Tort S, Acartürk F, Beşikci A. Evaluation of three-layered doxycycline-collagen loaded nanofiber wound dressing. Int J Pharm. 2017;529:642.

  33. Tan EP, Ng SY, Lim CT. Tensile testing of a single ultrafine polymeric fiber. Biomaterials. 2005;13:1453.

    Article  Google Scholar 

  34. Lim CT, Tan EPS, Ng SY. Effects of crystalline morphology on the tensile properties of electrospun polymer nanofibers. Appl Phys Lett. 2008;92:141908. https://doi.org/10.1063/1.2857478.

  35. Han D, Steckl AJ. Selective pH-responsive core−sheath nanofiber membranes for chem/bio/med applications: targeted delivery of functional molecules. ACS Appl Mater Interfaces. 2017;9:42653.

    Article  CAS  Google Scholar 

  36. Cesare FD, Mattia ED, Zussman E, Macagnano A. A study on the dependence of bacteria adhesion on the polymer nanofiber diameter. Environ Sci Nano. 2019;6:778.

    Article  Google Scholar 

  37. Xue J, He M, Niu Y, Liu H, Crawford A, Coates P, Chen D, Shi R, Zhang L. Preparation and in vivo efficient anti-infection property of GTR/GBR implant made by metronidazole loaded electrospun polycaprolactone nanofiber membrane. Int J Pharm. 2014;475:566.

    Article  CAS  Google Scholar 

Download references

Acknowledgements

Ms. Priyanka P. Rade gratefully acknowledges the Department of Science and Technology, New Delhi, India for the award of DST-INSPIRE fellowship (IF160594) for her doctoral research. The authors also gratefully acknowledge LIA MATSUCAT, France for the collaboration. The authors express their heartfelt gratitude to Evonik Industries, Mumbai, India, for providing Eudragit S 100 as a gift sample.

Author information

Authors and Affiliations

  1. Polymer Science and Engineering Division, CSIR- National Chemical Laboratory, Pune, 411008, India

    Priyanka P. Rade, Prabhanjan S. Giram & Baijayantimala Garnaik

  2. Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India

    Priyanka P. Rade, Prabhanjan S. Giram & Baijayantimala Garnaik

  3. Symbiosis School of Biological Sciences, Symbiosis International (Deemed University), Pune, 412115, India

    Ajinkya A. Shitole & Neeti Sharma

Authors
  1. Priyanka P. Rade
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Prabhanjan S. Giram
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Ajinkya A. Shitole
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Neeti Sharma
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. Baijayantimala Garnaik
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Baijayantimala Garnaik.

Ethics declarations

Conflict of interest

The author(s) declared no potential conflicts of interest with respect to the research, authorship, and/or publication of this article.

Supplementary Information

Below is the link to the electronic supplementary material.

Supplementary file1 (DOC 2092 kb)

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Rade, P.P., Giram, P.S., Shitole, A.A. et al. Physicochemical and in Vitro Antibacterial Evaluation of Metronidazole Loaded Eudragit S-100 Nanofibrous Mats for the Intestinal Drug Delivery. Adv. Fiber Mater. 4, 76–88 (2022). https://doi.org/10.1007/s42765-021-00090-y

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s42765-021-00090-y

Keywords

Search

Navigation