The relationship between mucoadhesive polymers and surface coating in tablets for the controlled colonic delivery of a poorly water-soluble drug

Abstract

Background

The mucoadhesive polymers play an important role in targeted and controlled drug delivery.

Objectives

This study aimed to investigate the drug release behaviour and interpret the role of mucoadhesive polymers involved in the coating layer of mucoadhesive tablets for the sustained release of a poorly water-soluble drug.

Methods

A solid dispersion of prednisolone and zein was used in the core tablets created with two mucoadhesive polymers, which included Carbopol 940 and hydroxypropyl methylcellulose K4M. In addition, the properties of a single-layer coating, created from the combination of zein and Kollicoat MAE 100P to delay release through the upper parts of the gastrointestinal tract, were investigated in the presence of the above mucoadhesive polymers; these properties included drug dissolution, mucoadhesion, surface morphology, swelling and erosion.

Results

The mucoadhesive polymer concentrations and types were integrated not only into the core tablets through a swelling/erosion mechanism but also into the surface polymer coatings for controlled drug release. HPMC was preferred in the formulations due to the ability to form pores on the surface coating, allowing water uptake so that the coating could control drug release for a later stage via a swelling/erosion mechanism.

Conclusion

The proposed mechanism determined in this project could be beneficial in the selection of polymers for applications targeting the colon with coated mucoadhesive tablets.

Graphical abstract

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References

  1. 1.

    Felton LA. Film coating of oral solid dosage forms. Encyclopedia of Pharmaceutical Technology. 2006;3:1729–47.

    Google Scholar 

  2. 2.

    Kinget R, Kalala W, Vervoort L, Van den Mooter G. Colonic drug targeting. J Drug Target. 1998;6(2):129–49.

    CAS  Article  Google Scholar 

  3. 3.

    Shuddhodana JZ. Alginate-coating of artemisinin-loaded cochleates results in better control over gastro-intestinal release for effective oral delivery. Journal of Drug Delivery Science and Technology. 2019;52:27–36.

    CAS  Article  Google Scholar 

  4. 4.

    Kazlauske J, Gårdebjer S, Almer S, Larsson A. The importance of the molecular weight of ethyl cellulose on the properties of aqueous-based controlled release coatings. Int J Pharm. 2017;519(1):157–64.

    CAS  Article  Google Scholar 

  5. 5.

    Xu Y, Shrestha N, Préat V, Beloqui A. Overcoming the intestinal barrier: a look into targeting approaches for improved oral drug delivery systems. J Control Release. 2020;322:486–508.

    CAS  Article  Google Scholar 

  6. 6.

    Yang L, Chu JS, Fix JA. Colon-specific drug delivery: new approaches and in vitro/in vivo evaluation. Int J Pharm. 2002;235(1–2):1–15.

    CAS  Article  Google Scholar 

  7. 7.

    Radtke J, Wiedey R, Kleinebudde P. Effect of coating time on inter- and intra-tablet coating uniformity. Eur J Pharm Sci. 2019;137:104970.

    CAS  Article  Google Scholar 

  8. 8.

    Tran PHL, Duan W, Lee BJ, Tran TTD. Drug stabilization in the gastrointestinal tract and potential applications in the colonic delivery of oral zein-based formulations. Int J Pharm. 2019;569:118614.

    CAS  Article  Google Scholar 

  9. 9.

    Palugan L, Cerea M, Zema L, Gazzaniga A, Maroni A. Coated pellets for oral colon delivery. Journal of Drug Delivery Science and Technology. 2015;25:1–15.

    CAS  Article  Google Scholar 

  10. 10.

    Khan MZI, Prebeg Ž, Kurjaković N. A pH-dependent colon targeted oral drug delivery system using methacrylic acid copolymers: I. manipulation of drug release using Eudragit® L100-55 and Eudragit® S100 combinations. J Control Release. 1999;58(2):215–22.

    CAS  Article  Google Scholar 

  11. 11.

    Shahdadi Sardou H, Akhgari A, Afrasiabi Garekani H, Sadeghi F. Screening of different polysaccharides in a composite film based on Eudragit RS for subsequent use as a coating for delivery of 5-ASA to colon. Int J Pharm. 2019;568:118527.

    CAS  Article  Google Scholar 

  12. 12.

    Phuong T, Thao T. The use of natural materials in film coating for controlled Oral drug release. Curr Med Chem. 2020;27:1–12.

    Article  Google Scholar 

  13. 13.

    Andrews GP, Laverty TP, Jones DS. Mucoadhesive polymeric platforms for controlled drug delivery. Eur J Pharm Biopharm. 2009;71(3):505–18.

    CAS  Article  Google Scholar 

  14. 14.

    Kurra P, Narra K, Puttugunta SB, Kilaru NB, Mandava BR. Development and optimization of sustained release mucoadhesive composite beads for colon targeting. Int J Biol Macromol. 2019;139:320–31.

    CAS  Article  Google Scholar 

  15. 15.

    de Oliveira Cardoso VM, Evangelista RC, Daflon Gremião MP, Stringhetti Ferreira Cury B. Insights into the impact of cross-linking processes on physicochemical characteristics and mucoadhesive potential of gellan gum/retrograded starch microparticles as a platform for colonic drug release. Journal of Drug Delivery Science and Technology. 2020;55:101445.

    Article  Google Scholar 

  16. 16.

    Shah KP, Chafetz L. Use of sparingly soluble salts to prepare oral sustained release suspensions. Int J Pharm. 1994;109(3):271–81.

    CAS  Article  Google Scholar 

  17. 17.

    Woertz C, Preis M, Breitkreutz J, Kleinebudde P. Assessment of test methods evaluating mucoadhesive polymers and dosage forms: an overview. Eur J Pharm Biopharm. 2013;85(3):843–53.

    CAS  Article  Google Scholar 

  18. 18.

    Ozeki T, Yuasa H, Kanaya Y. Controlled release from solid dispersion composed of poly (ethylene oxide)–Carbopol® interpolymer complex with various cross-linking degrees of Carbopol®. J Control Release. 2000;63(3):287–95.

    CAS  Article  Google Scholar 

  19. 19.

    Yu T, Andrews GP, Jones DS. Mucoadhesion and characterization of mucoadhesive properties. Mucosal Delivery of Biopharmaceuticals. Springer; 2014. p. 35–58.

  20. 20.

    Hägerström H, Edsman K. Interpretation of mucoadhesive properties of polymer gel preparations using a tensile strength method. J Pharm Pharmacol. 2001;53(12):1589–99.

    Article  Google Scholar 

  21. 21.

    Nguyen MNU, Tran PHL, Tran TTD. A single-layer film coating for colon-targeted oral delivery. Int J Pharm. 2019;559:402–9.

    CAS  Article  Google Scholar 

  22. 22.

    Nguyen MN-U, Van Vo T, Tran PH-L, Tran TT-D. Zein-based solid dispersion for potential application in targeted delivery. Journal of Pharmaceutical Investigation. 2017;47(4):357–64.

    CAS  Article  Google Scholar 

  23. 23.

    Leuner C, Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur J Pharm Biopharm. 2000;50(1):47–60.

    CAS  Article  Google Scholar 

  24. 24.

    Chary R, Vani G, Rao YM. In vitro and in vivo adhesion testing of mucoadhesive drug delivery systems. Drug Dev Ind Pharm. 1999;25(5):685–90.

    CAS  Article  Google Scholar 

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Acknowledgements

We would like to thank International University for the support to our studies. Dr. Phuong HL Tran is the recipient of Australian Research Council’s Discovery Early Career Researcher Award (project number DE160100900).

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Correspondence to Thao T. D. Tran.

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Phan, T.Q., Tran, P.H.L. & Tran, T.T.D. The relationship between mucoadhesive polymers and surface coating in tablets for the controlled colonic delivery of a poorly water-soluble drug. DARU J Pharm Sci (2020). https://doi.org/10.1007/s40199-020-00360-x

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Keywords

  • Mucoadhesive
  • Sustained release
  • Solid dispersion
  • Single-coated layer
  • Delayed release