Skip to main content
Log in

Formulation and In Vitro Evaluation of Xanthan Gum or Carbopol 934-Based Mucoadhesive Patches, Loaded with Nicotine

  • Research Article
  • Theme: Advanced Technologies for Oral Controlled Release
  • Published:
AAPS PharmSciTech Aims and scope Submit manuscript

Abstract

Bilayer nicotine mucoadhesive patches were prepared and evaluated to determine the feasibility of the formulation as a nicotine replacement product to aid in smoking cessation. Nicotine patches were prepared using xanthan gum or carbopol 934 as a mucoadhesive polymers and ethyl cellulose as a backing layer. The patches were evaluated for their thickness, weight and content uniformity, swelling behavior, drug–polymers interaction, adhesive properties, and drug release. The physicochemical interactions between nicotine and the polymers were investigated by Fourier transform infrared (FTIR) spectroscopy. Mucoadhesion was assessed using two-arm balance method, and the in vitro release was studied using the Franz cell. FTIR revealed that there was an acid base interaction between nicotine and carbopol as well as nicotine and xanthan. Interestingly, the mucoadhesion and in vitro release studies indicated that this interaction was strong between the drug and carbopol whereas it was weak between the drug and xanthan. Loading nicotine concentration to non-medicated patches showed a significant decrease in the mucoadhesion strength of carbopol patches and no significant effect on the mucoadhesion strength of xanthan patches. In vitro release studies of the xanthan patches showed a reasonable fast initial release profile followed by controlled drug release over a 10-h period.

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.

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

Similar content being viewed by others

REFERENCES

  1. Yildiz D. Nicotine, its metabolism and an overview of its biological effects. (Review). Toxicon. 2004;43:619–32.

    Article  PubMed  CAS  Google Scholar 

  2. Galanti L. Tobacco smoking cessation management: integrating varenicline in current practice. Vasc Health Risk Manag. 2008;4(4):837–45. PMCID: PMC2597768.

    PubMed  CAS  Google Scholar 

  3. D’Orlando KJ, Fox BS. Tolerability and pharmacokinetics of single and repeated doses of nicotine with the straw, a novel nicotine replacement product. Nicotine Tob Res. 2004;6(1):63–70.

    Article  PubMed  Google Scholar 

  4. Hajek P, West R, Foulds J, Nilsson F, Burrows S, Meadow A. Randomized comparative trial of nicotine polacrilex, a transdermal patch, nasal spray and an inhaler. Arch Intern Med. 1999;159:2033–8.

    Article  PubMed  CAS  Google Scholar 

  5. Park CR, Munday DL. Development and evaluation of a biphasic buccal adhesive tablet for nicotine replacement therapy. Int J Pharmaceut. 2002;237:215–26.

    Article  CAS  Google Scholar 

  6. Hao J, Heng P. Buccal delivery systems. Drug Dev Ind Pharm. 2003;29(8):821–32.

    Article  PubMed  CAS  Google Scholar 

  7. Shojaei A. Buccal mucosa as a route for systemic drug delivery: a review. J Pharm Pharm Sci. 1998;1(1):15–30.

    PubMed  CAS  Google Scholar 

  8. Xiang J, Fang X, Li X. Transbuccal delivery of 2′, 3′-dideoxycytidine: in vitro permeation study and histological investigation. Int J Pharmaceut. 2002;231:57–66.

    Article  CAS  Google Scholar 

  9. Veuillez F, Kalia Y, Jacques Y, Deshusses J, Buri P. Factors and strategies for improving buccal absorption of peptides. Eur J Pharm Biopharm. 2001;51:93–109.

    Article  PubMed  CAS  Google Scholar 

  10. Swarbrick A. Oral mucosal drug delivery. New York: Marcel Dekker; 1996.

    Google Scholar 

  11. Shin S, Kim J, Oh I. Mucoadhesive and physicochemical characterization of carbopol-poloxamer gels containing triamcinolone acetonide. Drug Dev Ind Pharm. 2000;26(3):307–12.

    Article  PubMed  CAS  Google Scholar 

  12. Park CR, Munday DL. Evaluation of selected Polysaccharide Excipients in buccoadhesive tablets for sustained release of nicotine. Drug Dev Ind Pharm. 2004;30(6):609–17.

    Article  PubMed  CAS  Google Scholar 

  13. Smart JD. Recent developments in the use of bioadhesive systems for delivery of drugs to the oral cavity. Crit Rev Ther Drug Carrier Syst. 2004;21:319–44.

    Article  PubMed  CAS  Google Scholar 

  14. Roubroeks JP, Andersson R, Mastromauro DI, Christensen BE, Aman P. Molecular weight, structure and shape of oat (1 → 3), (1 → 4)-b-d-glucan fractions obtained by enzymatic degradation with (1 → 4)-b-d-glucan 4-glucanohydrolase from Trichoderma reesei. Carbohydr Polym. 2001;46:275–85.

    Article  CAS  Google Scholar 

  15. Perez-Marcos B, Gutierrez C, Gomez-Amoza JL, Martinez-Pacheco R, Souto C, Concheiro A. Usefulness of certain varieties of Carbopol in the formulation of hydrophilic furosemide matrices. Int J Pharmaceut. 1991;67(2):113–21.

    Article  CAS  Google Scholar 

  16. Lee J, Park J, Robinson R. Bioadhesive-based dosage forms; the next generation. J Pharm Sci. 2000;89:850–66.

    Article  PubMed  CAS  Google Scholar 

  17. Hao J, Paul Heng WS. Buccal delivery systems. Drug Dev Ind Pharm. 2003;29(8):821–32.

    Article  PubMed  CAS  Google Scholar 

  18. Majithiya RJ, Ghosh PK, Umrethia ML, Murthy RS. Thermoreversible-mucoadhesive gel for nasal delivery of sumatriptan. AAPS PharmSciTech. 2006;7(3):67. doi:10.1208/pt070367.

    Article  PubMed  Google Scholar 

  19. Abu-Huwaij R, Assaf S, Salem M, Sallam A. Potential mucoadhesive dosage form of lidocaine hydrochloride: II. In vitro and in vivo evaluation. Drug Dev Ind Pharm. 2007;33(4):437–48.

    Article  PubMed  CAS  Google Scholar 

  20. Patel VM, Prajapati BG, Patel HV, Patel KM. Mucoadhesive bilayer tablets of propranolol hydrochloride. AAPS PharmSciTech. 2007;8(3):77. doi:10.1208/pt0803077.

    CAS  Google Scholar 

  21. Tamburic S, Craig D. A comparison of different in vitro methods for measuring mucoadhesive performance. Eur J Pharm Biopharm. 1997;44:159–67.

    Article  CAS  Google Scholar 

  22. Parodi B, Russo E, Caviglioli G, Cafaggi S, Bigbardi G. Development and characterization of a buccoadhesive dosage form of oxycodane hydrochloride. Drug Dev Ind Pharm. 1996;22(5):445–50.

    Article  CAS  Google Scholar 

  23. Emami J, Varshosaz J, Saljoughian N. Development and evaluation of controlledrelease buccoadhesive verapamil hydrochloride tablets. DARU. 2008;16(2):60–9.

    CAS  Google Scholar 

  24. Desai KGH, Kumar TMP. Preparation and evaluation of a novel buccal adhesive system. AAP PharmSciTech. 2004;5(3):35.

    Google Scholar 

  25. Agarwal V, Mishra B. Design, development, and biopharmaceutical properties of buccoadhesive compacts of pentazocine. Drug Dev Ind Pharm. 1999;25(6):701–9.

    Article  PubMed  CAS  Google Scholar 

  26. Perioli L, Ambrogi V, Angelici A, Ricci M. Development of mucoadhesive patches for buccal administration of ibuprofen. J Control Release. 2004;99(1):73–82.

    Article  PubMed  CAS  Google Scholar 

  27. Okamoto H, Nakamori T, Arakawa Y, Iida K, Danjo K. Development of polymer film dosage forms of lidocaine for buccal administration: II. Comparison of preparation methods. J Pharm Sci. 2002;91(11):2424–32.

    Article  PubMed  CAS  Google Scholar 

  28. Abu-Huwaij R, Assaf S, Salem M, Sallam A. Potential mucoadhesive dosage form of lidocaine hydrochloride: I. Mucoadhesive and physicochemical characterization. Drug Dev Ind Pharm. 2007;33(8):855–64.

    Article  PubMed  CAS  Google Scholar 

  29. Harding S. Mucoadhesive interactions. Biochem Soc Trans. 2003;31(5):1036–42.

    Article  PubMed  CAS  Google Scholar 

  30. Ceulemans J, Vinckier I, Ludwig A. The use of xanthan gum in an ophthalmic liquid dosage form: rheological characterization of the interaction with mucin. J Pharm Sci. 2002;91(4):1117–27.

    Article  PubMed  CAS  Google Scholar 

  31. Liabot J, Manzo R, Allemandi D. Double layered mucoadhesive tablets containing nystatin. AAPS PharmSciTech. 2002;3(3):22.

    Article  Google Scholar 

  32. Salamat-Miller N, Chittchang M, Johnston TP. The use of mucoadhesive polymers in buccal drug delivery. Adv Drug Deliv Rev. 2005;57:1666–91.

    Article  PubMed  CAS  Google Scholar 

  33. Guo J. Bioadhesive polymer buccal patches for buprenorphine controlled delivery: formulation, in vitro adhesion and release properties. Drug Dev Ind Pharm. 1994;20(18):2809–21.

    Article  CAS  Google Scholar 

  34. Richardson RK, Ross-Murphy SB. Non-linear viscoelasticity of polysaccharide solutions. 2: xanthan polysaccharide solutions. Int J Biol Macromol. 1987;9:257–64.

    Article  CAS  Google Scholar 

  35. Lopez C, Portero A, Jato J, Alonso M. Design and evaluation of chitosan/ethylcellulose mucoadhesive bilayered devices for buccal drug delivery. J Control Release. 1998;55:143–52.

    Article  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Rana M. Obaidat.

Additional information

Guest Editors: Michael Repka, Joseph Reo, Linda Felton, and Stephen Howard

Rights and permissions

Reprints and permissions

About this article

Cite this article

Abu-Huwaij, R., Obaidat, R.M., Sweidan, K. et al. Formulation and In Vitro Evaluation of Xanthan Gum or Carbopol 934-Based Mucoadhesive Patches, Loaded with Nicotine. AAPS PharmSciTech 12, 21–27 (2011). https://doi.org/10.1208/s12249-010-9534-5

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1208/s12249-010-9534-5

KEY WORDS

Navigation