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AAPS PharmSciTech

, Volume 8, Issue 1, pp E147–E154 | Cite as

Formulation, evaluation, and comparison of bilayered and multilayered mucoadhesive buccal devices of propranolol hydrochloride

  • Vishnu M. PatelEmail author
  • Bhupendra G. Prajapati
  • Madhabhai M. Patel
Article

Abstract

The purpose of this research work was to establish mucoadhesive buccal devices of propranolol hydrochloride (PRH) in the forms of bilayered and multilayered tablets. The tablets were prepared using sodium carboxymethylcellulose (SCMC) and Carbopol-934 (CP) as bioadhesive polymers to impart mucoadhesion and ethyl cellulose (EC) to act as an impermeable backing layer. Buccal devices were evaluated by different parameters such as weight uniformity, content uniformity, thickness, hardness, surface pH, swelling index, ex vivo mucoadhesive strength, ex vivo mucoadhesion time, in vitro drug release, and in vitro drug permeation. As compared with bilayered tablets, multilayered tablets showed slow release rate of drug with improved ex vivo bioadhesive strength and enhanced ex vivo mucoadhesion time. The mechanism of drug release was found to be non-Fickian diffusion (value of n between 0.5 and 1.0) for both the buccal devices. The stability of drug in both the optimized buccal devices was tested for 6 hours in natural human saliva; both the buccal devices were found to be stable in natural human saliva. The present study concludes that mucoadhesive buccal devices of PRH can be a good way to bypass the extensive hepatic first-pass metabolism and to improve the bioavailability of PRH.

Keywords

Bilayered buccal tablet multilayered buccal tablet buccal delivery mucoadhesion propranolol hydrochloride 

References

  1. 1.
    Anders R, Merkle HP. Evaluation of laminated mucoadhesive patches for buccal drug delivery.Int J Pharm. 1989;49:231–240.CrossRefGoogle Scholar
  2. 2.
    Chen WG, Hwang G. Adhesive and in vitro release characteristics of propranolol bioadhesive disc system.Int J Pharm. 1992;82:61–66.CrossRefGoogle Scholar
  3. 3.
    Alur HH, Pather SI, Mitra AK. Transmucosal sustained-delivery of chlorpheniramine maleate in rabbits using a novel natural mucoadhesive gum as an excipient in buccal tablets.Int J Pharm. 1999;188:1–10.CrossRefGoogle Scholar
  4. 4.
    Guo JH. Bioadhesive polymer buccal patches for buprenorphine-controlled delivery: formulation in vitro adhesion and release properties.Drug Dev Ind Pharm. 1994;20:2809–2821.CrossRefGoogle Scholar
  5. 5.
    Ahuja A, Dorga M, Agarwal SP. Development of buccal tablets of diltiazem hydrochloride.Indian J Pharm Sci. 1995;57:26–30.Google Scholar
  6. 6.
    Nagai T, Konishi R. Buccal/gingival drug delivery systems.J Control Release. 1987;6:353–360.CrossRefGoogle Scholar
  7. 7.
    Harris D, Robinson JR. Drug delivery via the mucous membranes of the oral cavity.J Pharm Sci. 1992;81:1–10.CrossRefGoogle Scholar
  8. 8.
    Dortune B, Ozer L, Uyanik N. Development and in vitro evaluation of a buccoadhesive pindolol tablet formulation.Drug Dev Ind Pharm. 1998;24:281–288.Google Scholar
  9. 9.
    Schor JM, Davis SS, Nigalaye A, Bolton S. Susadrin transmucosal tablets (nitroglycerin in synchron-controlled release base).Drug Dev Ind Pharm. 1983;9:1359–1377.CrossRefGoogle Scholar
  10. 10.
    Ishida M, Nambu N, Nagai T. Highly viscous gel ointment containing Carbopol for application to the oral mucosa.Chem Pharm Bull (Tokyo). 1983;31:4561–4564.Google Scholar
  11. 11.
    Bremecker KD, Strempel H, Klein G. Novel concept for a mucosal adhesive ointment.J Pharm Sci. 1984;73:548–552.CrossRefGoogle Scholar
  12. 12.
    Gu JM, Robinson JR, Leung SHS. Binding of acrylic polymers to mucin/epithelial surfaces: structure-property relationships.Crit Rev Ther Drug Carrier Syst. 1988;5:21–67.Google Scholar
  13. 13.
    Duchene DE, Touchard F, Pappas NA. Pharmaceutical and medical aspects of bioadhesive systems for drug administration.Drug Dev Ind Pharm. 1988;14:283–318.CrossRefGoogle Scholar
  14. 14.
    Desai KGH, Kumar TMP. Preparation and evaluation of a novel buccal adhesive system.AAPS PharmSciTech. 2004;5:article 35.CrossRefGoogle Scholar
  15. 15.
    Remunan-Lopez C, Portero A, Vila-Jato JL, Alonso MJ. Design and evaluation of chitosan/ethylcellulose mucoadhesive bilayered devices for buccal drug delivery.J Control Release. 1998;55:143–152.CrossRefGoogle Scholar
  16. 16.
    Cid E, Mella F, Lucchini L, Carcamo M, Monasterio J. Plasma concentrations and bioavailability of propranolol by oral, rectal and intravenous administration in man.Biopharm Drug Dispos. 1986;7:559–566.CrossRefGoogle Scholar
  17. 17.
    Walle T, Conradi EC, Walle UK, Fagan TC, Gaffney TE. The predictable relationship between plasma levels and dose during chronic propranolol therapy.Clin Pharmacol Ther. 1978;24:668–677.Google Scholar
  18. 18.
    Gupta A, Garg S, Khar RK. Measurement of bioadhesive strength of muco-adhesive buccal tablets: design of an in-vitro assembly.Indian Drugs. 1992;30:152–155.Google Scholar
  19. 19.
    Parodi B, Russo E, Caviglioli G, Cafaggi S, Bignardi G. Development and characterization of a buccoadhesive dosage form of oxycodone hydrochloride.Drug Dev Ind Pharm. 1996;22:445–450.CrossRefGoogle Scholar
  20. 20.
    Bottenberg P, Cleymaet R, Muynek CD, Remon JP, Coomans D, Slop D. Development and testing of bioadhesive, fluoride-containing slow-release tablets for oral use.J Pharm Pharmacol. 1991;43: 457–464.Google Scholar
  21. 21.
    Han RY, Fang JY, Sung KC, Hu OYP. Mucoadhesive buccal disks for novel nalbuphine prodrug controlled delivery: effect of formulation variables on drug release and mucoadhesive performance.Int J Pharm. 1999;177:201–209.CrossRefGoogle Scholar
  22. 22.
    Pharmacopoeia of India. New Delhi, India: Controller of Publications Ministry of Health and Welfare, Govemment of India; 1996:634.Google Scholar
  23. 23.
    Guo JH, Cooklock M. The effect of backing materials and multilayered systems on the characteristics of bioadhesive buccal patches.J Pharm Pharmacol. 1996;48:255–257.Google Scholar
  24. 24.
    Peppas NA, Bury PA. Surface interfacial and molecular aspects of polymer bioadhesion on soft tissues.J Control Release. 1985;2:257–275.CrossRefGoogle Scholar
  25. 25.
    Park H, Robinson JR. Mechanisms of bioadhesion of poly(acrylic acid) hydrogels.Pharm Res. 1987;4:457–464.CrossRefGoogle Scholar
  26. 26.
    Ilango R, Kavimani S, Mullaicharam AR, Jayakar B. In vitro studies on buccal strips of glibenclamide using chitosan.Indian J Pharm Sci. 1997;59:232–235.Google Scholar
  27. 27.
    Peppas NA. Analysis of Fickian and non-Fickian drug release from polymers.Pharm Acta Helv. 1985;60:110–111.Google Scholar
  28. 28.
    Choi HG, Kim CK. Development of omeprazole buccal adhesive tablets with stability enhancement in human saliva.J Control Release. 2000;68:397–404.CrossRefGoogle Scholar
  29. 29.
    Anlar S, Capan Y, Hincal A. Physico-chemical and bioadhesive properties of polyacrylic acid polymers.Pharmazie. 1993;48:285–287.Google Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2007

Authors and Affiliations

  • Vishnu M. Patel
    • 1
    Email author
  • Bhupendra G. Prajapati
    • 1
  • Madhabhai M. Patel
    • 1
  1. 1.S.K. Patel College of Pharmaceutical Education & ResearchGanpat UniversityKherva, MehsanaIndia

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