Skip to main content
NCBI home page
AAPS PharmSciTech logoLink to AAPS PharmSciTech
. 2007 Mar 16;8(1):E147–E154. doi: 10.1208/pt0801022

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

Vishnu M Patel 1,✉, Bhupendra G Prajapati 1, Madhabhai M Patel 1
PMCID: PMC2750433  PMID: 17408221

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

Full Text

The Full Text of this article is available as a PDF (216.4 KB).

References

  • 1.Anders R, Merkle HP. Evaluation of laminated mucoadhesive patches for buccal drug delivery. Int J Pharm. 1989;49:231–240. doi: 10.1016/0378-5173(89)90347-5. [DOI] [Google Scholar]
  • 2.Chen WG, Hwang G. Adhesive and in vitro release characteristics of propranolol bioadhesive disc system. Int J Pharm. 1992;82:61–66. doi: 10.1016/0378-5173(92)90072-A. [DOI] [Google Scholar]
  • 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. doi: 10.1016/S0378-5173(99)00211-2. [DOI] [PubMed] [Google Scholar]
  • 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. doi: 10.3109/03639049409042682. [DOI] [Google Scholar]
  • 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.Nagai T, Konishi R. Buccal/gingival drug delivery systems. J Control Release. 1987;6:353–360. doi: 10.1016/0168-3659(87)90088-5. [DOI] [Google Scholar]
  • 7.Harris D, Robinson JR. Drug delivery via the mucous membranes of the oral cavity. J Pharm Sci. 1992;81:1–10. doi: 10.1002/jps.2600810102. [DOI] [PubMed] [Google Scholar]
  • 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. doi: 10.3109/03639049809085621. [DOI] [PubMed] [Google Scholar]
  • 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. doi: 10.3109/03639048309046323. [DOI] [Google Scholar]
  • 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. doi: 10.1248/cpb.31.4561. [DOI] [PubMed] [Google Scholar]
  • 11.Bremecker KD, Strempel H, Klein G. Novel concept for a mucosal adhesive ointment. J Pharm Sci. 1984;73:548–552. doi: 10.1002/jps.2600730429. [DOI] [PubMed] [Google Scholar]
  • 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. [PubMed] [Google Scholar]
  • 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. doi: 10.3109/03639048809151972. [DOI] [Google Scholar]
  • 14.Desai KGH, Kumar TMP. Preparation and evaluation of a novel buccal adhesive system. AAPS PharmSciTech. 2004;5:35–35. doi: 10.1208/pt050335. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 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. doi: 10.1016/S0168-3659(98)00044-3. [DOI] [PubMed] [Google Scholar]
  • 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. doi: 10.1002/bdd.2510070605. [DOI] [PubMed] [Google Scholar]
  • 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. doi: 10.1002/cpt1978246668. [DOI] [PubMed] [Google Scholar]
  • 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.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. 2007;22:445–450. doi: 10.3109/03639049609069353. [DOI] [Google Scholar]
  • 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. doi: 10.1111/j.2042-7158.1991.tb03514.x. [DOI] [PubMed] [Google Scholar]
  • 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. doi: 10.1016/S0378-5173(98)00343-3. [DOI] [PubMed] [Google Scholar]
  • 22.Pharmacopoeia of India. New Delhi, India: Controller of Publications Ministry of Health and Welfare, Govemment of India; 1996:634.
  • 23.Guo JH, Cooklock M. The effect of backing materials and multilayered systems on the characteristics of bioadhesive buccal patches. J Pharm Pharmacol. 2007;48:255–257. doi: 10.1111/j.2042-7158.1996.tb05912.x. [DOI] [PubMed] [Google Scholar]
  • 24.Peppas NA, Bury PA. Surface interfacial and molecular aspects of polymer bioadhesion on soft tissues. J Control Release. 1985;2:257–275. doi: 10.1016/0168-3659(85)90050-1. [DOI] [Google Scholar]
  • 25.Park H, Robinson JR. Mechanisms of bioadhesion of poly(acrylic acid) hydrogels. Pharm Res. 1987;4:457–464. doi: 10.1023/A:1016467219657. [DOI] [PubMed] [Google Scholar]
  • 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.Peppas NA. Analysis of Fickian and non-Fickian drug release from polymers. Pharm Acta Helv. 1985;60:110–111. [PubMed] [Google Scholar]
  • 28.Choi HG, Kim CK. Development of omeprazole buccal adhesive tablets with stability enhancement in human saliva. J Control Release. 2000;68:397–404. doi: 10.1016/S0168-3659(00)00276-5. [DOI] [PubMed] [Google Scholar]
  • 29.Anlar S, Capan Y, Hincal A. Physico-chemical and bioadhesive properties of polyacrylic acid polymers. Pharmazie. 1993;48:285–287. [PubMed] [Google Scholar]

Articles from AAPS PharmSciTech are provided here courtesy of American Association of Pharmaceutical Scientists

RESOURCES