Design and characterization of chitosan-containing mucoadhesive buccal patches of propranolol hydrochloride

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Design and characterization of chitosan-containing mucoadhesive buccal patches of propranolol hydrochloride

Mucoadhesive buccal patches containing propranolol hydrochloride were prepared using the solvent casting method. Chitosan was used as bioadhesive polymer and different ratios of chitosan to PVP K-30 were used. The patches were evaluated for their physical characteristics like mass variation, drug content uniformity, folding endurance, ex vivo mucoadhesion strength, ex vivo mucoadhesion time, surface pH, in vitro drug release, and in vitro buccal permeation study. Patches exhibited controlled release for a period of 7 h. The mechanism of drug release was found to be non-Fickian diffusion and followed the first-order kinetics. Incorporation of PVP K-30 generally enhanced the release rate. Swelling index was proportional to the concentration of PVP K-30. Optimized patches (F4) showed satisfactory bioadhesive strength of 9.6 ± 2.0 g, and ex vivo mucoadhesion time of 272 minutes. The surface pH of all patches was between 5.7 and 6.3 and hence patches should not cause irritation in the buccal cavity. Patches containing 10 mg of drug had higher bioadhesive strength with sustained drug release as compared to patches containing 20 mg of drug. Good correlation was observed between the in vitro drug release and in vitro drug permeation with a correlation coefficient of 0.9364. Stability study of optimized patches was done in human saliva and it was found that both drug and buccal patches were stable.

  • A. J. Hoogstraate, J. C. Verhoef, B. Tuk, A. Pijpers, L. A. M. G. van Leengoed, J. H. M. Verheijden, H. E. Junginger and H. E. Bodde, In vitro buccal delivery of fluorescein isothiocyanate - dextran 4400 with glycodeoxycholate as an absorption enhancer in pigs, J. Pharm. Sci. 85 (1996) 457-460.

  • J. Ali, R. K. Khar and A. Ahuja, Formulation and characterization of a buccoadhesive erodible tablet for the treatment of oral lesions, Pharmazie 53 (1998) 329-334.

  • Y. Kohda, H. Kobayashi, Y. Baba, H. Yuasa, T. Ozeki, Y. Kanaya and E. Sagara, Controlled release of lidocaine hydrochloride from buccal mucosa-adhesive films with solid dispersion, Int. J. Pharm. 15 (1983) 147-155.

  • M. M. Nair and Y. W. Chien, Development of anticandidal delivery systems. (II) Mucoadhesive devices for prolonged drug delivery in the oral cavity, Drug Dev. Ind. Pharm. 22 (1996) 243-253.

  • B. Parodi, E. Russo, G. Caviglioli, S. Cafaggi and G. Bignardi, Development and characterization of a buccoadhesive dosage form of oxycodone hydrochloride, Drug Dev. Ind. Pharm. 22 (1996) 445-450.

  • R. Hango, S. Kavimani, A. R. Mullaicharam and B. Jayakar, In vitro studies on buccal strips of glibenclamide using chitosan, Ind. J. Pharm. Sci. 59 (1997) 232-235.

  • K. D. Bremecker, H. Strempel and G. Klein, Novel concept for a mucosal adhesive ointment, J. Pharm. Sci. 73 (1984) 548-552.

  • S. C. Shin, J. P. Bum and J. S. Choi, Enhanced bioavailability by buccal administration of triamcinolone acetonide from the bioadhesive gels in rabbits, Int. J. Pharm. 209 (2000) 37-43.

  • J. M. Gu, J. R. Robinson and S. H. S. Leung, Binding of acrylic polymers to mucin/epithelial surfaces: Structure-property relationships, CRC Crit. Rev. Ther. Drug Carrier Systems 21 (1988) 21-67.

  • C. M. Lehr, J. A. Bouwstra, E. H. Schacht and H. E. Junginger, In vitro evaluation of mucoadhesive properties of chitosan and some other natural polymers, Int. J. Pharm. 78 (1992) 43-48.

  • R. A. A. Muzarelli, Chitin, Pergamon Press, Oxford 1977.

  • S. Hirano, H. Seino, I. Akiyama and I. Nonaka, Chitosan a Biocompatible Material for Oral and Intravenous Administrations: Progress in Biomedical Polymers, Plenum Press, New York 1990, pp. 283-289.

  • T. Nagai, Y. Sawayanagi and N. Nambu, Application of Chitin and Chitosan to Pharmaceutical Preparations: Chitin, Chitosan and Related Enzymes, Academic Press, Orlando 1984, pp. 21-39.

  • K. Y. Inouye, T. Machida, Sannan and T. Nagai, Buoyant sustained release tablets based on chitosan, Drug Des. Deliv. 2 (1988) 165-175.

  • C. Ramunan-Lopez and R. Bodmeier, Mechanical and water vapor transmission properties of polysaccharide films, Drug Dev. Ind. Pharm. 22 (1996) 1201-1209.

  • B. B. Hoffman and R. J. Lefkowitz, Goodman and Gillman's: The Pharmacological Basis of Therapeutics, 9th ed., Mc Graw-Hill, New Delhi 1994, pp. 128-130.

  • Y. Sawayanaga, N. Nambu and T. Nagai, Permeation of drugs through chitosan membranes, Chem. Pharm. Bull. 30 (1982) 3297-3301.

  • R. Khurana, A. Ahuja and R. K. Khar, Development and evaluation of mucoadhesive films of miconazole nitrate, Indian J. Pharm. Sci. 60 (2000) 449-453.

  • J. Kemken, A. Ziegler and B. W. Muller, Pharmacodynamic effects of transdermal bupranolol and timolol in vivo: comparison of micro emulsions and matrix patches as vehicles, Math. Find. Exp. Clin. Pharmacol. 13 (1991) 361-365.

  • Pharmacopoeia of India, 3rd ed., Controller of Publications, New Delhi 1996, p. 634.

  • A. S. Gupta, Garg and R. K. Khar, Measurement of bioadhesive strength of muco-adhesive buccal tablets: design of an in vitro assembly, Indian Drugs 30 (1992) 152-155.

  • R. Y. Han, J. Y. Fang, K. C. Sung and O. Y. P. Hu, Mucoadhesive buccal disks for novel nalbuphine prodrug controlled delivery: effect of formulation variables on drug release and mucoadhesive performance, Int. J. Pharm. 177 (1999) 201-209.

  • P. Bottenberg, R. Cleymaet, C. D. Muynek, J. P. Remon, D. Coomans and D. Slop, Development and testing of bioadhesive, fluoride containing slow-release tablets for oral use, J. Pharm. Pharmacol. 43 (1991) 457-464.

  • USP, 23/NF 18, USP Convention, Rockville 1995, pp. 1792-1795.

  • N. A. Peppas and P. A. Bury, Surface interfacial and molecular aspects of polymer bioadhesion on soft tissues, J. Control Rel. 2 (1985) 257-275.

  • H. Park and J. R. Robinson, Mechanisms of bioadhesion of poly(acrylic acid) hydrogels, Pharm. Res. 4 (1987) 457-464.

  • R. W. Korsmeyer, R. Gurny, E. Doelker, P. Buri and N. A. Peppas, Mechanisms of solute release from porous hydrophilic polymers, Int. J. Pharm. 15 (1983) 25-35.

  • N. A. Peppas, Analysis of Fickian and non-Fickian drug release from polymers, Pharm. Acta Helv. 60 (1985) 110-111.

Acta Pharmaceutica

The Journal of Croatian Pharmaceutical Society

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