Skip to main content
PMC home page
AAPS PharmSciTech logoLink to AAPS PharmSciTech
. 2004 Apr 29;5(3):1–9. doi: 10.1208/pt050335

Preparation and evaluation of a novel buccal adhesive system

Kashappa Gould H Desai 1,✉, T M Pramod Kumar 2
PMCID: PMC2750259  PMID: 15760069

Abstract

The aim of the present study was to prepare and evaluate a novel buccal adhesive system (NBAS) containing propranolol hydrochloride (PH). A special punch was fabricated and used while preparing an NBAS. Solubility of PH in phosphate buffer solution (pH 6.6), partition coefficient between phosphate buffer (pH 6.6) and 1-octanol, and permeability coefficient through the porcine buccal mucosa were performed and found to be 74.66 mg/mL, 5.17, and 5.6, respectively. Stability of NBAS was determined in natural human saliva, and it was found that both PH and device are stable in human saliva. NBAS was evaluated by weight uniformity, thickness, hardness, friability, swelling, mucoadhesive strength, in vitro drug release, and in vivo human acceptability studies. Swelling index was higher (4.4) for formulations containing hydroxyl propyl methyl cellulose (HPMC) K4M alone, and it decreases with its decreasing concentration in the NBAS. Mucoadhesive strength (MS) was measured by using a modified apparatus. All NBASs showed higher MS with porcine buccal mucosa when compared with that of rabbit buccal mucosa. NBASs containing carbopol (CP) 934P and HPMC K4M at the ratio of 1∶1 showed higher MS (44.76 g) with porcine buccal mucosa when compared with 1∶2 (39.76 g), 0∶1 (23.29 g), and 1∶0 (22.22 g) ratios, respectively. The mechanism of PH release was found to be by non-Fickian diffusion (value of “n” between 0.5 and 1.0) and followed first order kinetics. In vivo human acceptability study showed that the newly prepared NBAS was comfortable in the human buccal cavity. It can be concluded that NBAS is a superior, novel system that overcomes the draw-back associated with the conventional buccal adhesive tablet.

Keywords: buccal delivery, carbopol 934P, HPMC K4M, propranolol hydrochloride, mucoadhesion

Full Text

The Full Text of this article is available as a PDF (258.2 KB).

References

  • 1.Alur HH, Pather SI, Mitra AK, Johnston TP. 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]
  • 2.Benes L, Claustrat B, Horriere F, et al. Transmucosal, oral controlled release, and transdermal drug administration in human subjects: A cross-over study with melatonin. J Pharm Sci. 1997;86:1115–1119. doi: 10.1021/js970011z. [DOI] [PubMed] [Google Scholar]
  • 3.Alur HH, Pather SI, Mitra AK, Johnston TP. Evaluation of the gum from hakea gibbosa as a sustained release and mucoadhesive component in buccal tablets. Pharm Dev Technol. 1999;4:347–358. doi: 10.1081/PDT-100101370. [DOI] [PubMed] [Google Scholar]
  • 4.Gavini E, Sanna V, Juliano C, Bonferoni MC, Giunchedi P. Mucoadhesive vaginal tablets as veterinary delivery system for the controlled release of an antimicrobial drug, Acriflavine. AAPS PharmSciTech. 2002;3(3):E20–E20. doi: 10.1208/pt030320. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 5.Chowdary KPR, Rao YS. Design and in vitro and in vivo evaluation of mucoadhesive microcapsules of glipizide for oral controlled release: a technical note. AAPS PharmSciTech. 2003;4:E39–E39. doi: 10.1208/pt040339. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 6.Junginger HE, Hoogstraate JA, Verhoef JC. Recent advances in buccal drug delivery and absorption: In vitro and in vivo studies. J Control Release. 1999;62:149–159. doi: 10.1016/S0168-3659(99)00032-2. [DOI] [PubMed] [Google Scholar]
  • 7.Pramodkumar TM, Desai KGH, Shivakumar HG. Buccal permeation enhancers. Ind J Pharm Edu. 2002;36:147–151. [Google Scholar]
  • 8.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]
  • 9.Khanna R, Agarwal SP, Ahuja A. Preparation and evaluation of bioerodible buccal tablets containing clotrimazole. Int J Pharm. 1996;138:67–73. doi: 10.1016/0378-5173(96)04531-0. [DOI] [Google Scholar]
  • 10.Chen LLH, Chetty DJ, Chien YW. A mechanistic analysis to characterize oramucosal permeation properties. Int J Pharm. 1999;184:63–72. doi: 10.1016/S0378-5173(99)00091-5. [DOI] [PubMed] [Google Scholar]
  • 11.Giunchedi P, Juliano C, Gavini E, Cossu M, Sorrenti M. Formulation and in vivo evaluation of chlorhexidine buccal tablets prepared using drug-loaded chitosan microspheres. Eur J Pharm Biopharm. 2002;53:233–239. doi: 10.1016/S0939-6411(01)00237-5. [DOI] [PubMed] [Google Scholar]
  • 12.Martin L, Wilson CG, Koosha F, Uchegbu IF. Sustained buccal delivery of the hydrophobic drug denbufylline using physically cross-linked palmitoyl glycol chitosan hydrogels. Eur J Pharm Biopharm. 2003;55:35–45. doi: 10.1016/S0939-6411(02)00118-2. [DOI] [PubMed] [Google Scholar]
  • 13.Lee Y, Chien YW. Oral mucosal controlled delivery of LHRH by bilayer mucoadhesive polymer systems. J Control Release. 1995;37(3):251–261. doi: 10.1016/0168-3659(95)00082-8. [DOI] [Google Scholar]
  • 14.Park CR, Munday DL. Development and evaluation of a biphasic buccal adhesive tablet for nicotine replacement therapy. Int J Pharm. 2002;237:215–226. doi: 10.1016/S0378-5173(02)00041-8. [DOI] [PubMed] [Google Scholar]
  • 15.Minghetti P, Colombo A, Montanari L, Gaeta GM, Gombos F. Buccoadhesive slow-release tablets of acitretin: Design and in vivo evaluation. Int J Pharm. 1998;169(2):195–202. doi: 10.1016/S0378-5173(98)00119-7. [DOI] [Google Scholar]
  • 16.Llabot JM, Manzo RH, Allemandi DA. Double layered mucoadhesive tablets containing nystatin. AAPS PharmSciTech. 2002;3(3):E22–E22. doi: 10.1208/pt030322. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 17.Lopez CR, Portêro 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]
  • 18.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]
  • 19.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]
  • 20.Tanaka M, Yanagibashi N, Fukuda H, Nagai T. Absorption of salicylic acid through the oral mucous membrane of hamster cheek pouch. Chem Pharm Bull (Tokyo) 1980;28:1056–1061. doi: 10.1248/cpb.28.1056. [DOI] [PubMed] [Google Scholar]
  • 21.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]
  • 22.Mumtaz AM, Chung HS. Design of a dissolution apparatus suitable for in situ release study of triamcinolone acetonide from bioadhesive buccal tablets. Int J Pharm. 1995;121(2):129–139. doi: 10.1016/0378-5173(94)00406-U. [DOI] [Google Scholar]
  • 23.Kerec M, Bogataj M, Mugerle B, Gasperlin M, Mrhar A. Mucoadhesion on pig vesical mucosa: Influence of polycarbophil/calcium interactions. Int J Pharm. 2002;241:135–143. doi: 10.1016/S0378-5173(02)00231-4. [DOI] [PubMed] [Google Scholar]
  • 24.Spiegeleer BD, Vooren LV, Voorspoels J, Thoné D, Rosier J. Dissolution stability and IVIVC investigation of a buccal tablet. Anal Chim Acta. 2001;446:345–351. doi: 10.1016/S0003-2670(01)01074-1. [DOI] [Google Scholar]
  • 25.Schoenwald RD, Hung HS. In vitro corneal permeation of β-blocking agents. J Pharm Sci. 1983;72:1266–1271. doi: 10.1002/jps.2600721108. [DOI] [PubMed] [Google Scholar]
  • 26.Mahaguna V, Talbert RL, Peters JI, et al. Influence of hydroxypropyl methylcellulose polymer on in vitro and in vivo performance of controlled release tablets containing alprazolam. Eur J Pharm Biopharm. 2003;56:461–468. doi: 10.1016/S0939-6411(03)00116-4. [DOI] [PubMed] [Google Scholar]
  • 27.Park H, Robinson JR. Mechanisms of mucoadhesion of poly(acrylic acid) hydrogels. Pharm Res. 1987;4:457–464. doi: 10.1023/A:1016467219657. [DOI] [PubMed] [Google Scholar]
  • 28.Shojaei AH, Li X. Mechanisms of buccal mucoadhesion of novel copolymers of acrylic acid and polyethylene glycol monomethylether monomethacrylate. J Control Release. 1997;47(2):151–161. doi: 10.1016/S0168-3659(96)01626-4. [DOI] [Google Scholar]
  • 29.Agarwal V, Mishra B. Design, development, and biopharmaceutical properties of buccoadhesive compacts of pentazocine. Drug Dev Ind Pharm. 1999;25:701–709. doi: 10.1081/DDC-100102229. [DOI] [PubMed] [Google Scholar]
  • 30.Capan Y, Jiang G, Giovagnoli S, Na KH, DeLuca PP. Preparation and characterization of poly (D, L-lactide-co-glycolide) microspheres for controlled release of human growth hormones. AAPS PharmSciTech. 2003;4(2):E28–E28. doi: 10.1208/pt040228. [DOI] [PMC free article] [PubMed] [Google Scholar]

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

RESOURCES