Search tips
Search criteria 


Logo of aapspharmspringer.comThis journalToc AlertsSubmit OnlineOpen Choice
AAPS PharmSciTech. 2004 September; 5(3): 1–9.
Published online 2004 April 29. doi:  10.1208/pt050335
PMCID: PMC2750259

Preparation and evaluation of a novel buccal adhesive system


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[ratio]1 showed higher MS (44.76 g) with porcine buccal mucosa when compared with 1[ratio]2 (39.76 g), 0[ratio]1 (23.29 g), and 1[ratio]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.

Full Text

The Full Text of this article is available as a PDF (258K).

Selected References

These references are in PubMed. This may not be the complete list of references from this article.
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. [PubMed] [Cross Ref]
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. [PubMed] [Cross Ref]
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. [PubMed] [Cross Ref]
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. [PMC free article] [PubMed] [Cross Ref]
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. [PMC free article] [PubMed] [Cross Ref]
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. [PubMed] [Cross Ref]
7. Pramodkumar TM, Desai KGH, Shivakumar HG. Buccal permeation enhancers. Ind J Pharm Edu. 2002;36:147–151.
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. [Cross Ref]
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. [Cross Ref]
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. [PubMed] [Cross Ref]
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. [PubMed] [Cross Ref]
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. [PubMed] [Cross Ref]
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. [Cross Ref]
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. [PubMed] [Cross Ref]
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. [Cross Ref]
16. Llabot JM, Manzo RH, Allemandi DA. Double layered mucoadhesive tablets containing nystatin. AAPS PharmSciTech. 2002;3(3):E22–E22. doi: 10.1208/pt030322. [PMC free article] [PubMed] [Cross Ref]
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. [PubMed] [Cross Ref]
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. [PubMed] [Cross Ref]
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. [PubMed]
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. [PubMed]
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. [PubMed] [Cross Ref]
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. [Cross Ref]
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. [PubMed] [Cross Ref]
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. [Cross Ref]
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. [PubMed] [Cross Ref]
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. [PubMed] [Cross Ref]
27. Park H, Robinson JR. Mechanisms of mucoadhesion of poly(acrylic acid) hydrogels. Pharm Res. 1987;4:457–464. doi: 10.1023/A:1016467219657. [PubMed] [Cross Ref]
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. [Cross Ref]
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. [PubMed] [Cross Ref]
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. [PMC free article] [PubMed] [Cross Ref]

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