Buccal Drug Delivery: Past, Present and Future – A Review

A. Puratchikody, Prasanth V.V., Sam T. Mathew, Ashok Kumar B


The major hindrance for the absorption of a drug taken orally is extensive first pass metabolism or stability problems within the GI environment like instability in gastric pH and complexation with mucosal membrane. These obstacles can be overcome by altering the route of administration as parenteral, transdermal or trasmucosal. Among these trasmucosal has the advantage of ease of administration, patient compliance and are economic too. The mucosa of the buccal cavity is the most easily accessible transmuocosal site. Buccal transmucosal delivery helps to bypass first- pass metabolism by allowing direct access to the systemic circulation through the internal jugular vein. The buccal transmucosal route has been researched for a wide variety of drugs. Several methodologies have been considered so far, to design and manipulate the release properties towards the invention of buccal mucosal delivery systems. This article aims at reviewing the numerous techniques that has been designed till date for optimizing buccal transmucosal drug delivery.

Keywords: complexation; parenteral; transdermal; trasmucosal


complexation; parenteral; transdermal; trasmucosal

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Vogler EA. Water and the acute biological response to surfaces. J Biomater Sci Polym 1999;10:1015-1045.

Jones DS, Woolfson AD, Djokic J, Coulter WA. Development and mechanical characterization of bioadhesive semi-solid, polymeric systems containing tetracycline for the treatment of periodontal diseases. Pharm Res 1996;13:1734-1738.

Mizrahi B, Domb A. J. Mucoadhesive polymers for delivery of drugs to the oral cavity. Recent Pat Drug Deliv Formula 2008;2:108-119.

Salamat-Miller N, Chittchang M, Johnston TP. The use of mucoadhesive polymers in buccal drug delivery. Adv Drug Deliv Rev 2005;57:1666-1691.

Woodley J. Bioadhesion new possibilities for drug administration. Clin Pharmacokinet 2001;40:77-84.

Harding SE .Mucoadhesive interactions. Biochem Soc Trans 2003;31:1036-1041.

Haas J, Lehr CM. Developments in the area of bioadhesive drug delivery systems. Expert Opin Biol Ther 2002;2:287-298.

Edsman K, Hagerstrom H. Pharmaceutical applications of mucoadhesion for the non-oral routes. J Pharm Pharmacol 2005;57:3-22.

Jimenez MR, Castellanous, Zia H, Rhodes CT. Drug Dev Ind Pharm 1993;19:143.

Bomberag LE, Buxton DK, Friden PM. Novel periodontal drug delivery system for treatment of periodontitis. J.Control.Rel 2001;71:251-259.

James C, Boylan. Drug delivery buccal route. In: James Swarbrick, editor. Encyclopedia of Pharmaceutical Technology: Supplement 3, Marcel Dekker INC 2001; Vol 20:P. 800-11

Metia PK, Bandyopadhyay AK. In vitro evaluation of novel mucoadhesive buccal tablet of oxytocin prepared with Diospyros peregrina fruit mucilages. Yakugaku Zasshi 2008;128:603-609.

Tanabe M, Watanabe M, Yanagi M, Nishizawa S, Chigono Y, Matsuda J, Yamaoka K, Inoue K. Controlled indomethacin release from mucoadhesive film in vitro and clinical evaluations. Yakugaku Zasshi 2008;128:1673-1679.

Malik DK, Baboota S, Ahuja A, Hasan S, Ali. Recent advances in protein and peptide drug delivery systems. J Curr Drug Deliv 2007;4:141-151.

Munasur VAP, Pillay DJ, Chetty, Govender T. Statistical optimization of the mucoadhesivity and characterization of multipolymeric propranolol matrices for buccal therapy. International Journal of Pharmaceutics 2006;323:43-51.

Wong.TW. Chitosan and its use in design of insulin delivery system. Recent Pat Drug Deliv Formul 2009;3:8-25.

Ludwig A. The use of mucoadhesive polymers in ocular drug delivery.Adv Drug Deliv Rev 2005;57:1595-1639.

Chopra S, Mahdi S, Kaur J, Iqbal Z, Talegaonkar S, Ahmad FJ. Advances and potential applications of chitosan derivatives as mucoadhesive biomaterials in modern drug delivery. J Pharm Pharmacol 2006;58:1021-1032.

Sudhakar Y, Knotsu K, Bandopadhyay AK. Bio adhesive drug delivery – A promising option for orally less efficient drugs. J Control Rel 2006;114:15-40.

Silvia Rossi, Giuseppina Sandri , Carla M. Caramella. Buccal drug delivery -A challenge already won. Drug Spring 2005;2:59-65.

Di Colo G, Zambito Y, Zaino C. Polymeric enhancers of mucosal epithelia permeability: synthesis, transepithelial penetration-enhancing properties, mechanism of action, safety issues. J Pharm Sci 2008;97:1652-1680.

Senel S, Hincal AA. Drug permeation enhancement via buccal route: possibilities and limitations. J Control Release 2001;72:133-144.

Sayani AP, Chien YW. Systemic delivery of peptides and proteins across absorptive mucosa. Crit Rev Ther Drug Carrier Syst 1996;13:85-184.

Rajashree Mashru, Vijay Sutariya, Mayur Sankalia, Jolly Sankalia. Transbuccal delivery of lamotrigine across procine buccal mucosa in vitro determination of routes of buccal transport. J Pharm Pharmaceut Sci 2005;8:54-62.

Ceschel GC, Maffei P, Moretti MD, Demontis LS, Peana A. International Journal of Pharmaceutics 2000;195:45.

Miyazaki S, Nakayama A, Oda M, Takada M, Attwood D. Chitosan and sodium alginate based bioadhesive tablets for intraoral drug delivery. Biol Pharm Bull 1994;17:745–747.

Ceschel GC, Maffei P, Borgia SL. Design and evaluation of a new Mucoadhesive bilayered tablet containing nimesulide for buccal administration. Drug Deliv 2004;11:225–230.

Remunan-Lopez C, Portero A, Vila-Jato JL, Alonso MJ. Design and evaluation of chitosan/ethyl cellulose mucoadhesive bilayered devices for Buccal drug delivery. J. Control. Release 1998;55:143–152.

Abuja A, Khar RK, Ali J. Mucoadhesive drug delivery systems. Drug Dev. Ind. Pharm 1997;23:489–517.

Bouckaert S, Schautteet H, Lefebvre RA, Remon JP, Clooster RV. Double-layered mucoadhesive tablets containing nystatin. Eur. J. Clin.Pharmacol 1992;43:137.

Gupta A, Garg S, Khar RK. Interpolymer complexation and its effect on bioadhesion strength and dissolution characteristics of buccal drug delivery systems. Drug Dev Ind Pharm 1994;20:315–325.

Taylan B, Capan Y, Guven O, Kes S, Hincal AA. Design and evaluation of sustained release and buccal adhesive propronolol hydrochloride tablets. J Control Release 1996;38:11–20.

Desai KGH, Kumar TMP. Preparation and evaluation of a novel buccal adhesive system. AAPS PharmSciTech 2004;5:1–9.

Goud HK, Kumar TMP. Preparation and evaluation of a novel buccal Adhesive systems. AAPS PharmSciTech 2004;5:35.

Labot JM, Manzo RH, Allemandi A. Double layered mucoadhesive tablets containing nystatin. AAPS PharmSciTech 2002;3:22.

Rajesh K, Agarwal SP, Ahuja A. Buccoadhesive erodible carriers for local drug delivery: design and standardization. Int J Pharm 1996;138:68–73.

Nagai T. Adhesive topical drug delivery system. J Control Release 1985;2:121–134.

Ceschel GC, Maffei P, Borgia SL, Ronchi C. Design and evaluation of buccal adhesive hydrocortisone acetate tablets. Int J Pharm 2002;238:161–170.

Rafiee-Tehrani M, Jazayeri G, Toliyat T, Bayati K, Khalkhali K, Shamimi K, Miremadi A, Dorkoosh FA. Development and in-vitroevaluation of novel buccoadhesive tablet formulation of prednisolone, Acta Pharm 2002;52:123–130.

Nagai T, Konishi R. Buccal/gingival drug delivery systems. J. Control. Release 1987;6:353–360.

Agarwal V, Mishra B. Design development and biopharmaceutical a property of buccoadhesive compacts of pentazocine. Drug Dev Ind Pharm 1999;25:701–709.

Cassidy JP, Landzert NM, Quadros E. Controlled buccal delivery of Buprenorphine. J Control Release 1993;25:21–29.

Anlar S, Capan Y, Guven O, Gogus A, Dlakara T, Hincal AA. Formulation and in vitro and in vivo evaluation of buccoadhesive morphine sulphate tablets. Pharm. Res 1994;11:231–236.

Choi HG, Kim CK. Development of Omeprazole buccal adhesive tablets with stability enhancement in human saliva. J Control Release 2000;68:397–404.

Choi H, Jung J, Yong CS, Rhee C, Lee M, Han J, Park K, Kim C. Formulation and in vivo evaluation of Omeprazole buccal adhesive Tablet. J Control Release 2000;68:405–412.

Park CR, Munday DL. Development and evaluation of a biphasic buccal adhesive tablet for nicotine replacement therapy. Int J Pharm 2002;237:215–226.

Ikinci G, Senel S, Wilson CG, Şumnu M. Development of buccal bioadhesive nicotine tablet formulation for smoking cessation. Int J Pharm 2004;277:173–178.

Nagai T, Machida Y. Buccal delivery systems using hydrogels. Adv Drug Del Rev 1993;11:179–191.

Ponchel G, Touchard F, Wouessidjewe D, Duchene D, Peppas NA. Bioadhesive analysis of controlled release systems III. Bioadhesive and release behaviour of metronidazole containing poly (acrylic acid)- hydoxypropyl methylcellulose systems. Int J Pharm 1987;38:65–70.

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 tablet. Int J Pharm 1999;188:1–10.

Mizrahi B, Golenser J, Wolnerman JS, Dombi AJ. Adhesive tablet effective for treating canker sores in humans. Assoc J Pharm Sci 2004;93:2927–2935.

Du Q, Ping QN, Liu GJ. Preparation of Buspirone hydrochloride buccal adhesive tablet and study on its drug release mechanism. Yao Xue Xue Bao 2002;37:653–656.

Tsutsumi K, Obata Y, Nagai T, Loftsson T, TakayamaK. Buccal absorption of ergotamine tartrate using the bioadhesive tablet system in Guinea-pigs. Int J Pharm 2002;238:161–170.

Dinsheet, Agarwal SP, Ahuja A. Preparation and evaluation of buccal adhesive tablets of Hydralazine hydrochloride. Indian J Pharm Sci 1997;59:135–141.

Beyssac E, Aiche JM, Chezaubernarul C, Caplin H, Douin MJ. Renoux A. Proc Int Symp Control. Rel Biact Mater. Contr Rel Sci 1984;21.

Collins AE, Deasy PB. Bioadhesive lozenge for the improved delivery of cetylpyridinium chloride. J Pharm Sci 1990;79:116.

Cui Z, Mumper RJ. Bilayer films for mucosal (genetic) immunization via the buccal route in rabbits. Pharm Res 2002;19:947–953.

Perugini P, Genta I, Conti B, Modena T, Pavanetto F. Periodontal delivery of ipriflavone new chitosan/PLGA film delivery system for a lipophilic drug. Int J Pharm 2003;18:1–9.

Senel S, Ikinci G, Kas G, Yousefi-Rad A, Sargon MF, Hıncal AA. Chitosan films and hydrogels of chlorhexidine gluconate for oral mucosal Delivery. Int J Pharm 2000;193:197–203.

Tiwari D, Goldman D, Sause R, Madan PL. Evaluation of Polyoxyethylene homopolymers for buccal bioadhesive drug delivery device formulations. AAPS PharmSci 1999;1:1–8.

Guo JH. Investigating the surface properties and bioadhesion of buccal Patches. J Pharm Pharmacol 1994;46:647–650.

Danjo K, Kato H, Otsuka A, Ushimaru K. Fundamental study on the evaluation of strength of granular particles. Chem Pharm Bull 1994;42:2598–2603.

Ishida M, Nambu N, Nagai T. Mucosal dosage form of lidocaine for toothache using hydroxypropyl cellulose and carbopol. Chem Pharm Bull 1982;30:980–984.

Nafee NA, Ismail FA, Nabila A, Boraie LM. Mucoadhesive buccal patches of miconazole nitrate in vitro/in vivo performance and effect of ageing. Int J Pharm 2003;264:1–14.

Save T, Shah UM, Ghamande AR, Venkatachalam P. Comparative study of buccoadhesive formulations and sublingual capsules of nifedipine. J Pharm Pharmacol 1994;46:192–195.

Shojaei AH, Li X. Mechanisms of buccal mucoadhesion of novel copolymers of acrylic acid and polyethylene glycol monomethylether monomethacrylate. J Control Release 1997;47:151–161.

Hoogstraate AJ, Verhoef JC, Pijpers A, Leengoed LAV, Verheijden JH, Junginger, HE, Bodde. In vivo buccal delivery of the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs. Pharm Res 1996;13:1233–1237.

Alur H, Beal JD, Pather SI, Mitra AK, Johnston TP. J Pharm Sci 1999;88(12):1313–1319.

Yaziksiz-Iscan Y ,Capan Y, Senel S, Sahin MF, Kes S, Duchene, AA, Hincal, STP Pharma Pharm Sci 1998;8:357–363.

Ito Y, Hu Z, Yoshikawa M, Murakami M, Takada K. Proc Int Symp .Control Release Bioact Mater 1999;26:6303–6304.

Mcelnay JC, Furaih TA, Hughes CH, Scott MG, Elborn JS, Nicholls DP. Eur. J. Clin. Pharmacol 1998;54:609–614.

Gutniak MK, Larsson H, Heiber SJ, Juneskans OT, Holst JJ, Ahren B, Diabetes Care 1996;19:843–848.

Chien Y, Nakane S, Lee Y, Kakumoto M, Yukimatsu K. Proc. 1st World Meeting APGI/APV, Budapest; 1995;813–814.

Towey MG, Maury C. J Interferon Cytokine Res 1999;19(2):145–155.

Zhang J, Nui S, Ebert C, Stanley TH. Int J Pharm 1994;101:15–22.

Nakane S, Kakumoto M, Yukimatsu K, Chien YW. Pharm Dev Technol 1996;1:251–259.

Merkle HP, Wolany GJM. J Control Release 1992;21:155–164.

Li C, Padmanabh PB, Johnston TP. Pharm Dev Technol 1997;2(3):265–274.

Anders R, Merkle HP, Schurr W, Ziegler R. J Pharm Sci 1983;72:1481–1483.

Bayley D, Temple C, Clay V, Steward A, Lowther NJ. Pharm. Pharmacol 1995;47:721–724.


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