Buccal Drug Delivery System and Penetration Enhancer: A Review

Jaya Gopal Meher, Narayan P. Yadav*, Kuldeep Singh Yadav and Vineet Rai

Abstract: Buccal drug delivery has become one of the popular drug delivery system as it has got some significant advantages over conventional dosage forms. Drugs having high first pass metabolism, low aqueous solubility, instability in gastric pH, low molecular weight, low dose and less biological half life can be suitably delivered through buccal route. Buccal mucosa has a very complex structure and acts as a barrier for drug absorption. In order to facilitate the drug absorption across buccal membrane, penetration enhancers are co-administered with the drugs, which consequently increase the bioavailability of administered drug. Penetration enhancers act by several mechanisms which include increasing retention time of drug around the buccal mucosa, interaction with the buccal mucosal protein and intracellular lipid and/or enhancing the drug partitioning across the buccal mucosa. Present review describes the role of penetration enhancers, and their mechanism of action, in significantly increasing the drug absorption across the buccal mucosa.

Introduction: Active pharmaceutical ingredients are exhaustively studied before developing any formulation. The Preformulation data, pharmacokinetic and dynamic parameters suggest which dosage form will be appropriate for a specific drug molecule.1 The key factors that determine the development of dosage forms are solubility, partition co-efficient, therapeutic dose, drug excipients compatibility, biological half life as well as other pharmacokinetic and pharmacodynamic parameters.2 Drugs having less biological half life are suitable for sustained release dosage forms. At the same time if the drug molecules have high first-pass metabolism then, route of drug administration is required to be changed. The alternatives that by pass first-pass metabolism are buccal, transdermal, rectal, vaginal routes and some organ targeted drug delivery systems.3 Buccal drug delivery is one of the emerging delivery system for its significant advantages over other delivery systems. Certain drugs such as carvedilol, metoprolol, ibuprofen, miconazole etc. are extensively studied and buccal patches are developed for these drugs.4 Combination of hydrophilic, hydrophobic as well as mucoadhesive polymers are used in required ratio to develop patches of different drug release characteristic and flexibility.5 As the buccal mucosa acts as a barrier for drug absorption, penetration enhancers are used to facilitate the drug absorption across the buccal mucosa, which consequently increase the bioavailability of administered drug.6 Important penetration enhancers with their chemical category have been depicted in Table-1. These penetration enhancers may act in one or more possible mechanisms to enhance the drug absorption. In the following parts of this review details of the barrier function of buccal mucosa and role as well as mechanism of penetration enhancers are discussed.



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