The future potential of buccal and sublingual delivery systems looks favorable. It is envisaged that in the future, buccal and sublingual delivery technologies will provide a platform for the successful delivery of vaccines and antigens. It is also foreseen that physical means of enhancing drug uptake (e.g., sonophoresis, iontophoresis and electroporation) will be commercialized for buccal delivery, thereby expanding the current drug candidate list for this area. The formulation of delivery systems for photosensitizers in photodynamic therapy is a potential emerging area, while buccal and sublingual delivery, in general, is attractive for the development of intellectual property.
Abstract. The influence of experimental temperature on the permeability of model diffusants across porcine buccal mucosa was investigated in vitro. The permeability increased significantly as the experimental temperature was increased in increments of approximately 7°C. It was observed that the apparent permeability and temperature were related by an exponential relationship that conformed to the Arrhenius equation. Diffusants with higher lipophilicities-buspirone and bupivacaine-had lower activation energies for diffusion when compared to hydrophilic diffusants-antipyrine and caffeine. The activation energy for diffusion of the model diffusants decreased linearly with increasing distribution coefficients across porcine buccal mucosa. The results suggested that the buccal mucosa acts as a stronger barrier to the diffusion of hydrophilic diffusants than the lipophilic ones. The log-linear relationship between permeability and temperature indicates that temperature should be carefully controlled in diffusion experiments. These results also point to the possibility of developing heat-generating buccal delivery devices, especially for hydrophobic diffusants.
The oral cavity is an attractive site for the delivery of drugs either locally or directly into the systemic circulation. Its attractiveness resides in the fact that the mucosal membranes, upon which drug delivery systems are located, are readily accessible to patients or their carers. This means that the delivery technology can be precisely placed on the specific oral cavity membrane that is chosen as the site of absorption. It also means that the delivery system can be removed in order to terminate delivery if signs of adverse reactions are observed during treatment. The oral cavity represents a challenging area to develop an effective drug delivery technology. This arises due to the various inherent functions of the oral cavity (eating, swallowing, speaking, chewing), as well as the presence of the fluid that is involved in all these activities, saliva. This fluid is continually secreted into, and then removed from, the mouth. There are many advantages and disadvantages associated with the oral cavity as a site for drug delivery. Overall, however, it remains a viable option as a route for drug administration and has been extensively studied for that purpose [1][2][3][4][5][6][7].In this chapter, the rationale behind companies pursuing the goal of developing oral mucosal drug delivery systems as well as the key considerations in the design and development of a drug delivery system intended for use in the oral cavity will be discussed. Finally, this chapter will briefly describe some of the formulation aspects of delivery systems that have been successfully developed to deliver drugs via this route.
The CRS flagship book series, Advances in Delivery Science and Technology, published in partnership with Springer, will serve as a wider forum for the dissemination of knowledge relating to delivery, science, technology, and innovation to the benefit of CRS members and to the general scientific community. Our aim is to deliver high-quality volumes edited by authoritarians and written by opinion leaders from around the globe. This work is subject to copyright. All rights are reserved by the Publisher, whether the whole or part of the material is concerned, specifically the rights of translation, reprinting, reuse of illustrations, recitation, broadcasting, reproduction on microfilms or in any other physical way, and transmission or information storage and retrieval, electronic adaptation, computer software, or by similar or dissimilar methodology now known or hereafter developed. The use of general descriptive names, registered names, trademarks, service marks, etc. in this publication does not imply, even in the absence of a specific statement, that such names are exempt from the relevant protective laws and regulations and therefore free for general use. The publisher, the authors and the editors are safe to assume that the advice and information in this book are believed to be true and accurate at the date of publication. Neither the publisher nor the authors or the editors give a warranty, express or implied, with respect to the material contained herein or for any errors or omissions that may have been made. Printed on acid-free paperSpringer is part of Springer Science + Business Media (www.springer.com). Editors PrefaceAcademia and industry have expressed a high interest throughout the past three decades in delivering drugs to or across the oral mucosa for the purpose of achieving desired therapeutic outcomes. However, because the membranes that line the oral cavity exhibit relatively poor permeability to drugs, and due to the fact that only a limited number of drugs possess the innate physicochemical properties to allow them to inherently cross the mucosa in clinically relevant amounts, we have failed to witness a large number of oral mucosal drug delivery systems become commercially available. This situation has stimulated much interest in conducting research that has focused on increasing the potential drug candidate list for oral mucosal therapeutic applications. Research on the use of oral mucosal permeation enhancers and mucoadhesives has resulted in advances in our knowledge of how to modify drug permeation through the oral mucosa and delivery system retention at the site of administration. It is the editors' belief that the prospect of the oral cavity as a site for drug delivery has yet to meet its full potential and that the oral mucosal route of administration is ideally suited to improve the delivery of several existing drugs. Such delivery systems would offer market differentiation for these drugs through improved, painfree, patient-friendly delivery systems that, when optimized, would offer a...
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