ABSTRACT
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The quest for alternative modes of drug delivery to the ever-popular oral route of admin-
istration has led to exploration of the various mucosae as possible delivery routes. Since the
invention of the nitroglycerin sublingual tablet, the oral mucosal route has generated
interest as a substitute delivery approach. Recent developments in the design of dosage
forms range from tablets and patches to ‘‘lollipops’’ and insertable chips. One of the leading
examples of successful buccal delivery includes the oral transmucosal fentanyl citrates
(OTFCs). The OTFC in the form of a lollipop, Actiq1 (Cephalon, Inc., Frazer, PA) has
revolutionized the treatment for breakthrough cancer pain relief (BTCP) [1], providing
better pain relief as compared to morphine sulfate immediate release (MSIR) tablets.
Another novel dosage form is the Periochip1 (Dexcel-Pharma Ltd., UK), composed of
chlorhexidine gluconate in a biodegradable matrix of hydrolyzed gelatin and cross-linked
with glutaraldehyde, which is inserted into the intraperiodontal pocket. This has proven to
be an excellent treatment for periodontitis, and is often given in conjunction with other
dental procedures such as scaling and root planing [2]. Recent investigations have also
concentrated on delivery of macromolecules such as peptides using the buccal route. The
avoidance of first-pass metabolism and intermediate permeation properties make it attract-
ive for drugs which are sensitive to pH and enzymatic degradation. This chapter aims to
provide an overview of the physiology and biopharmaceutics of the oral mucosal route and
present an insight into the delivery systems designed for this route.
