Buccal Drug Delivery Systems

· TGI - Formulations



The permeability of mucous membranes provides a convenient route for the systemic delivery of new and existing therapeutic drugs. Drug delivery through various mucosal surfaces may improve bioavailability by bypassing the first-pass effects and avoiding the elimination of the drug within the gastrointestinal (GI) tract.
Transmucosal drug delivery is being considered as an attractive delivery route for new and existing drug compounds, some of which are only available today through parenteral delivery. Of the various sites available for transmucosal drug delivery, the buccal mucosa and the sublingual area are the best suited sites for local as well as systemic delivery of drugs due to their physiological features. 
For compromised patient populations in which swallowing is difficult or the potential choking hazard is present, a buccal delivery device presents an effective dosage format with rapid onset and improved bioavailability compared to other oral formats. A number of buccal products are emerging for the treatment of chronic conditions, as well as breakthrough treatments for central nervous system conditions and pain therapies in the form of oral sprays, buccal films or tablets, and sublingual films or wafers.

As with transdermal applications, there are limitations to delivering higher molecular weight (Mw) compounds through buccal mucosal tissue. This is because the buccal and sublingual membranes contain a stratified (multilayered) epithelium that demonstrates differentiation of various cell layers. This is different than the single epithelium cell layer lining of the (GI) tract, thereby resulting in less resistance to permeability. Several approaches can be taken to increase the permeation of a drug through the buccal mucosal membrane.

  1. One of these approaches is to improve the bioadhesion properties to increase residence time and drug release of the device in the oral cavity.
  2. Another approach is to modify the physiochemical properties of the drug, such as a drug’s partition coefficient.
  3. A third approach, which is also used in transdermal drug delivery, is to employ the use of chemical permeation enhancers.

…The next generation of buccal product designs will evolve to include options for controlled release up to 12 to 24 hours. The general challenge for controlled-release applications is to design systems that slowly erode over time without becoming dislodged and swallowed as a result of normal activities, such as eating and drinking. Increased residence times of new buccal delivery devices may make it possible to deliver sensitive biological compounds that would otherwise be deactivated in the GI tract and thereby can only be dispensed currently through an injectable dose.

Product developers must be cognizant of an increased potential for irritation to occur for longer-wearing devices – some of these concerns can be addressed through proper mucoadhesion ingredient selection.

To view this issue and all back issues online, please visit http://www.drug-dev.com.


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