Abstract

The buccal mucosa provides an alternative route of drug delivery that can be more beneficial compared to other administration routes. Although numerous studies and reviews have been published on buccal drug delivery, an extensive review of the permeability data is not available. Understanding the buccal mucosa barrier could provide insights into the approaches to effective drug delivery and optimization of dosage forms. This paper provides a review on the permeability of the buccal mucosa. The intrinsic permeability coefficients of porcine buccal mucosa were collected. Large variability was observed among the published permeability data. The permeability coefficients were then analyzed using a model involving parallel lipoidal and polar transport pathways. For the lipoidal pathway, a correlation was observed between the permeability coefficients and permeant octanol/water partition coefficients (Kow) and molecular weight (MW) in a subset of the permeability data under specific conditions. The permeability analysis suggested that the buccal permeation barrier was less lipophilic than octanol. For the polar pathway and macromolecules, a correlation was observed between the permeability coefficients and permeant MW. The hindered transport analysis suggested an effective pore radius of 1.5 to 3 nm for the buccal membrane barrier.

Highlights

  • Division of Pharmaceutical Sciences, College of Pharmacy, University of Cincinnati, 231 Albert Sabin Way, Abstract: The buccal mucosa provides an alternative route of drug delivery that can be more beneficial compared to other administration routes

  • In the analyses of all permeability data including the permeants with pH dependent ionization, the permeability was described better by log Dow than log Kow for membrane partitioning and permeation, but the correlation was relatively poor with no observable effect of permeant molecular weight (MW)

  • For the permeability data of pH independent permeants, a better correlation was observed and the correlation improved with the incorporation of MW as the additional independent variable

Read more

Summary

Introduction

For effective drug delivery across a biological membrane, it is important to understand the transport behavior of the membrane for the drugs. The barrier property of a membrane due to passive transport can be described by its permeability coefficient. Review papers are available on the topics of buccal delivery of macromolecules such as peptides, oligonucleotides, and vaccines [7,23–26]. The effect of temperature and activation energy of membrane permeation were investigated to understand the transport mechanism of buccal mucosa [29]. The present paper provides a review on the permeability of the buccal mucosa for drug delivery. The permeability coefficients of the buccal mucosa without the influence of formulations or the use of penetration enhancers (i.e., membrane intrinsic permeability) were summarized in this paper. Analyses were performed to provide insights into a possible quantitative structure permeability relationship of passive transport across the buccal membrane that could be valuable in future drug delivery development

Buccal Mucosa and Drug Delivery
Permeability of Buccal Mucosa and Data Variability
Membrane Transport Theory
Effects of Lipophilicity and Molecular Weight on the Permeation of
Effective Pore Size for the Permeation of Macromolecules
Permeability Analysis Discussion and Consideration
Conclusions
Full Text
Published version (Free)

Talk to us

Join us for a 30 min session where you can share your feedback and ask us any queries you have

Schedule a call