Transbuccal Delivery of Chlorpheniramine Maleate from Mucoadhesive Buccal Patches

Abstract

This article describes buccal permeation of chlorpheniramine
maleate (CPM) and its transbuccal delivery using mucoadhesive
buccal patches. Permeation of CPM was calculated in vitro using
porcine buccal membrane and in vivo in healthy humans. Buc-
cal formulations were developed with hydroxyethylcellulose (HEC)
and evaluated for in vitro release, moisture absorption, mechani-
cal properties, and bioadhesion, and optimized formulation was
subjected for bioavailability studies in healthy human volunteers.
In vitro flux of CPM was calculated to be 0.14 ± 0.03 mg.h−1.cm−2
and buccal absorption also was demonstrated in vivo in human vol-
unteers. In vitro drug release and moisture absorbed were governed
by HEC content and formulations exhibited good tensile and mu-
coadhesive properties. Bioavailability from optimized buccal patch
was 1.46 times higher than the oral dosage form and the results
showed statistically significant difference.