Purpose:
To develop an ibuprofen transdermal gel with a
capability for both topical and systemic drug delivery.
Methods:
Ibuprofen gel formulations, incorporating various
permeation enhancers, were prepared using chitosan as a
gelling agent. The formulations were examined for their
in vitro characteristics including viscosity, pH and
drug release as well as in vivo pharmacological
activities. Carrageenan-induced rat paw oedema model was
used for the evaluation of their analgesic and
anti-inflammatory activities. A commercial ibuprofen gel
product (Ibutop®) was used as a reference.
Results:
The formulations containing 5 % of either menthol or
glycerol as permeation enhancers gave drug release
patterns comparable to that of the reference product.
Propanol increased the apparent viscosity of the test
gels to the same extent as that of the reference. Drug
release from the formulations fitted best to the Higuchi
model. A significant in vivo analgesic effect was
produced by the test formulations containing 5 % menthol
and 20 % propylene glycol and the effect was superior to
that obtained with the reference product. However, no
significant anti-inflammatory activity was exerted by
any of the test gel formulations (p > 0.05).
Conclusion:
Ibuprofen gel preparations containing 5 % menthol and 20
% propylene glycol, respectively, exhibited pronounced
analgesic activity and could be further developed for
topical and systemic delivery of ibuprofen.
Keywords:
Transdermal gel, Chitosan, Ibuprofen, Menthol, Propylene
glycol, Penetration enhancer
