In Vitro and In Vivo Evaluation of DMSO and Azone as Penetration Enhancers for Cutaneous Application of Celecoxib
2017
Background: Celecoxib (CXB) has been explored as an anti-inflammatory or chemopreventive
drug for topical treatment of skin diseases and cancer.
Objective: The main aim of this work was to investigate the potential of dimethylsufoxide (DMSO) and
Azone (AZ) as penetration enhancers (P.Es) for topical delivery of CXB.
Method: The in vitro studies, drug release, skin permeability and potential cytotoxicity/genotoxicity
were carried out with formulations containing or not DMSO or AZ (5% and 10%). Skin irritation in
rabbits and topical anti-inflammatory activity in mice were assayed in vivo.
Results: Skin permeation was minimal while higher retention in SC and epidermis plus dermis was
found (28.0 and 3-fold respectively) from 10.0% AZ compared to the control indicating a localized
CXB effect. CXB associated to 5% or 10% DMSO has shown high drug permeation through skin with
low retention. Associations of CXB with both enhancers were not cytotoxic or genotoxic, suggesting
safety for cutaneous application. In vivo skin irritation assays of all formulations indicated mild irritation
effects and, thus, possible use for longer periods. In vivo anti-inflammatory tests showed that ear
edema could be inhibited by CXB associated with 5.0% DMSO (53.0%) or 10.0% AZ (40.0%). These
inhibition values were almost 2-fold higher when compared to a commercial formula.
Conclusion: Although DMSO- associated CXB is an efficient edema inhibitor its high skin permeation
suggests risks of systemic effects, whereas association to 10%AZ may improve topical delivery of the drug
with good anti-inflammatory activity and no cytotoxic/genotoxic or significant skin irritation effects.
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