چکیده (انگلیسی):

In the present study, 2 alternative strategies to optimize ketorolac
transdermal delivery, namely, prodrugs (polyoxyethylene
glycol ester derivatives, I-IV) and nanostructured
lipid carriers (NLC) were investigated. The synthesized prodrugs
were chemically stable and easily degraded to the
parent drug in human plasma. Ketorolac-loaded NLC with
high drug content could be successfully prepared. The obtained
products formulated into gels showed a different trend
of drug permeation through human stratum corneum and
epidermis. Particularly, skin permeation of ester prodrugs was
significantly enhanced, apart from ester IV, compared with
ketorolac, while the results of drug release from NLC outlined
that these carriers were ineffective in increasing ketorolac
percutaneous absorption owing to a high degree of mutual
interaction between the drug and carrier lipid matrix. Polyoxyethylene
glycol esterification confirmed to be a suitable
approach to enhance ketorolac transdermal delivery, while
NLC seemed more appropriate for sustained release owing to
the possible formation of a drug reservoir into the skin.