Enhancement of Skin Penetration of Nonsteroidal Anti-Inflammatory Drugs from Extemporaneously Compounded Topical-Gel Formulations
Author(s): Goodwin Donald A, Fuhram L Clifton
Issue: Nov/Dec 1999 - Compounding for Arthritis Patients
View All Articles in Issue
Page(s): 496-500
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Abstract: Ketoprofen and ibuprofen topical gels were compounded with
decyl methyl sulfoxide and the terpenes d-limonene, (-)-menthone,
terpinen-4-ol, and a-terpineol as penetration enhancers.
Transdermal penetration profiles for both ketoprofen
and ibuprofen were determined using full-thickness human
skin, modified Franz diffusion cells and an isotonic (pH 7.4)
phosphate buffer solution. Human skin was used in these experiments
to approximate the therapeutic use of these gels.
Ibuprofen was found to have superior transdermal kinetics
when compared to ketoprofen. Ibuprofen is a smaller and
more lipophilic molecule than ketoprofen, which gives it better
penetration properties. All enhancers tested significantly
increased the penetration (except (-)-menthone) and skin retention
(except terpinen-4-ol) of ketoprofen. None of the enhancers
tested significantly increased the penetration or
retention of ibuprofen. Despite the lack of enhancer activity,
ibuprofen still demonstrated higher skin penetration and retention
than enhanced delivery of ketoprofen. The results of
these studies suggest that the addition of penetration enhancers
can significantly increase the amount of ketoprofen
penetration, while enhancers demonstrated no significant increase
(and can actually decrease) the amount of ibuprofen penetrating
into and through the skin.
Related Keywords:
ketoprofen, ibuprofen, decyl methyl sulfoxide, penetration, transdermal, skin
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