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THE PHARMA REVIEW
(AUGUST 2008) |
Development of Captopril
Gels for Optimized Transdermal Delivery
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Dr. P.G. Yeole, Dhanalakshmi
Iyer |
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Abstracts: The rationale of the current study was
to design and evaluate bio-adhesive carbopol gels of
captopril for the best possible transdermal permeation.
The influence of various drug concentrations and pH of
the carbopol gels, enhancing effect of the type and
concentration of various enhancers were assessed in this
investigation across rat skin. Optimized formulations
were obtained by studying the release pattern via human
skin with 1% hyaluronic acid as an enhancer. Studies
indicated that the increase in target flux by using an
effective enhancer reduces the administered area for
transdermal delivery, thus making it advantageous for
further development and establishing its commercial
feasibility. Comparative analysis via three skin types
concluded that, a correction factor need be considered
for human skin, if in vitro trials were done using
rodent skin type.
Introduction
Captopril an angiotensin I converting enzyme inhibitor,
is effective in reduction of hypertension and treatment
of congestive heart failure. Captopril has a relatively
short elimination half life in plasma with estimates in
man ranging from 1.6 to 1.9 h. Food may decrease the
oral absorption of captopril by 25-40%. Also it has been
reported that captopril has good penetration effect, the
serum level (31ng/ml) of therapeutic minimum effect is
obtained by using about 10cm2 of administered area of
captopril gel. Hence transdermal drug delivery for
captopril that could provide the desired constant drug
delivery for a predetermined period is beneficial for an
effective and safe therapy of hypertension and
congestive heart failure.
Transdermal drug delivery does offer significant
potential for non-invasive administration of therapeutic
agents but the architecture and composition of the
stratum corneum (SC) have severely limited the number of
molecules that can be delivered passively across the
skin. The use of penetration enhancers has been well
documented for transdermal drug delivery, which
penetrate into skin to reversibly decrease SC’s barrier
resistance. In this study the effect of drug
concentration and pH on captopril penetration, enhancing
effect of the type and concentration of penetration
enhancers on the skin permeation of captopril from
carbopol gels and the in-vitro flux of captopril through
various membrane barriers from different hydrogel
formulations were evaluated.
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