Development of Captopril Gels for Optimized Transdermal Delivery

Dr. P.G. Yeole, Dhanalakshmi Iyer

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.
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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