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. 2018;15(10):1449-1458.
doi: 10.2174/1567201815666180730125941.

The Influence of Microneedles on the Percutaneous Penetration of Selected Antihypertensive Agents: Diltiazem Hydrochloride and Perindopril Erbumine

Emmy Luu  1 , Kevin B Ita  1 , Matthew J Morra  2 , Inna E Popova  2
Affiliations

The Influence of Microneedles on the Percutaneous Penetration of Selected Antihypertensive Agents: Diltiazem Hydrochloride and Perindopril Erbumine

Emmy Luu et al. Curr Drug Deliv. 2018.

Abstract

Background: It is well documented in the scientific literature that high blood pressure can lead to cardiovascular disease. Untreated hypertension has clinical consequences such as coronary artery disease, stroke or kidney failure. Diltiazem hydrochloride (DH), a calcium-channel blocker, and perindopril erbumine (PE), an inhibitor of the angiotensin converting enzyme are used for the management of hypertension.

Objective: This project will examine the effect of microneedle rollers on the transport of DH and PE across pig ear skin. The use of the transcutaneous route of administration reduces and in sometimes eliminates the trauma and pain associated with injections. Furthermore, there is increased patient compliance. The purpose of this project was to study the effect of stainless steel microneedles on the transdermal delivery of DH and PE.

Method: We utilized vertical Franz diffusion cells to study in vitro transport of DH and PE across microneedle- treated pig ear skin. Confocal laser scanning microscopy (CLSM) was used to characterize microchannel depth. Transdermal flux values were determined from the slope of the linear portion of the cumulative amount versus time curve.

Results: There was a 113.59-fold increase in the transdermal permeation of DH following the application of microneedle roller compared to passive diffusion.

Conclusion: In the case of PE, there was an 11.99-fold increase in the drug transport across pig skin following the application of microneedle rollers in comparison with passive diffusion. Student's t-test and Mann-Whitney's rank sum test were used to determine statistically significant differences between experimental and control groups.

Keywords: Hypertension; diltiazem hydrochloride; microneedles; perindopril erbumine; skin; transdermal drug delivery..

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Figures

Fig. (1)
Fig. (1)
Microneedle roller.
Figs. (2)
Figs. (2)
Chemical structures of (a) diltiazem hydrochloride and (b) perindopril erbumine.
Fig. (3)
Fig. (3)
Confocal laser scanning images made with AlexaFluor 633 on (A) untreated porcine ear skin and (B) microneedle-treated porcine ear skin at 5x magnification. The single microchannel of microneedle-treated porcine ear skin has a depth of 133± 1.6 µm (n=6).
Fig. (4)
Fig. (4)
Average cumulative amount versus time curve (A) and transdermal flux (B) of diltiazem hydrochloride across untreated and microneedle-treated porcine ear skin over 12 hours.
Fig. (5)
Fig. (5)
Average cumulative amount versus time curve (A) and transdermal flux (B) of perindopril erbumine across untreated and microneedle-treated porcine ear skin over 12 hours.
See this image and copyright information in PMC

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