Abstract
The aim of this project was to examine the effect of microneedle rollers on the percutaneous penetration of tiagabine hydrochloride and carbamazepine across porcine skin in vitro. Liquid chromatography-mass spectrometric analysis was carried out using an Agilent 1200 Series HPLC system coupled to an Agilent G1969A TOF-MS system. Transdermal flux values of the drugs were determined from the steady-state portion of the cumulative amount versus time curves. Following twelve hours of microneedle roller application, there was a 6.74-fold increase in the percutaneous penetration of tiagabine hydrochloride (86.42 ± 25.66 µg/cm2/h) compared to passive delivery (12.83 ± 6.30 µg/cm2/h). For carbamazepine in 20% ethanol, passive transdermal flux of 7.85 ± 0.60 µg/cm2/h was observed compared to 10.85 ± 0.11 µg/cm2/h after microneedle treatment. Carbamazepine reconstituted in 30% ethanol resulted in only a 1.19-fold increase in drug permeation across porcine skin (36.73 ± 1.83 µg/cm2/h versus 30.74 ± 1.32 µg/cm2/h). Differences in flux values of untreated and microneedle-treated porcine skin using solid microneedles for the transdermal delivery of tiagabine were statistically significant. Although there were 1.38- and 1.19-fold increases in transdermal flux values of carbamazepine when applied as 20% and 30% ethanol solutions across microneedle-treated porcine skin, respectively, the increases were not statistically significant.
Highlights
The transdermal route of drug administration is advantageous because it avoids shortcomings of oral drug delivery [1]
The pores (Figure 2b,d) were identified as the openings filled to untreated porcine skin after staining
We showed that the application of microneedle rollers led to increased flux values of tiagabine hydrochloride
Summary
The transdermal route of drug administration is advantageous because it avoids shortcomings of oral drug delivery [1]. The advantages of the percutaneous route include painlessness, avoidance of first pass metabolism and the absence of erratic absorption, control over the rate of drug release, easy termination of therapy, and the possibility of self-administration and sustained drug release with a single application [2,3,4]. Despite the obvious advantages of this route of drug administration, only about 20 active pharmaceutical ingredients are used in clinical practice in the form of transdermal patches [5,6,7]. This is because the skin forms a remarkably strong barrier against drug penetration [8]. The human skin protects the internal organs and permits extremely low drug absorption from the skin surface
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