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Pharmaceutics 2016, 8(4), 33; doi:10.3390/pharmaceutics8040033

The Influence of Solid Microneedles on the Transdermal Delivery of Selected Antiepileptic Drugs

College of Pharmacy, Touro University California, Mare Island-Vallejo, CA 94592, USA
Department of Plant, Soil and Entomological Sciences, University of Idaho, Moscow, ID 83844, USA
Author to whom correspondence should be addressed.
Academic Editor: Yvonne Perrie
Received: 10 September 2016 / Revised: 22 October 2016 / Accepted: 4 November 2016 / Published: 15 November 2016
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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. View Full-Text
Keywords: epilepsy; carbamazepine; tiagabine hydrochloride; transdermal drug delivery; microneedles epilepsy; carbamazepine; tiagabine hydrochloride; transdermal drug delivery; microneedles

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MDPI and ACS Style

Nguyen, J.; Ita, K.B.; Morra, M.J.; Popova, I.E. The Influence of Solid Microneedles on the Transdermal Delivery of Selected Antiepileptic Drugs. Pharmaceutics 2016, 8, 33.

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