Migraine is a common neurological disorder characterized by nausea, vomiting, photophobia, aching, fever, pain and chills. Triptans are selective serotonin agonists which can used to relieve migraine symptoms. Almotriptan malate and naratriptan hydrochloride are currently used for the management of migraine in the form of oral tablets. Oral tablets may be problematic for patients experiencing nausea and vomiting which are often associated with migraine. The microneedle-assisted transdermal drug delivery of these triptans may improve patient compliance. A vertical six-celled, static Franz diffusion cell system was used to conduct in vitro permeation experiments on porcine ear skin to determine the influence of microneedle-assisted transdermal delivery of both almotriptan malate and naratriptan hydrochloride. HPLC-MS analysis was performed using an Agilent 1200 series high performance liquid chromatography system in combination with an Agilent time of flight mass spectrometer (TOF-MS) system model 6230 (Agilent, Santa Clara, CA, USA). A reversed phase liquid chromatography column (Agilent Zorbax Eclipse Plus C18, 100 mm X 2.1 mm, 3.5 µm), was utilized for chromatographic separation. Confocal laser scanning microscopy was used to characterize the depth of the microchannels created after stainless-steel microneedle roller application. Transdermal flux of both triptans was calculated from the linear portion of the cumulative amount of drug permeated versus time curve. The mean passive flux of almotriptan malate was 13.044 ± 0.32 µg.cm2 .h, while the mean flux following microneedle roller application was 11.281 ± 0.22 µg.cm2 .h. The mean flux values for naratriptan hydrochloride for passive and after microneedle roller application was 0.88 ± 0.29 µg.cm2 .h and 4.18 ± 1.39 µg.cm2 .h, respectively. Statistical analysis was performed using the Student’s t-test (GradPad Prism 7). A statistically significant difference (p<0.05) between microneedle-treated porcine skin samples compared to untreated skin samples was found for the transdermal flux values of naratriptan hydrochloride. Solid stainless-steel microneedle rollers enhanced the transdermal delivery of naratriptan hydrochloride. In contrast, transdermal flux values obtained for almotriptan malate indicate that differences between microneedle-treated and untreated skin samples was not statistically significant (p>0.05).
Ahmad, I., Ita, K. B., Morra, M. J., & Popova, I. E. (2018). Microneedle-Assisted Delivery of Anti-Migraine Drugs Across Porcine Skin: Almotriptan Malate and Naratriptan Hydrochloride. Frontiers in Nanoscience and Nanotechnology, 4 (2), 1-7. Retrieved from https://touroscholar.touro.edu/tuccop_pubs/241
Originally published in Frontiers in Nanoscience and Nanotechnology, 4(2), 1-7. The original material can be found here.
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