Publication: Effect of pH on Iontophoretic Transport of Pramipexole Dihydrochloride across Human Epidermal Membrane
Issued Date
2021-04-01
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ISSN
1573904X
07248741
07248741
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2-s2.0-85103893337
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Mahidol University
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SCOPUS
Bibliographic Citation
Pharmaceutical Research. Vol.38, No.4 (2021), 657-668
Suggested Citation
Kamchai Saepang, S. Kevin Li, Doungdaw Chantasart Effect of pH on Iontophoretic Transport of Pramipexole Dihydrochloride across Human Epidermal Membrane. Pharmaceutical Research. Vol.38, No.4 (2021), 657-668. doi:10.1007/s11095-021-03001-3 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/76227
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Title
Effect of pH on Iontophoretic Transport of Pramipexole Dihydrochloride across Human Epidermal Membrane
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Abstract
Purpose: Drugs with higher molecular charges generally show higher flux enhancement when electromigration is the main mechanism in transdermal iontophoresis. This study evaluated the effect of decreasing the formulation pH to increase the positive charges of pramipexole dihydrochloride (PXCl) on its iontophoretic transport across skin. Methods: In vitro transdermal iontophoresis of PXCl in buffer solution isotonized with either sodium chloride or mannitol were performed in a pH range of 3.0–7.0. Experiments of iontophoresis under symmetric condition with respect to donor and receiver pH and passive transport of the drugs after pretreatment with iontophoresis were conducted to investigate the transport mechanism involved. Results: Iontophoretic permeation of PXCl was pH-dependent in drug solution isotonized with mannitol. The iontophoretic flux of PXCl with valence z = +2 at pH 3.0 was half of that of PXCl with z = +1 at pH 7.0. The results suggest that the decrease in PXCl delivery at higher valence at pH 3 was mainly due to pH-dependent selectivity of PX ion permeation across the skin and not electroosmosis. Conclusions: Skin permselectivity is a significant factor for iontophoretic transport of PXCl, and reducing formulation pH to increase the positive charges on PX ions did not enhance PXCl delivery.