Journal
PHARMACEUTICS
Volume 12, Issue 7, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics12070608
Keywords
flurbiprofen; iontophoresis; plantar heel pain; local delivery
Categories
Funding
- China National Natural Science Foundation [81603044]
- China Postdoctoral Science Foundation [2017M611886]
- Innovation and Entrepreneurship Training Program for College Students in Jiangsu Province [201710304080Y, 201810304040Z]
- Large Instruments Open Foundation of Nantong University [KFJN1852]
- Nantong University Cooperative Innovation Program of Small Molecular Compound RD [NTU2016-1]
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The objective of this study was to investigate the topical iontophoresis of flurbiprofen (FBF) as a means to enhance its local bioavailability and thereby provide an improved and targeted treatment of plantar heel pain. Initial in vitro experiments using porcine ear skin investigated iontophoretic transport of FBF under different conditions. Local FBF biodistribution in the rat paw in vivo was compared after topical or oral administration. Efficacy of pain management was investigated using a plantar incisional model by evaluating pharmacodynamic responses to local pain stimuli. The results demonstrated that iontophoresis of FBF significantly increased cutaneous deposition and transdermal permeation of FBF as compared to passive delivery-it also enabled drug input to be controlled by modulation of current density and drug concentration (r(2)> 0.99). Topical iontophoresis of FBF in vivo enabled higher drug levels in skin and muscle in rat plantar aspect and superior pharmacodynamic responses to local pain stimuli, in comparison to oral and passive delivery. In conclusion, short-duration topical iontophoresis of FBF may better help to relieve plantar heel pain than oral or passive administration, which should be of clinical interest.
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