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Tissue Levels of Flurbiprofen in the Rat Plantar Heel after Short-Duration Topical Iontophoresis Are Sufficient to Induce Pharmacodynamic Responses to Local Pain Stimuli

1
Laboratory for Drug Delivery & Translational Medicine, School of Pharmacy, Nantong University, 19 Qixiu Road, Nantong 226001, Jiangsu Province, China
2
School of Pharmaceutical Sciences, University of Geneva & University of Lausanne, CMU, 1 rue Michel Servet, 1211 Geneva, Switzerland
3
Laboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasília, Brasília 70910-900, Brazil
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(7), 608; https://doi.org/10.3390/pharmaceutics12070608 (registering DOI)
Received: 8 June 2020 / Revised: 27 June 2020 / Accepted: 28 June 2020 / Published: 30 June 2020
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 (r2 > 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. View Full-Text
Keywords: flurbiprofen; iontophoresis; plantar heel pain; local delivery flurbiprofen; iontophoresis; plantar heel pain; local delivery
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MDPI and ACS Style

Cai, Y.; Zhou, Y.; Zhang, P.; Kalia, Y.N.; Gratieri, T.; Chen, Y. Tissue Levels of Flurbiprofen in the Rat Plantar Heel after Short-Duration Topical Iontophoresis Are Sufficient to Induce Pharmacodynamic Responses to Local Pain Stimuli. Pharmaceutics 2020, 12, 608.

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