Abstract
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.
Highlights
The integration of an electro-medical technique—iontophoresis, which refers to the ordered movement of ions under a potential gradient—into the field of topical and transdermal drug delivery [1], has shown its ability to make the “undeliverable” deliverable or to make the suboptimal candidates optimal (e.g., ARN14140 [3])
The results indicated that FBF was stable under the conditions for the planned iontophoretic delivery experiments
The results showed that the resulting systemic exposure after oral administration was much higher than what was observed with topical FBF iontophoresis (Table 5); this superior systemic exposure did not translate to higher FBF levels in the plantar muscle and skin
Summary
The integration of an electro-medical technique—iontophoresis, which refers to the ordered movement of ions under a potential gradient—into the field of topical and transdermal drug delivery [1], has shown its ability to make the “undeliverable” deliverable (e.g., cetuximab [2]) or to make the suboptimal candidates optimal (e.g., ARN14140 [3]). This powerful technique can individualize the administered dose more readily than many other delivery methods—the transdermal drug flux is adjustable by tuning the intensity of the current applied. Plantar heel pain is commonly caused by soft tissue related fat pad atrophy or
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