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Electrically Modulated Transdermal Delivery of Fentanyl

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Abstract

Purpose. Test to determine if iontophoresis and electroporation, alone or in combination, can be used for rapid and modulated delivery of fentanyl.

Methods. Fentanyl citrate (5 mg/ml) dissolved in pH 4.0 citrate buffer was delivered in vitro across human epidermis. For iontophoresis, a current of 0.5 mA/cm2 was applied for 5 h, using silver/silver chloride electrodes. Electroporation protocol consisted of applying 15 exponential pulses of 500V (applied voltage) and 200 msec duration at the rate of 1 pulse per minute at time zero and, in some cases, repeating at 1.5 and 2.5 h.

Results. There was no measurable permeation of fentanyl through human epidermis under passive conditions. A significant flux (about 80 μg/cm2-hr) was achieved using iontophoresis and decreased once the current was turned off. A 4-fold higher flux and shorter lag time was observed with electroporation as compared to iontophoresis. The flux was found to recover quickly (within 1 h) following pulsing. Modulation of transdermal delivery of fentanyl was demonstrated by both iontophoresis and electroporation.

Conclusions. Electrically assisted transdermal delivery of fentanyl significantly increased transport compared to passive delivery. Also, rapid and modulated delivery was shown to be feasible by programming the electrical parameters.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, School of Pharmacy, Mercer University, 3001 Mercer University Drive, Atlanta, Georgia, 30341

    Rajkumar Conjeevaram & Ajay K. Banga

  2. Genetronics, Inc., 11199 Sorrento Valley Road, San Diego, California, 92121

    Lei Zhang

Authors
  1. Rajkumar Conjeevaram
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  2. Ajay K. Banga
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  3. Lei Zhang
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Correspondence to Ajay K. Banga.

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Conjeevaram, R., Banga, A.K. & Zhang, L. Electrically Modulated Transdermal Delivery of Fentanyl. Pharm Res 19, 440–444 (2002). https://doi.org/10.1023/A:1015135426838

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  • DOI: https://doi.org/10.1023/A:1015135426838

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