Microneedle-mediated transdermal delivery of naloxone hydrochloride for treatment of opioid overdose

Ashana Puri, Dorcas Frempong, Dhruv Mishra, Prashant Dogra

Research output: Contribution to journalArticlepeer-review

16 Scopus citations


Naloxone (NAL) is administered parenterally or intranasally for treating opioid overdose. The short duration of action of NAL calls for frequent re-dosing which may be eliminated by the development of a transdermal system. This study aimed to assess the effect of microneedles on improving the skin permeation of NAL hydrochloride. In vitro permeation of NAL across intact and microneedle-treated (Dr. Pen™ Ultima A6) porcine skin was evaluated. The effect of microneedle length and application duration, and donor concentration on NAL permeation were investigated. In-vitro in-vivo correlation of the permeation results was done to predict the plasma concentration kinetics of NAL in patients. In vitro passive permeation of NAL after 6 h was observed to be 8.25±1.06 µg/cm2. A 56- and 37-fold enhancement was observed with 500 and 250 µm needles applied for 1 min, respectively. Application of 500 µm MNs for 2 min significantly reduced the lag time to ~ 8 min and increasing the donor concentration for the same treatment group doubled the permeation (p < 0.05). Modeling simulations demonstrated the attainment of pharmacokinetic profile of NAL comparable to those obtained with the FDA-approved intramuscular and intranasal devices. Microneedle-mediated transdermal delivery holds potential for rapid and sustained NAL delivery for opioid overdose treatment.

Original languageEnglish (US)
Article number120739
JournalInternational Journal of Pharmaceutics
StatePublished - Jul 15 2021


  • Microneedles
  • Microporation
  • Naloxone
  • Opioid addiction
  • Skin permeation
  • Transdermal

ASJC Scopus subject areas

  • Pharmaceutical Science


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