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Bulletin of Experimental Biology and Medicine

, Volume 163, Issue 6, pp 737–741 | Cite as

Analysis of the Efficiency of Microencapsulated Sustained-Release Form of Naloxone on the Experimental Model of Fentanyl Poisoning

  • N. G. VengerovichEmail author
  • M. A. Yudin
  • V. N. Bykov
  • A. S. Nikiforov
  • O. I. Aleshina
  • A. A. Kuz’min
  • T. M. Ustinova
  • S. V. Gadzikovskii
Article

We compared samples of microencapsulated naloxone prepared by using spray drying technique. 2-Hydroxypropyl-β-cyclodextrin, sodium alginate, polycaprolactone, and carboxymethyl cellulose were used as the carriers. It was found that the combination of naloxone with sodium alginate was characterized by the highest naloxone content in the matrix and the lowest release rate (100% release time was 60 min). Using the model of respiratory disturbances caused by 10 ED50 fentanyl (anesthetic effect), we studied the effects of naloxone—sodium alginate complex on the dynamics of CO2 concentration in the expired air. It was shown that treatment with the developed microencapsulated naloxone after fentanyl injection allowed reducing the therapeutic dose of the antagonist by more than 2 times and eliminated the necessity of repeated injections.

Key Words

naloxone microencapsulation sustained-release fentanyls opioid intoxication 

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Copyright information

© Springer Science+Business Media, LLC 2017

Authors and Affiliations

  • N. G. Vengerovich
    • 1
    Email author
  • M. A. Yudin
    • 1
  • V. N. Bykov
    • 1
  • A. S. Nikiforov
    • 1
  • O. I. Aleshina
    • 1
  • A. A. Kuz’min
    • 1
  • T. M. Ustinova
    • 1
  • S. V. Gadzikovskii
    • 2
  1. 1.State Research Testing Institute of Military Medicine, Ministry of Defense of the Russian FederationMoscowRussia
  2. 2.Silver-Farm Innovative Pharmaceutical CompanyssSt. PetersburgRussia

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