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Biovector™ Nanoparticles Improve Antinociceptive Efficacy of Nasal Morphine

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Abstract

Purpose. We have studied the antinociceptive activity and blood andbrain delivery of nasal morphine with or without Biovector™nanoparticles in mice.

Methods. A tail flick assay was used to evaluate theantinociceptive activity. The kinetics of morphine were evaluated in blood andbrain, using tritiated morphine as tracer.

Results. These nanoparticles were shown to increase the durationof the antinociceptive activity of morphine after nasal administration.This effect was not due to an increase of morphine in the blood; andthe analgesic activity of morphine in association with nanoparticleswas reversed by naloxone. The ED50 value was 33.6 ±15.6 mg/kg for morphine alone and 14.4 ± 7.6 mg/kg in presenceof nanoparticles. They were only effective at low doses (1.5 to 2.5 μg),a higher or a lower dose had no effect. No interaction was found betweennanoparticles and morphine. NaDOC, a permeation enhancer, was unable toimprove nasal morphine activity.

Conclusions. These results show the presence of nanoparticles onlyat a very specific dose increases the antinociceptive activity of nasalmorphine in mice. The occurrence of a direct transport of morphinefrom the nasal mucosa to the brain is discussed.

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Authors and Affiliations

  1. Biovector Therapeutics SA. Chemin du Chébe Vert, BP 169 31676, Labège cedex, France

    Didier Betbeder

  2. Biovector Therapeutics SA. Chemin du Chébe Vert, BP 169 31676, Labège cedex, France

    Sandrine Spérandio & Alain Etienne

  3. Institut de Pharmacologie et de Biologie Structurale, CNRS, 205 Route de Narbonne, 31077, Toulouse cedex, France

    Jean-Philippe Latapie, Josette de Nadaí, Jean-Marie Zajac & Bernard Francés

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  1. Didier Betbeder
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  2. Sandrine Spérandio
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  4. Josette de Nadaí
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  5. Alain Etienne
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  6. Jean-Marie Zajac
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  7. Bernard Francés
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Betbeder, D., Spérandio, S., Latapie, JP. et al. Biovector™ Nanoparticles Improve Antinociceptive Efficacy of Nasal Morphine. Pharm Res 17, 743–748 (2000). https://doi.org/10.1023/A:1007594602449

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