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Intranasal delivery of morphine
1West Pharmaceutical Services, Drug Delivery and Clinical Research Centre Ltd., Albert Einstein Centre, Nottingham Science and Technology Park, Nottingham, United Kingdom. lisbeth_illum@westpharma.com
The Journal of Pharmacology and Experimental Therapeutics
|March 22, 2002
Summary
Novel chitosan-based nasal morphine formulations significantly enhance drug absorption. This development offers a non-injectable option for rapid and effective pain relief, improving patient outcomes.
Area of Science:
- Pharmacology
- Drug Delivery Systems
- Biomaterials
Background:
- Nasal morphine solutions exhibit limited bioavailability (around 10%) compared to intravenous administration.
- Developing effective non-injectable morphine delivery is crucial for pain management.
Purpose of the Study:
- To develop and evaluate novel chitosan-based nasal morphine formulations for enhanced bioavailability.
- To compare the pharmacokinetic profile of these formulations with intravenous morphine in humans.
Main Methods:
- Development of chitosan-morphine nasal formulations.
- Pre-clinical evaluation in a sheep model to assess bioavailability enhancement.
- Clinical study in healthy volunteers comparing nasal formulation to slow intravenous morphine infusion.
Main Results:
- Chitosan-morphine nasal formulations demonstrated a 5- to 6-fold increase in bioavailability in sheep.
- In humans, nasal formulations achieved rapid absorption (Tmax ≤ 15 min) and high bioavailability (nearly 60%).
- Plasma and metabolite profiles of nasal delivery closely matched slow intravenous administration, with lower glucuronide metabolite levels.
Conclusions:
- Chitosan-based nasal morphine formulations significantly improve morphine absorption and bioavailability.
- These formulations provide a viable non-injectable alternative for rapid and efficient pain relief.
- The developed nasal delivery system offers a promising approach for opioid administration.