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Heat-Stable Dry Powder Oxytocin Formulations for Delivery by Oral Inhalation
Karine Fabio1, Kieran Curley2, Joseph Guarneri2
1Mannkind Corporation, One Casper Street, Danbury, Connecticut, 06810, USA. kfabio@mannkindcorp.com.
AAPS Pharmscitech
|March 18, 2015
Summary
Heat-stable oxytocin (OT) dry powders were developed for oral inhalation. Formulations with citrate and zinc salts significantly improved OT stability and reduced impurities during storage.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Biotechnology
Background:
- Oxytocin (OT) is a peptide hormone with therapeutic applications.
- Developing stable, inhalable formulations of OT presents significant challenges.
- Oral inhalation offers a non-invasive alternative for drug delivery.
Purpose of the Study:
- To prepare heat-stable dry powders of oxytocin (OT) for oral inhalation.
- To optimize excipient combinations for enhanced OT stability and aerodynamic performance.
- To evaluate the physicochemical and aerodynamic properties of the prepared OT dry powders.
Main Methods:
- Spray drying was employed to produce OT dry powders using selected excipients.
- Particle size distribution was analyzed using laser diffraction.
- Aerodynamic performance was assessed using Andersen cascade impaction (ACI) and an anatomically correct airway (ACA) model.
- Physicochemical properties were characterized by X-ray diffraction (XRD) and modulated differential scanning calorimetry (MDSC).
- Oxytocin assay and impurity profiling were performed using reverse-phase HPLC and LC-MS after accelerated storage.
Main Results:
- Spray-dried OT powders exhibited a median particle size of 2 μm, suitable for inhalation.
- The powders demonstrated excellent aerodynamic performance, with respirable fractions up to 77%.
- Physicochemical characterization revealed amorphous powders with a high glass transition temperature, indicating stabilization.
- OT dry powders formulated with citrate and zinc salts retained over 90% of the initial assay after 32 weeks of storage at 40°C/75%RH.
- These optimized formulations showed a threefold reduction in dimer and trisulfide formation compared to controls.
Conclusions:
- Heat-stable, amorphous oxytocin dry powders suitable for oral inhalation were successfully prepared.
- The combination of citrate and zinc salts significantly enhanced OT stability and reduced degradation products.
- The developed formulation demonstrates promising potential for a stable, inhalable oxytocin product.
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