Heat-Stable Dry Powder Oxytocin Formulations for Delivery by Oral Inhalation

AAPS PharmSciTech
Karine FabioAndrea Leone-Bay

Abstract

In this work, heat stable dry powders of oxytocin (OT) suitable for delivery by oral inhalation were prepared. The OT dry powders were prepared by spray drying using excipients chosen to promote OT stability including trehalose, isoleucine, polyvinylpyrrolidone, citrate (sodium citrate and citric acid), and zinc salts (zinc chloride and zinc citrate). Characterization by laser diffraction indicated that the OT dry powders had a median particle size of 2 μm, making them suitable for delivery by inhalation. Aerodynamic performance upon discharge from proprietary dry powder inhalers was evaluated by Andersen cascade impaction (ACI) and in an anatomically correct airway (ACA) model, and confirmed that the powders had excellent aerodynamic performance, with respirable fractions up to 77% (ACI, 30 L/min). Physicochemical characterization demonstrated that the powders were amorphous (X-ray diffraction) with high glass transition temperature (modulated differential scanning calorimetry, MDSC), suggesting the potential for stabilization of the OT in a glassy amorphous matrix. OT assay and impurity profile were conducted by reverse phase HPLC and liquid chromatography-mass spectrometry (LC-MS) after storage up to 32 weeks at 40°C/75%RH. ...Continue Reading

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Citations

Jan 19, 2016·Advanced Drug Delivery Reviews·Lan ChenHak-Kim Chan
May 28, 2015·Acta Biomaterialia·Mithun Varghese VadakkanG S Vinod Kumar
May 20, 2016·Pharmaceutical Research·Mikolaj MilewskiShunji Haruta
Nov 30, 2016·Journal of Pharmaceutical Sciences·Teddy J ZbacnikMark Cornell Manning
Jul 25, 2019·Pharmaceutics·Brandon Banaschewski, Thomas Hofmann
Mar 27, 2021·Journal of Peptide Science : an Official Publication of the European Peptide Society·Mostafa GhasemisarabbadiehBenjamín Ragnar Sveinbjörnsson
Jul 16, 2021·Journal of Controlled Release : Official Journal of the Controlled Release Society·Yasmine GomaaMark R Prausnitz
Oct 2, 2021·International Journal of Pharmaceutics·Ebtesam Abdullah Al-SuhaimiAbdelgadir M Homeida

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