Inhalable tranexamic acid for haemoptysis treatment

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Journal Article
European Journal of Pharmaceutics and Biopharmaceutics, 2015, 93 pp. 311 - 319
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© 2015 Elsevier B.V. All rights reserved. Purpose An inhalable dry powder formulation of tranexamic acid (TA) was developed and tested in a novel high-dose Orbital® multi-breath inhaler. The formulation was specifically intended for the treatment of pulmonary haemorrhage and wound healing associated with haemoptysis. Methods Inhalable TA particles were prepared by spray drying and the powder characterised using laser diffraction, electron microscopy, thermal analysis, moisture sorption and X-ray powder diffraction. The aerosol performance was evaluated using cascade impaction and inline laser diffraction and interaction with epithelia cells and wound healing capacity investigated using Calu-3 air interface model. Results The spray dried TA particles were crystalline and spherical with a D0.5 of 3.35 μm. The powders were stable and had limited moisture sorption (0.307% w/w at 90% RH). The Orbital device delivered ca. 38 mg powder per 'inhalation' at 60 l·min-1 across four sequential shots with an overall fine particle fraction (≤6.4 μm) of 59.3 ± 3.5% based on the emitted mass of ca. 150 mg. The TA particles were well tolerated by Calu-3 bronchial epithelia cells across a wide range of doses (from 1 nM to 10 nM) and no increase in inflammatory mediators was observed after deposition of the particles (a decrease in IL-1β, IL-8 and INFγ was observed). Time lapse microscopy of a damaged confluent epithelia indicated that wound closure was significantly greater in TA treated cells compared to control. Conclusion A stable, high performance aerosol of TA has been developed in a multi-breath DPI device that can be used for the treatment of pulmonary lesions and haemoptysis.
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