Science
Pulmonary Delivery of ROSE-010
Preclinical evidence supporting pulmonary delivery and pharmacodynamic activity of ROSE-010 using Technosphere® technology.
Preclinical Study of Pulmonary ROSE-010
A controlled study in animal model of gastric motility evaluated whether a dry powder formulation of ROSE-010 could produce pharmacodynamic activity following pulmonary administration, compared with intravenous (IV) and subcutaneous (SC) injection.
Study Design:
- The end point was smooth muscle contraction, associated with motor activity in the small intestine.
- ROSE-010 was adsorbed onto Technosphere® particles to create a dry powder for pulmonary administration.
- Pulmonary delivery by insufflation was evaluated at ROSE-010 doses of 0.1 and 0.2 mg/kg.
- IV and SC ROSE-010 were each evaluated at 0.1 mg/kg. Air insufflation alone and injected saline served as controls.
- Intestinal smooth muscle activity was monitored over 6-8 hours, including a baseline period before dosing.
Key Results:
- Pulmonary ROSE-010 at 0.1 mg/kg and 0.2 mg/kg significantly slowed smooth muscle motor function and was comparable to 0.1 mg/kg iv and sc administration with a similar onset of action.
- No decrease in smooth muscle motor function was observed following treatment with air insufflation or injected saline controls.
Implications for Inhaled Delivery
- Demonstrated that ROSE-010 formulated as a Technosphere® dry powder retained pharmacodynamic activity after pulmonary administration.
- Supported the feasibility of a non-invasive pulmonary delivery approach for ROSE-010.
- Supported the potential of pulmonary ROSE-010 as a delivery mechanism.
This was a preclinical animal study. The findings do not establish the safety or efficacy of inhaled ROSE-010 in humans.
The research was funded in part by MannKind Corporation and Rose Pharma.