Inhalable Remdesivir Dry Powder Formulation for Pulmonary Delivery
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Solution Overview
Problem
Current formulations of remdesivir for COVID-19 treatment require intravenous infusion, limiting its early administration outside hospital settings and preventing direct delivery to the lungs, where it may be most effective.
Innovation Solution
Development of dry powder pharmaceutical compositions of remdesivir for inhalation, formulated with high drug loading and specific excipients like Captisol and leucine, allowing for direct delivery to the lungs and improved aerosol performance, enabling administration via dry powder inhalers.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If remdesivir is administered via intravenous infusion, then the drug can be delivered systemically, but the administration is limited to hospital or medical facility settings and cannot be performed early in the infection cycle
Solution Approach 1:
The patent changes the physical form of remdesivir from a solution suitable for intravenous infusion to a dry powder formulation suitable for inhalation. This parameter change enables the drug to be administered via inhalation rather than intravenous infusion, allowing early intervention outside hospital settings while maintaining therapeutic effectiveness.
Solution Approach 2:
The patent introduces specific excipients (mannitol, leucine, Captisol) as intermediaries to enable the delivery of remdesivir via inhalation. These excipients facilitate the formation of breathable dry powder particles that can carry the drug directly to the lungs, bridging the gap between systemic delivery requirements and inhalation administration needs.
2Quantity of substance
If remdesivir is administered via intravenous infusion, then the drug reaches systemic circulation, but it cannot be delivered directly to the lungs where it may be most effective
Solution Approach 1:
The patent applies local quality by formulating remdesivir as a dry powder specifically designed for pulmonary delivery. The formulation concentrates the drug in breathable particles that deposit directly in the lungs, providing high local concentration at the target organ rather than systemic distribution. This allows the drug to be most effective where needed - in the respiratory tissues.
Solution Approach 2:
The patent uses composite materials by combining remdesivir with specific excipients (mannitol, leucine, Captisol) to create an inhalable dry powder formulation. These composite particles have optimized properties for pulmonary delivery, including appropriate size, flow characteristics, and dissolution properties, enabling direct lung delivery while managing the complexity through careful material selection.
3Reliability
If remdesivir is formulated as dry powder for inhalation, then direct delivery to the lungs is enabled, but the drug loading and aerosol performance must be optimized
Solution Approach 1:
The patent optimizes multiple formulation parameters including the ratio of remdesivir to excipients, particle size distribution, and crystalline versus amorphous content. These parameter changes are carefully controlled to ensure the dry powder achieves appropriate aerosolization characteristics, breathability, and drug loading while maintaining manufacturing feasibility and delivery reliability.
Data Source
AI summary
The present disclosure provides pharmaceutical compositions of remdesivir that may be administered by inhalation. These compositions may allow the achievement of a therapeutically effective dose of remdesivir directly to the lungs. These compositions may be used to treat one or more diseases or disorders such as a viral infection like an infection of a coronavirus.