Liposomal Trans-Crocetin Formulation for Hypoxia Treatment Stability
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Solution Overview
Problem
Trans-crocetin and its salt compositions face limitations due to poor solubility, instability, low bioavailability, and short half-life, which hinder their clinical therapeutic efficacy and development as treatments for conditions such as ischemia, ARDS, pneumonia, sepsis, and hypoxia.
Innovation Solution
Development of liposomal trans-crocetin formulations and dosing regimens that enhance bioavailability and stability, allowing for effective treatment of various disorders and conditions through targeted administration schedules.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If trans-crocetin is administered in free form (unencapsulated), then it offers promise in treatment for conditions caused by hypoxia and ischemia, but it has poor solubility, instability, low bioavailability and short half-life
Solution Approach 1:
The patent uses cyclodextrin molecules as intermediary carriers to encapsulate trans-crocetin. The cyclodextrin forms inclusion complexes with trans-crocetin, improving its solubility and stability in aqueous environments while maintaining its therapeutic activity. This mediator approach resolves the contradiction by protecting the active ingredient without compromising its efficacy.
Solution Approach 2:
The invention creates a composite formulation combining trans-crocetin with cyclodextrin molecules. This composite structure leverages the hydrophobic cavity of cyclodextrin to house the trans-crocetin molecule, thereby improving solubility and stability while preserving the therapeutic properties of trans-crocetin.
2Ease of manufacture
If trans-crocetin is administered in free form, then it can be given as a simple formulation, but it has low bioavailability and short half-life of only about 30 minutes
Solution Approach 1:
Cyclodextrin serves as a mediator that extends the circulation half-life of trans-crocetin by preventing its rapid clearance from the bloodstream. The inclusion complex protects trans-crocetin from metabolism and excretion, thereby extending its duration of action from 30 minutes to several hours while maintaining manufacturing feasibility.
3Ease of manufacture
If trans-crocetin is administered in free form, then the formulation is simple, but it has poor solubility in water
Solution Approach 1:
Cyclodextrin molecules act as solubilizing agents that form inclusion complexes with hydrophobic trans-crocetin molecules. This intermediary approach enables trans-crocetin to be delivered in aqueous formulations at clinically relevant concentrations without requiring complex formulation technologies.
Data Source
AI summary
Liposomal trans-crocetin pharmaceutical compositions, dosing regimens and methods of treating or preventing disorders and conditions associated with, but not limited to, infection, ischemia, hypoxia, ARDS, inflammation, sepsis, shock, stroke, traumatic injury, and proliferative disorders such as cancer are provided. Methods of using the provided trans-crocetin pharmaceutical compositions and dosing regimens to treat cardiovascular, renal, liver, inflammatory, metabolic, pulmonary, neurological, and other disorders and conditions are also provided, as are methods of increasing the delivery of oxygen and increasing the efficacy of a therapeutic agent using the provided compositions and dosing regimens.