Albumin-Bound Ophthalmic Composition for Solubility and Tolerability
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Solution Overview
Problem
Current ophthalmic medications for conditions like dry eye and inflammation have insufficient efficacy and cause unwanted side effects such as burning and stinging sensations due to low aqueous solubility and tolerability of active compounds.
Innovation Solution
Formulating ophthalmic compositions with pharmaceutically active compounds non-covalently bound to albumin, particularly human serum albumin, to enhance aqueous solubility and tolerability, reducing side effects and improving therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional ophthalmic medications are used to treat dry eye and inflammation, then therapeutic effects are achieved, but aqueous solubility is insufficient and tolerability is poor causing burning and stinging sensations
Solution Approach 1:
The patent uses albumin as an intermediary carrier molecule to bind with pharmaceutically active compounds. This albumin-drug complex serves as a mediator that improves aqueous solubility of the drug while reducing direct contact between the drug and ocular tissues, thereby minimizing irritation. The albumin acts as a protective vehicle that delivers the therapeutic agent to the target site without causing burning or stinging sensations.
Solution Approach 2:
The patent changes the physical and chemical parameters of the drug formulation by forming non-covalent complexes with albumin. This binding alters the solubility characteristics, stability, and tissue interaction properties of the pharmaceutically active compound. The complexation with albumin increases aqueous solubility and modifies the drug's pharmacokinetic profile to improve tolerability while maintaining therapeutic efficacy.
2Reliability
If pharmaceutically active compounds are administered to improve therapeutic efficacy, then treatment effectiveness increases, but aqueous solubility remains insufficient limiting drug delivery
Solution Approach 1:
The patent creates a composite formulation consisting of albumin and pharmaceutically active compounds bound together through non-covalent interactions. This composite structure combines the benefits of albumin (high aqueous solubility, biocompatibility) with the therapeutic properties of the active compound. The resulting albumin-drug complex functions as a unified delivery system that overcomes the solubility limitations of the individual drug molecule.
Solution Approach 2:
Albumin serves as an intermediary carrier that bridges the gap between the hydrophobic pharmaceutically active compound and the aqueous environment required for ocular administration. The albumin molecule provides hydrophilic surfaces and binding pockets that solubilize the drug, enabling adequate concentrations to be achieved in the aqueous tear film while maintaining the drug's biological activity.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The binding of active compounds to albumin increases solubility by at least 10% and significantly reduces eye irritation, providing a more comfortable and effective treatment for ocular conditions.
Implementation Method 1
a pharmaceutically active compound non-covalently bound to albumin
Data Source
AI summary
The present invention provides an ophthalmic composition comprising an active pharmaceutically compound non-covalently bound to albumin. The composition of the present invention is useful for treatment of ophthalmic diseases and disorders.