Cyclodextrin Inclusion Complex for Ophthalmic Drug Solubility
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Solution Overview
Problem
Current glaucoma treatments face challenges with poorly soluble compounds, leading to visual disturbances and discomfort during eye drop administration, and lack direct optic nerve protection, relying mainly on intraocular pressure reduction methods.
Innovation Solution
Development of an ophthalmic formulation using an inclusion complex of a poorly water-soluble drug entrapped in cyclodextrin or its derivatives in an aqueous solution at pH 10 or higher, allowing penetration through the corneal epithelium for direct optic nerve protection.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If poorly water-soluble drugs are used for direct optic nerve protection, then neuroprotective efficacy is improved, but solubility and deliverability to ocular tissues deteriorates
Solution Approach 1:
The patent uses cyclodextrin as an intermediary substance to solubilize the poorly water-soluble neuroprotective drug. The cyclodextrin forms an inclusion complex with the drug, enabling it to dissolve in aqueous ophthalmic solutions and deliver adequate amounts to ocular tissues while maintaining neuroprotective efficacy
Solution Approach 2:
The patent changes the chemical parameters of the drug delivery system by forming an inclusion complex with cyclodextrin, which fundamentally alters the solubility characteristics of the poorly water-soluble neuroprotective drug, enabling its use in aqueous ophthalmic formulations
2Stress or pressure
If conventional glaucoma medications are used to reduce intraocular pressure, then IOP control is improved, but direct optic nerve protection is lost
Solution Approach 1:
The patent extracts the neuroprotective function from conventional IOP-lowering mechanisms by introducing a separate poorly water-soluble neuroprotective drug that directly protects optic nerve cells, complementing rather than replacing IOP control strategies
Solution Approach 2:
The patent develops a multi-functional ophthalmic formulation that combines both IOP-lowering activity and direct neuroprotective effects in a single eye drop preparation, allowing simultaneous achievement of pressure control and optic nerve protection
3Reliability
If eye drops are administered frequently for glaucoma treatment, then therapeutic efficacy is improved, but visual disturbances and discomfort increase
Solution Approach 1:
The patent employs cyclodextrin inclusion complexes that provide stable drug delivery in a single-use ophthalmic formulation, reducing the need for frequent re-dosing and minimizing cumulative visual disturbances associated with repeated eye drop administration
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 formulation achieves effective delivery of the drug to ocular tissues, providing neuroprotection by inhibiting 11β-HSD1 and activating the Nrf2/HO-1 pathway, reducing ischemic damage and intraocular pressure while minimizing systemic side effects.
Implementation Method 1
an ophthalmic formulation comprising an inclusion complex of a poorly water soluble drug of Formula 1 entrapped in cyclodextrin or a cyclodextrin derivative in an aqueous solution at pH 10 or higher
Data Source
AI summary
Ophthalmic therapeutic agents having as pharmaceutically active ingredient a poorly water soluble drug of formula 1 are described. Specifically, an ophthalmic formulation containing an inclusion complex of a poorly soluble drug of formula 1 enclosed in cyclodextrin or a cyclodextrin derivative in an aqueous solution of pH 10 or higher is administered to a patient in need of optic nerve protection.