Ocular Drug Delivery via Cyclodextrin Inclusion Complexes
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Solution Overview
Problem
Current topical ocular drug delivery methods face challenges in effectively targeting the posterior segment of the eye due to barriers such as the corneal epithelium and anterior segment structures, leading to limited bioavailability and increased systemic exposure, which can result in toxicity and reduced therapeutic efficacy.
Innovation Solution
Development of pharmaceutical formulations in solution or suspension form that utilize solubilizing agents like cyclodextrin to reduce corneal exposure and increase bioavailability at the posterior segment, specifically for ocular neovascularization treatment using kinase inhibitors like Compound-I.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If topical drugs are applied to treat posterior segment diseases, then the ease of administration is improved, but the delivery efficiency to the target site deteriorates due to corneal barriers
Solution Approach 1:
The patent employs cyclodextrin solubilizing agents as intermediaries to facilitate drug delivery. These agents form inclusion complexes with hydrophobic drugs, enabling them to penetrate the corneal epithelium more effectively while maintaining solubility in the aqueous formulation, thus resolving the contradiction between ease of topical administration and delivery efficiency to the posterior segment
Solution Approach 2:
The patent modifies the physicochemical parameters of the drug formulation by using cyclodextrin complexes. This changes the solubility, permeability, and stability characteristics of the drug, allowing it to overcome the corneal barrier while maintaining the advantages of topical administration for posterior segment delivery
2Reliability
If topical formulations are used to increase posterior segment bioavailability, then the therapeutic efficacy is improved, but the corneal exposure and potential toxicity worsen
Solution Approach 1:
Cyclodextrin acts as a protective intermediary that temporarily binds the drug molecule, reducing its direct interaction with and potential toxicity to the corneal epithelium. The inclusion complex allows controlled release of the drug at the target site while minimizing harmful effects on the cornea
Solution Approach 2:
The patent converts the potential harm of drug-cornea interaction into a benefit by using cyclodextrin to mask the hydrophobic drug molecule. The cyclodextrin-drug complex reduces corneal irritation and toxicity while maintaining or enhancing therapeutic efficacy at the posterior segment target site
3Ease of operation
If conventional topical formulations are applied, then the ease of application is maintained, but the systemic absorption and loss of substance increase
Solution Approach 1:
The cyclodextrin complex serves as a delivery vehicle that directs the drug to the posterior segment through the cornea, reducing premature systemic absorption. The inclusion complex maintains drug stability and controls release, ensuring more of the substance reaches the intended target rather than being lost to systemic circulation
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 formulations achieve higher therapeutic index and bioavailability at the posterior segment while minimizing corneal exposure, reducing toxicity and enhancing treatment efficacy for conditions like diabetic retinopathy and age-related macular degeneration.
Implementation Method 1
The solution comprises a solubilizing agent, and is suitable for delivering to the posterior segment of the eye
Data Source
AI summary
The present invention relates to topical formulations comprising a compound of the following formula:for treating ocular neovascularization. The Compound-I is present in a solution or a suspension in about 0.005% to about 5.0% w/v, such that the solution or suspension delivers the compound at the posterior segment of the eye for inhibiting VEGF in the retina and/or the choroid.