Eye Treatment Formulations for Corneal Cross-Linking Delivery
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Solution Overview
Problem
Existing eye treatments for conditions like keratoconus and post-LASIK ectasia face challenges in efficiently delivering cross-linking agents, such as riboflavin, through the corneal epithelium, leading to patient discomfort and potential complications, while conventional methods may not achieve optimal cross-linking efficiency due to factors like oxygen depletion and photochemical reactions.
Innovation Solution
Formulations incorporating anesthetic, analgesic, tonicity, and shear-thinning agents, along with non-ionic surfactants and chelating agents, enhance epithelial permeability, and controlled photoactivation using pulsed light and oxygen management to optimize cross-linking in the stroma, employing multiphoton excitation and DMD technology for precise dosimetry.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If conventional methods are used to deliver cross-linking agents through the corneal epithelium, then the treatment process is simple, but cross-linking efficiency is insufficient and treatment time is prolonged
Solution Approach 1:
The patent applies preliminary action by using preparatory formulations containing zinc metalloproteinase, copper metalloproteinase, papain, bromelain, actinidin, ficain, N-acetylcysteine, ambroxol, carbocisteine, or erdosteine to enhance epithelial permeability before applying the therapeutic formulation. This preliminary treatment of the epithelium prepares it to allow more efficient penetration of the cross-linking agent, thereby improving cross-linking efficiency and reducing the time required to achieve optimal results.
2Productivity
If formulations with multiple delivery agents are used, then epithelial permeability is enhanced and cross-linking efficiency is improved, but formulation complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the formulation into two distinct parts: a preparatory formulation applied first to enhance epithelial permeability, and a therapeutic formulation containing the photosensitizer and cross-linking agent applied second. This segmentation allows each formulation to be optimized for its specific function while managing overall complexity. The preparatory formulation contains specific enzymes and permeability enhancers, while the therapeutic formulation contains the active cross-linking components.
Solution Approach 2:
The preparatory formulation serves as a preliminary action that prepares the epithelium for subsequent therapeutic agent delivery. By applying permeability-enhancing agents first, the formulation system achieves improved cross-linking efficiency without requiring all components to be present in a single complex formulation, thus managing formulation complexity while improving productivity.
3Ease of operation
If anesthetic and analgesic agents are included in the formulation, then patient discomfort is reduced, but the risk of complications from substance accumulation increases
Solution Approach 1:
The patent applies the intermediary principle by using specific delivery agents and formulation components that mediate between the therapeutic effect and potential harm. The formulation includes controlled amounts of anesthetic and analgesic agents combined with specific delivery agents that control their penetration and distribution, acting as intermediaries to provide pain relief while limiting the risk of complications from substance accumulation in the cornea.
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
Enhances cross-linking efficiency, reduces treatment time, minimizes patient discomfort, and achieves precise refractive corrections by optimizing corneal collagen bonding, addressing conditions like keratoconus and post-LASIK ectasia.
Implementation Method 1
Certain photosensitizers may be applied to the eye for eye treatments. For example, photosensitizers can generate cross-linking activity in the cornea.
Implementation Method 2
employing multiphoton excitation and DMD technology for precise dosimetry
Implementation Method 3
The one or more delivery agents may include one or more shear-thinning, viscosity-increasing agents
Data Source
AI summary
Formulations, are used for eye treatments, e.g., cross-linking treatments. For example, a therapeutic formulation includes a photosensitizer and delivery agent(s), wherein the delivery agent(s) include at least one of: anesthetic agent(s), analgesic agent(s), tonicity agent(s), or shear-thinning, or viscosity-increasing agent(s). In another example, a method includes applying preparatory formulation(s) to increase a permeability of a corneal epithelium, and applying therapeutic formulation(s) to the epithelium, where the preparatory formulation(s) include zinc metalloproteinase, copper metalloproteinase, papain, bromelain, actinidin, ficain, N-acetylcysteine, ambroxol, carbocisteine, and/or erdosteine. In yet another example, a method includes applying therapeutic formulation(s) to a corneal epithelium to deliver the therapeutic formulation(s) to a stroma, and applying enhancement formulation(s) to the epithelium in response to applying the therapeutic formulation(s), where: the enhancement formulation(s) remove the therapeutic formulation(s) from the epithelium; close tight junctions of the epithelium; promote oxidation for the therapeutic agent(s); and/or further deliver the therapeutic formulation(s) to the stroma.