Lanosterol Prodrug Eye Drops for Cataract Treatment

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Solution Overview

Problem

Current treatments for cataracts are largely ineffective in reversing the condition and are often costly and associated with surgical complications, while existing drugs can only delay deterioration and not reverse cataract formation.

Innovation Solution

A composition comprising a compound of formula (I) combined with various excipients, such as solubilizers, pH modifiers, and surfactants, formulated as eye drops to treat cataracts by improving lens transparency and glutathione peroxidase activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If surgical treatment is used to treat cataract, then visual acuity is improved, but the risk of complications and cost increase

Engineering Contradiction:
Improvecure rateVSAvoidsurgical complications
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses lanosterol as an intermediary substance that mediates the treatment of cataract. Lanosterol acts as a mediator between the external environment and the lens proteins, preventing protein aggregation and maintaining lens transparency without requiring surgical intervention. This resolves the contradiction by providing an effective treatment pathway that avoids surgical complications while achieving the therapeutic goal.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical surgical intervention with a chemical/biological approach using lanosterol administration. Instead of mechanically removing the cloudy lens through surgery, the treatment uses lanosterol to chemically/biologically restore lens transparency by preventing protein aggregation, thereby substituting a mechanical system with a chemical/biological one to avoid surgical risks.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

2Duration of action of moving object

If existing cataract drugs are used, then disease progression is delayed, but the condition cannot be reversed

Engineering Contradiction:
Improveduration of drug effectVSAvoidcurative effect
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent changes the fundamental parameter of drug action from merely delaying progression to actively reversing cataract. Lanosterol achieves this by altering the biochemical parameters within the lens, specifically by preventing protein aggregation and restoring lens transparency. This parameter change enables the drug to not only extend the duration of effectiveness but also achieve a reliable curative effect by reversing the pathological condition.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If lanosterol is administered to treat cataract, then lens transparency is restored, but intraocular penetration and stability must be optimized

Engineering Contradiction:
Improvecurative effectVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent employs composite material formulation by combining lanosterol with excipients and adjuvants to create a complex ophthalmic preparation. This composite formulation optimizes the stability and intraocular penetration of lanosterol while maintaining its curative effect. The composite structure allows the active ingredient to function effectively within the complex environment of the eye, resolving the contradiction between efficacy and formulation complexity.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS12329763B2Composition of lanosterol prodrug compound, preparation method therefor and use thereof
Publication Date: 2025.06.17 OCUSUN OPHTHALMIC PHARM (GUANGZHOU) CO LTD
  • US12329763B2 patent drawing
  • US12329763B2 patent drawing
  • US12329763B2 patent drawing

AI summary

A composition includes a compound as shown in formula (I). The compound and composition can be used in the preparation of a drug for treating ophthalmic diseases.