Bi-functional Copolymer for Ocular Surface Hydration and Infection Control

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Solution Overview

Problem

Current pharmaceutical formulations for ocular surfaces fail to provide sustained hydration and protection against infection, with limited duration of action and inadequate prevention of bacterial adhesion, leading to discomfort and dry eye syndrome.

Innovation Solution

A bi-functional polymer composition with a positively charged or hydrophobic moiety and a hydrophilic moiety is applied topically or locally to modify the wettability and tribological properties of ocular surfaces, enhancing hydration and reducing bacterial adhesion through prolonged contact with the cornea and conjunctiva.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If conventional pharmaceutical formulations are used for ocular surfaces, then basic lubrication is provided, but sustained hydration and protection against infection are not achieved

Engineering Contradiction:
Improveduration of actionVSAvoidprotection against infection
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent employs a copolymer comprising a cationic polymer and a hydrophilic polymer as a composite material. The cationic polymer provides antimicrobial properties and prolonged adhesion to the ocular surface, while the hydrophilic polymer ensures sustained hydration. This composite structure resolves the contradiction by combining materials with complementary functions to achieve both long duration of action and reliable infection protection.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The copolymer formulation is designed to perform multiple functions simultaneously: lubrication, sustained hydration, and protection against bacterial and fungal infections. By integrating these diverse functions into a single pharmaceutical formulation, the patent achieves reliable multi-functional performance that conventional single-function formulations cannot provide, thereby resolving the contradiction between duration and reliability.

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Duration of action of stationary object

If conventional formulations are applied to ocular surfaces, then temporary relief is provided, but prolonged prevention of bacterial adhesion is not achieved

Engineering Contradiction:
Improveduration of protectionVSAvoidbacterial adhesion
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The copolymer of cationic and hydrophilic polymers creates a composite material that simultaneously provides prolonged adhesion to the ocular surface and sustained antimicrobial activity. The cationic component maintains long-term presence on the surface while actively preventing bacterial adhesion, and the hydrophilic component ensures continuous hydration to support prolonged protection, achieving both extended duration and effective harm prevention.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent utilizes a pharmaceutical formulation that can be applied repeatedly as artificial tears or eye drops. Each application provides a new supply of the copolymer that adheres to the ocular surface and provides prolonged protection. This approach allows for sustained protection through multiple applications of a relatively simple formulation, achieving long-term prevention of bacterial adhesion.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Stability of the object's composition

If the ocular surface is kept hydrated, then comfort is improved, but bacterial growth risk increases due to prolonged moisture

Engineering Contradiction:
Improvehydration stabilityVSAvoidbacterial growth
Core Design Contradiction:
Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The copolymer formulation combines a hydrophilic polymer that provides sustained hydration with a cationic polymer that delivers antimicrobial protection. The hydrophilic component maintains stable hydration to improve comfort, while the cationic component simultaneously prevents bacterial growth by disrupting microbial cell membranes. This composite material resolves the contradiction by incorporating two functional components that work together to provide both hydration stability and protection against harmful bacterial growth.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent converts the potential harm of prolonged moisture (which could promote bacterial growth) into a benefit by using the hydrated environment to enhance the effectiveness of the cationic polymer's antimicrobial action. The cationic polymer remains stable and active in the hydrated environment, and the moisture facilitates its contact with and disruption of bacterial cell membranes, thereby preventing infection while maintaining comfort.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

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 bi-functional polymer composition significantly prolongs tear film stability, reduces bacterial adhesion, and enhances ocular surface hydration, providing prolonged relief from dry eye syndrome and discomfort.

Implementation Method 1

The PLL chain, which carries multiple positive charges, spontaneously adsorbs onto negatively charged surfaces while PEG is a polynonion which serves as a non-binding domain. This adsorption is strong and occurs rapidly, and renders surfaces protein and cell resistant.

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 2

contacting the surface with a composition containing a copolymer having a positively charged, or hydrophobic or covalent bonding moiety and a hydrophilic moiety, where the contacting is effected in an amount and for a duration so as to increase the wettability or treat discomfort of the biological surface

Methodology Applied
Scientific EffectWetting: Wetting

Data Source

PatentUS20220023334A1Bi-functional co-polymer use for ophthalmic and other topical and local applications
Publication Date: 2022.01.27 CALM WATER THERAPEUTICS LLC
  • US20220023334A1 patent drawing
  • US20220023334A1 patent drawing
  • US20220023334A1 patent drawing

AI summary

The invention contemplates a copolymer which is a graft or block copolymer useful to change the ocular surface temperature and other characteristics of biological or contact lens surfaces. Methods for use of these formulations and coatings to increase the temperature of the skin, mucous membranes, eye or eyelids will help treat many conditions including blepharitis and non-healing ulcers. Methods to decrease evaporation, improve wettability and stabilize the tear film, and lubricate biological surfaces in a subject, for example, in the treatment of dry eye syndrome, and to improve contact lens tolerability, are provided.