Vaginal Hydrogel with Thiol Crosslinking for pH-Matched Drug Delivery

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Solution Overview

Problem

Current treatments for vaginitis, such as intravaginal creams and systemic oral medications, face issues like messiness, reduced efficacy due to drug loss through vaginal secretions, pH imbalances, and side effects from systemic treatments, which do not effectively address vaginal dryness, infection, and inflammation simultaneously, especially since they are not formulated at the optimal pH of 3.2-5.0 for the vaginal environment.

Innovation Solution

Development of hydrogels with a pH between 3.2 and 5.0, incorporating glycosaminoglycans with thiol groups and thiol-reactive sites, and mucoadhesive agents like methylcellulose, which are covalently or ionically crosslinked to provide moisture and deliver therapeutic agents like antibacterial and anti-inflammatory agents, maintaining stability and efficacy within the vaginal environment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If intravaginal creams and gels are used to treat vaginitis, then the drug delivery is improved, but the messiness and drug loss through vaginal secretions worsen

Engineering Contradiction:
Improvedrug delivery efficacyVSAvoiddrug loss through vaginal secretions
Core Design Contradiction:
ReliabilityVSLoss of substance

Solution Approach 1:

The patent changes the pH parameter of the hydrogel formulation to match the vaginal environment (pH 3.2-5.0), which improves drug stability and reduces drug loss through vaginal secretions while maintaining delivery efficacy

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses composite hydrogel materials incorporating glycosaminoglycans with thiol groups and thiol-reactive sites that form crosslinked networks, creating a matrix that reduces drug loss through vaginal secretions while maintaining delivery effectiveness

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If systemic oral treatments are used to treat vaginitis, then the treatment coverage is improved, but the side effects worsen

Engineering Contradiction:
Improvetreatment coverageVSAvoidside effects
Core Design Contradiction:
Adaptability or versatilityVSObject-generated harmful factors

Solution Approach 1:

The patent delivers therapeutic agents locally via vaginal hydrogel administration, concentrating the drug action at the site of infection (vagina) rather than systemically, which treats the condition effectively while minimizing side effects throughout the body

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The hydrogel acts as an intermediary carrier that delivers therapeutic agents directly to the vaginal tissue, enabling localized treatment without the need for systemic absorption and associated side effects

Inventive Principle:
Principle #24Intermediary (Mediator)

3Stability of the object's composition

If hydrogels are formulated at standard physiological pH (7.4), then the hydrogel stability is improved, but the vaginal environment compatibility worsens

Engineering Contradiction:
Improvehydrogel stabilityVSAvoidpH imbalance in vaginal environment
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent adjusts the pH parameter of the hydrogel formulation from standard physiological pH (7.4) to match the vaginal environment (pH 3.2-5.0), which maintains hydrogel stability while ensuring compatibility with the vaginal microflora and preventing pH imbalance

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent formulates the hydrogel with locally appropriate pH characteristics (pH 3.2-5.0) that match the vaginal environment, creating a formulation that is both stable and compatible with the specific biological conditions of the vagina

Inventive Principle:
Principle #3Local quality

4Reliability

If current treatments are used to address vaginal dryness, infection, or inflammation, then the specific symptom treatment is improved, but the simultaneous treatment of multiple aspects worsens

Engineering Contradiction:
Improvesymptom treatment efficacyVSAvoidsimultaneous treatment capability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent creates a multi-functional hydrogel formulation that simultaneously addresses vaginal dryness, infection, and inflammation by incorporating multiple therapeutic agents and moisture-retaining components in a single product, eliminating the need for separate treatments for each condition

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

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 hydrogels effectively treat vaginal dryness, infection, and inflammation while maintaining stability and delivering therapeutic agents, ensuring prolonged action and minimizing side effects by matching the vaginal pH, thus addressing the limitations of existing treatments.

Implementation Method 1

These hydrogels can be based on natural or synthetic materials, or a combination of the two. Typically, hydrogels will be crosslinked, either through physical interaction—such as simple entanglement, hydrogen bonding, or ionic interaction—or through covalent bonds.

Methodology Applied
Scientific EffectCovalent bonding: Chemical Bonding

Implementation Method 2

the average pH of the vagina is typically between about 3.2 and 5.0, an environment that favors microflora that are beneficial to the vagina. If the pH of the vagina is increased, a shift in the balance of the microflora occurs

Methodology Applied
Scientific EffectpH buffering:

Implementation Method 3

The composition includes a glycosaminoglycan which has thiol groups and a molecule that has at least 2 thiol-reactive sites

Methodology Applied
Scientific EffectThiol-reactive crosslinking: Chemical Bonding

Data Source

PatentUS20240165238A1Vaginal Hydrogel
Publication Date: 2024.05.23 MANN BRENDA K
  • US20240165238A1 patent drawing
  • US20240165238A1 patent drawing
  • US20240165238A1 patent drawing

AI summary

The vaginal hydrogel may be a composition which includes a glycosaminoglycan, a reactive molecule, and, in some embodiments, a therapeutic agent. The glycosaminoglycan and the reactive molecule may include either thiol groups or thiol reactive sites and have a pH that is within a range of a normal vaginal environment. Some of the thiol groups may interact with the vaginal mucosa and allow the hydrogel to remain in the vagina for a longer period than existing compounds intended for intravaginal administration. Therapeutic agents may be included in the composition. In these embodiments, the hydrogel acts as a vehicle which delivers the therapeutic agent.