Stabilised Polymeric Silicate Compositions for Resorbable Delivery

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Solution Overview

Problem

Existing silicate composition formulations face challenges in achieving bioavailability and resorbability, often forming condensed forms that are poorly absorbed, and require dilute solutions or additional administration steps, limiting their therapeutic effectiveness.

Innovation Solution

The development of stabilised polymeric silicate compositions with polymeric silicic acid and nanosilicate particles of 20 nm or less, produced through a process involving an aqueous solution of silicate at pH greater than 9.5, followed by pH reduction and addition of polyalkylene glycols or sugars to inhibit condensation, allowing for intravenous or topical administration without drying or heating above 100°C.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If silicate concentration is increased to improve therapeutic effectiveness, then the silicate undergoes self-assembly and forms condensed forms that are poorly resorbable

Engineering Contradiction:
Improvesilicate concentrationVSAvoidresorbability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

A stabilising agent is introduced as an intermediary substance that binds to silicate monomers and prevents their self-assembly into condensed forms. This mediator allows high silicate concentrations to be maintained while preserving resorbability, as the stabilising agent blocks the self-assembly pathway without preventing subsequent dissolution and absorption processes.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs parameter changes by adjusting pH levels and using stabilising agents to alter the chemical state of silicate. By controlling pH and introducing stabilising agents, the system maintains silicate in a monomeric or lightly polymeric state that is both concentrated and resorbable, resolving the contradiction between quantity and reliability.

Inventive Principle:
Principle #35Parameter changes

2Ease of manufacture

If drying or heating above 100°C is applied to produce dry lyophilised composition, then the composition can be stored and administered, but condensed silicates form with poor resorbability

Engineering Contradiction:
Improvedrying processVSAvoidresorbability
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The stabilising agent is introduced beforehand to prevent the formation of condensed silicates that would otherwise form during drying or heating. This preliminary protective action ensures that even when drying processes are applied, the silicate remains in a resorbable state because the stabilising agent prevents condensation during the drying transition.

Inventive Principle:
Principle #9Preliminary anti-action

Solution Approach 2:

The stabilising agent acts as a protective intermediary during the drying process, maintaining silicate resorbability through heat treatment. The stabilising agent prevents direct condensation of silicate monomers during heating, allowing the drying process to proceed while preserving the resorbable character of the silicate composition.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Stability of the object's composition

If pH is reduced to cause polymerisation, then polymeric silicic acid forms, but further pH reduction leads to condensed silicate formation

Engineering Contradiction:
ImprovepolymerisationVSAvoidcondensation
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The stabilising agent serves as a mediator during pH adjustment, allowing polymerisation to proceed while preventing condensation. By binding to silicate species, the stabilising agent enables controlled polymerisation at reduced pH without allowing further condensation to occur, thus maintaining composition stability while preventing harmful condensation.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent uses parameter changes by carefully controlling pH levels in conjunction with stabilising agent concentration. By adjusting pH to a specific range and maintaining appropriate stabilising agent levels, the system achieves desired polymerisation while preventing condensation, resolving the contradiction between composition stability and prevention of condensation.

Inventive Principle:
Principle #35Parameter changes

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

This approach results in stable, bioavailable silicate compositions that are capable of efficient dissolution and administration, providing therapeutic benefits for various medical conditions without the need for dilution or additional steps, and can be tailored for specific particle sizes and uses.

Implementation Method 1

The stabilising agent is capable of inhibiting condensation of the silicate monomer, in particular by steric hindrance

Methodology Applied
Scientific EffectSteric hindrance:

Implementation Method 2

reducing the pH of the silicate solution to cause polymerisation of the silicate to form polymeric silicic acid and nanosilicate particles

Methodology Applied
Scientific EffectPolymerisation:

Implementation Method 3

capable of undergoing efficient dissolution to provide bioavailable soluble silicic acid

Methodology Applied
Scientific EffectDissolution:

Data Source

PatentUS11833171B2Materials and methods relating to stabilised polymeric silicate compositions
Publication Date: 2023.12.05 UNITED KINGDOM RESEARCH AND INNOVATION
  • US11833171B2 patent drawing
  • US11833171B2 patent drawing
  • US11833171B2 patent drawing

AI summary

Stabilised and aquated polymeric silicate compositions are described in which the compositions are poorly condensed compositions in which the silicates are resorbable and are capable of undergoing efficient dissolution to provide bioavailable soluble silicic acid. In particular, stabilised and aquated polymeric silicates are described that are capable of intravenous delivery, useful in the treatment of cancer or systemic infection, or for topical administration, e.g. in the form of a solid or semi-solid ointment useful in the treatment of wounds or the prevention of bacterial infection.