Silicon Nanoparticles With Lipid-Amino Acid Coatings for Controlled Release

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Solution Overview

Problem

Existing delivery systems for pharmaceutical and cosmetic agents face challenges in achieving controlled and slow-release of active ingredients, stability of biological compounds, penetration into deeper skin layers, and biocompatibility issues, with silicon-based carriers often leading to uncontrolled OSA polymerization and safety concerns.

Innovation Solution

Treat silicon nanoparticles with phospholipids and/or charged lipids, along with amino acids like arginine and glycine, to control the release of bioactive agents, stabilizing the silicon to form orthosilicic acid (OSA) and preventing polymerization, ensuring controlled release and biocompatibility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If silicon-based carrier material is used for controlled release delivery, then delivery control is improved, but uncontrolled OSA polymerization occurs causing safety concerns

Engineering Contradiction:
Improvecontrolled release durationVSAvoidOSA polymerization safety risks
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent introduces amino acids (arginine, glycine, histidine, or proline) as intermediary substances that complex with orthosilicic acid to prevent uncontrolled polymerization. These amino acids act as mediators between the silicon carrier material and the biological system, controlling the polymerization process while maintaining safety and bioavailability during the controlled release period.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent controls the polymerization process by changing chemical parameters - specifically by adjusting pH levels and introducing amino acid complexes that modify the polymerization kinetics. This allows the system to maintain controlled release characteristics while preventing harmful uncontrolled polymerization of orthosilicic acid.

Inventive Principle:
Principle #35Parameter changes

2Speed

If topical delivery systems are used to deliver active agents, then skin penetration is improved, but stability of biological compounds deteriorates

Engineering Contradiction:
Improveskin penetration rateVSAvoidbiological compound stability
Core Design Contradiction:
SpeedVSStability of the object's composition

Solution Approach 1:

The patent creates a composite delivery system combining silicon carrier material with amino acid complexes. This composite structure provides both the penetration enhancement needed for effective skin delivery and the stability required to protect biological compounds during transit and release, resolving the contradiction between speed of delivery and compound stability.

Inventive Principle:
Principle #40Composite materials

3Duration of action of moving object

If conventional delivery systems are used for long-term delivery, then delivery duration is improved, but residency time on skin deteriorates

Engineering Contradiction:
Improvedelivery durationVSAvoidskin residency time
Core Design Contradiction:
Duration of action of moving objectVSDuration of action of stationary object

Solution Approach 1:

The patent employs silicon carrier materials that provide continuous, sustained release of active ingredients over extended periods. The amino acid complexes ensure this release is controlled and stable, maintaining therapeutic levels continuously without requiring frequent reapplication, thus achieving both long delivery duration and adequate skin residency time.

Inventive Principle:
Principle #20Continuity of useful action

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 method allows for stable and controlled release of pharmaceutical or cosmetic agents, enhancing skin penetration and reducing safety risks by maintaining OSA in a bioavailable form, suitable for long-term delivery.

Implementation Method 1

Silicon has a structural role as a constituent of the protein-glycosaminoglycanes complexes found in the connective tissues matrix of mammals... Elemental silicon (Si) dissolves in an aqueous environment to form silicic acids

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Implementation Method 2

treating the surface of the silicon nanoparticles with one or more phospholipids and/or one or more further, charged lipids... treating the surface of the silicon nanoparticles with at least one amino acid which is arginine and/or glycine

Methodology Applied
Scientific EffectComplexation: Chemical Bonding

Implementation Method 3

treating the surface of the silicon nanoparticles with at least one amino acid which is arginine and/or glycine... stabilizing the silicon to form orthosilicic acid (OSA) and preventing polymerization

Methodology Applied
Scientific EffectComplexation: Chemical Bonding

Implementation Method 4

To enable a wider range of active ingredients to be delivered topically, considerable research has been focused on development of strategies for temporarily disrupting the stratum corneum barrier in a controllable fashion, so that drugs can permeate in sufficient and predictable quantities

Methodology Applied
Scientific EffectPermeation: Permeation

Data Source

PatentEP3946257B1A delivery system comprising silicon-containing material
Publication Date: 2025.08.27 SISAF LTD
  • EP3946257B1 patent drawingFigure 1
  • EP3946257B1 patent drawingFigure 2
  • EP3946257B1 patent drawingFigure 3

AI summary

A method for promoting the controlled binding and release of a bioactive or pharmaceutical agent from a composition comprising silicon nanoparticles, wherein the silicon nanoparticles comprise at least 50 % by weight silicon, the method comprising treating the surface of the silicon nanoparticles with at least one lipid, and treating the surface of the silicon nanoparticles with at least one amino acid, wherein the ratio of lipid to silicon isfrom1:1 to 15:1. Also related compositions and methods.