Sorbitan Ester Nanoparticles via Spontaneous Formation

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Solution Overview

Problem

Current methods for developing nanoparticles using sorbitan esters as the main component are limited, as they typically result in microparticulate systems or unstable formulations with low encapsulation capacity and size heterogeneity, and existing techniques like emulsification-evaporation and nanoprecipitation are inefficient for producing nanoparticles with significant sorbitan ester content.

Innovation Solution

Development of nanoparticles consisting exclusively of sorbitan esters, with a proportion by weight between 60% and 100%, using a simple spontaneous formation method that does not require injection or homogenization, allowing for the incorporation of additional components to modulate physicochemical characteristics and enhance stability, and enabling the encapsulation of both lipophilic and hydrophilic active ingredients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If sorbitan esters are used as the main component in nanoparticulate systems, then the biocompatibility and lipophilic surfactant properties are improved, but the system stability and size homogeneity deteriorate

Engineering Contradiction:
ImprovebiocompatibilityVSAvoidsystem stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent uses composite materials by combining sorbitan esters with other surfactants (ionic, non-ionic, or zwitterionic) to create nanoparticulate systems that maintain the biocompatibility of sorbitan esters while adding the stability provided by the complementary surfactant components. This composite approach allows the system to benefit from both the lipophilic properties of sorbitan esters and the stabilizing effects of other surfactant types.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent applies parameter changes by carefully controlling the concentration ratios of sorbitan esters to other surfactants, adjusting hydrophilic-lipophilic balance (HLB) values, and optimizing preparation conditions to achieve stable nanoparticulate systems. By modifying these parameters, the system maintains high sorbitan ester content while achieving adequate stability and size homogeneity.

Inventive Principle:
Principle #35Parameter changes

2Manufacturing precision

If conventional methods like emulsification-evaporation or nanoprecipitation are used, then the nanoparticle formation is achieved, but the encapsulation capacity and size homogeneity are limited

Engineering Contradiction:
Improvenanoparticle formationVSAvoidencapsulation capacity
Core Design Contradiction:
Manufacturing precisionVSQuantity of substance

Solution Approach 1:

The patent introduces other surfactants as intermediaries that facilitate the encapsulation of active ingredients within the nanoparticulate system. These intermediary surfactants help to stabilize the interface between the lipophilic sorbitan ester core and the aqueous phase, thereby enhancing the encapsulation capacity for both lipophilic and hydrophilic substances while maintaining nanoparticle size homogeneity.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If high proportions of sorbitan esters (60-100% by weight) are used, then the surfactant properties and biocompatibility are enhanced, but the formulation stability and reproducibility worsen

Engineering Contradiction:
Improvesurfactant propertiesVSAvoidformulation reproducibility
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent systematically optimizes the concentration parameters of sorbitan esters within the 60-100% by weight range, while simultaneously adjusting the concentrations and types of complementary surfactants. This parameter optimization approach enables the formulation to achieve both high sorbitan ester content for enhanced surfactant properties and adequate formulation reproducibility through balanced composition design.

Inventive Principle:
Principle #35Parameter changes

4Ease of operation

If sorbitan esters are used in low concentrations as surfactants, then the surfactant function is maintained, but the encapsulation capacity and nanoparticle stability deteriorate

Engineering Contradiction:
Improvesurfactant functionVSAvoidencapsulation capacity
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

The patent employs composite material strategy by formulating nanoparticulate systems where sorbitan esters constitute the major component (60-100% by weight) combined with other surfactants. This composite structure enables the system to provide both adequate surfactant function for ease of operation and enhanced encapsulation capacity through the synergistic effects of multiple surfactant types working together.

Inventive Principle:
Principle #40Composite materials

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 resulting nanoparticles are stable, have a homogenous size distribution, and exhibit improved encapsulation capacity, making them suitable for drug release and absorption promotion, while maintaining biological activity and stability during storage.

Implementation Method 1

The present invention provides a method of preparation of said nanoparticulate system characterized by the spontaneous formation occurring in a single step

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

Sorbitan esters are frequently used in the pharmaceutical industry. The use thereof is due to their properties as lipophilic non-ionic surfactants

Methodology Applied
Scientific EffectSurfactant action: Surfactant

Implementation Method 3

nanoparticles capable of encapsulating substances

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 4

enabling the encapsulation of both lipophilic and hydrophilic active ingredients

Methodology Applied
Scientific EffectAbsorption: Absorption (physical)

Data Source

PatentEP2792350B1Nanoparticulate systems prepared from sorbitan esters
Publication Date: 2020.12.30 UNIVERSITY OF SANTIAGO DE COMPOSTELA
  • EP2792350B1 patent drawingFigure 1~2D
  • EP2792350B1 patent drawingFigure 3~4
  • EP2792350B1 patent drawingFigure 5~6

AI summary

The invention relates to systems comprising homogenous nanoparticles having an average size of less than 1 micrometer and containing at least a sorbitan ester, a macrogol ester, a macrogol ether or a derivative of same and, optionally, at least one component derived from oxyethylene and/or at least one component having an electric charge (positive or negative). According to the invention, the components are incorporated in a single step consisting in mixing two solutions. The invention also relates to the use of said systems as medicines or medical devices, in tissue engineering or regenerative medicine, for cosmetic, hygienic or nutritional uses, and in surface coatings. The invention further relates to methods for preparing same.