Epidermal Lipid Microparticles Mannitol Spray-Drying

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Solution Overview

Problem

Existing methods for preparing solid microparticles from epidermal lipids like cholesterol, ceramides, and fatty acids using spray-drying face challenges such as agglomeration and non-homogeneous particle-size distribution, limiting their effectiveness in cosmetic and pharmaceutical applications.

Innovation Solution

Incorporating a polyalcohol like mannitol into the spray-drying process, at a weight ratio of 5% to 20% based on the weight of lipids, to enhance the formation of well-defined microparticles with a mean diameter of 20 to 25 µm, improving yield and preventing aggregate formation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If spray-drying is used to prepare solid microparticles from epidermal lipids, then microparticles can be formed, but agglomeration occurs and particle-size distribution becomes non-homogeneous

Engineering Contradiction:
Improveparticle-size distributionVSAvoidmicroparticle formation quality
Core Design Contradiction:
Manufacturing precisionVSReliability

Solution Approach 1:

A polyol compound is introduced as an intermediary substance in the spray-drying process. This polyol acts as a mediator between the epidermal lipids and the spray-drying conditions, modifying the physical-chemical properties of the solution to prevent agglomeration and achieve homogeneous particle-size distribution. The polyol facilitates controlled microparticle formation while maintaining the integrity of the lipid components.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical-chemical parameters of the spray-drying process by incorporating a polyol compound with specific molecular weight and hydrophilicity characteristics. This parameter modification alters the evaporation rate, solution viscosity, and interfacial tension, thereby controlling microparticle formation and preventing agglomeration to achieve uniform particle-size distribution.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If non-micronized lipids are used in cosmetic formulations, then occlusive properties are achieved, but the surface layer is easily removed by cleansers and mechanical agents

Engineering Contradiction:
Improveprotective effectivenessVSAvoidsurface layer stability
Core Design Contradiction:
ReliabilityVSStrength

Solution Approach 1:

The lipid material is segmented into microparticle form through spray-drying. This segmentation creates discrete, stable particles that can penetrate and adhere to the skin barrier more effectively than bulk lipids. The microparticles maintain occlusive properties while resisting removal by cleansers and mechanical agents due to their enhanced surface area and adhesion characteristics.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite structure where epidermal lipids are incorporated into microparticle matrices. This composite formation combines the occlusive properties of lipids with the stability and adhesion characteristics of microparticle structures, resulting in a surface layer that is both protective and resistant to removal by common cleansers and mechanical agents.

Inventive Principle:
Principle #40Composite materials

3Productivity

If spray-drying is used without polyalcohol, then the process is simpler, but microparticles form agglomerates and yield is reduced

Engineering Contradiction:
Improvemicroparticle yieldVSAvoidspray-drying process complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

A polyol compound is introduced as an intermediary substance in the spray-drying process. This polyol acts as a mediator between the epidermal lipids and the spray-drying conditions, modifying the physical-chemical properties of the solution to prevent agglomeration and achieve homogeneous particle-size distribution. The polyol facilitates controlled microparticle formation while maintaining the integrity of the lipid components.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical-chemical parameters of the spray-drying process by incorporating a polyol compound with specific molecular weight and hydrophilicity characteristics. This parameter modification alters the evaporation rate, solution viscosity, and interfacial tension, thereby controlling microparticle formation and preventing agglomeration to achieve uniform particle-size distribution.

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

The method significantly increases the yield of microparticles and ensures a homogeneous particle-size distribution, enhancing their occlusive properties and stability, making them suitable for topical cosmetic and pharmaceutical compositions without affecting flowability or structural properties.

Implementation Method 1

a solution or suspension containing one or more active ingredients and carriers in a suitable aqueous and/or organic solvent, is mixed with an inert gas, usually nitrogen, and run through a suitably heated nozzle (spray nozzle), to form a cloud of droplets from which the solvent evaporates, leaving solid particles

Methodology Applied
Scientific EffectEvaporation: Evaporation

Implementation Method 2

adding a polyalcohol, particularly mannitol, to the starting solution or suspension

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentEP2547312B1Microparticles of epidermal lipids containing polyalcohol for the preparation of cosmetic and pharmaceutical compositions
Publication Date: 2017.12.06 UNIFARCO SPA
  • EP2547312B1 patent drawingFigure 1
  • EP2547312B1 patent drawingFigure 2
  • EP2547312B1 patent drawingFigure 3

AI summary

The present invention relates to solid microparticles for preparing cosmetic or pharmaceutical compositions to restore skin integrity, promoting rehydration, maintaining hydration and attenuating and preventing roughness. The solid microparticles of the invention contain epidermal lipids, such as cholesterol, ceramides and fatty acids and a polyalcohol, preferably mannitol. The invention also relates to a process for preparing said microparticles by spray- drying. The solid microparticles of the invention are particularly advantageous because they are stable and may be incorporated in excipients and/or carriers for cosmetic or pharmaceutical use, without affecting flowability and without imparting oiliness to the finished product.