Multiple Emulsion Stability via Poloxamer and Triacylglycerides
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Solution Overview
Problem
Multiple water-in-oil-in-water emulsions are unstable due to phase boundary interfaces, making it difficult to transfer formulations between applications and protecting sensitive active ingredients like oligonucleotides, which are prone to degradation and microbial infestation, especially during large-scale production.
Innovation Solution
A multiple emulsion with an outer water phase containing a hydrophilic emulsifier like Poloxamer 407, an oil phase of triacylglycerides, and an inner water phase with a lipophilic emulsifier such as Cetyl PEG/PPG-10/1 Dimethicone, along with alkali or alkaline earth metal halides and sulfates, providing stability and protection for sensitive active ingredients like oligonucleotides.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional W/O/W emulsions are used, then they can encapsulate sensitive active ingredients, but they exhibit poor long-term stability and are prone to phase separation and microbial infestation
Solution Approach 1:
The patent applies parameter changes by selecting specific emulsifiers with defined HLB values (hydrophilic emulsifier: 10-16, lipophilic emulsifier: 3-8), controlling electrolyte concentrations (0.1-5% w/w), and setting pH ranges (4-8) to achieve stable multiple emulsions that resist phase separation and microbial growth over long periods
Solution Approach 2:
The patent uses composite materials by combining specific pairs of hydrophilic and lipophilic emulsifiers, adding electrolytes (salts), and incorporating preservatives to create a multi-component system that provides both structural stability and microbial protection, preventing both phase separation and microbial infestation simultaneously
2Reliability
If the composition of multiple emulsion is modified to improve stability, then protection of active ingredient is enhanced, but the formulation cannot be transferred to other applications
Solution Approach 1:
The patent achieves universality by establishing general formulation guidelines with emulsifier HLB value ranges, electrolyte concentration ranges, and pH ranges that can be applied across different active ingredients and applications, allowing stable multiple emulsion formulations to be transferred and adapted to various uses
3Object-affected harmful factors
If sensitive active ingredients like oligonucleotides are enclosed in inner water phase, then protection from external influences is achieved, but diffusion properties may be compromised
Solution Approach 1:
The patent applies parameter changes by controlling the pH (4-8) and ionic strength (electrolyte concentration 0.1-5% w/w) of the inner water phase to maintain both the stability of sensitive active ingredients like oligonucleotides and their ability to diffuse when needed, balancing protection and release
Data Source
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AI summary
The invention relates to a multiple emulsion for the application of at least one pharmaceutical or cosmetic active ingredient which has an external water phase W1, an oil phase O dispersed in the external water phase W1 and an internal water phase W2 dispersed in the oil phase O, where, in the internal water phase W2, at least one electrolyte selected from the group of the alkali metal and alkaline earth metal halides and sulphates and at least one hydrophilic active ingredient is provided. In order to achieve a high stability of the emulsion, the invention envisages that the external water phase comprises a hydrophilic emulsifier which is a polymer of ethylene oxide and propylene oxide, and that the oil phase O is formed by triacylglycerides and has a lipophilic emulsifier from the group of dimethicones. Also provided is the use of such a multiple emulsion for producing a medicament, a medicinal product or a cosmetic, in particular a medicament for topical use or for application of the active ingredient via mucosa or for the intraperitoneal application of the active ingredient.