Topical Acne Gel Formulation Stable at Physiological Skin pH
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Solution Overview
Problem
Existing topical formulations of lysozyme for treating acne vulgaris are not fully satisfactory due to limited antimicrobial activity against both Gram-positive and Gram-negative bacteria, instability at physiological skin pH, and the use of ethanol or surfactants that interfere with protein stability and viscosity.
Innovation Solution
A stable gel formulation comprising lysozyme, ovotransferrin, fatty ethoxylated dimeric urethanes, and optional humectants, which maintains antimicrobial synergy and stability over time without ethanol or surfactants, using a non-ionic thickener to stabilize the proteins at physiological skin pH.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If aqueous formulations containing lysozyme are used to treat acne vulgaris, then antimicrobial activity against Gram-positive bacteria is achieved, but antimicrobial activity against Gram-negative bacteria is limited
Solution Approach 1:
The patent combines lysozyme with ovotransferrin and EDTA in a single formulation. Lysozyme provides activity against Gram-positive bacteria while ovotransferrin and EDTA extend coverage to Gram-negative bacteria, creating a synergistic combination that broadens the antimicrobial spectrum without compromising effectiveness against Gram-positive organisms.
Solution Approach 2:
The formulation uses a composite approach by integrating multiple active ingredients (lysozyme, ovotransferrin, EDTA) with specific excipients (fatty ethoxylated dimeric urethanes, humectants) to create a multi-functional gel that simultaneously addresses Gram-positive and Gram-negative bacterial infections while maintaining stability at physiological pH.
2Reliability
If ethanol or surfactants are added to extend antimicrobial activity, then Gram-negative bacteria coverage is improved, but protein stability and viscosity are compromised
Solution Approach 1:
The patent introduces fatty ethoxylated dimeric urethanes as intermediary substances that perform multiple functions: they extend antimicrobial activity against Gram-negative bacteria without the harmful effects of ethanol or surfactants, while simultaneously maintaining protein stability and appropriate viscosity through their amphiphilic structure.
Solution Approach 2:
The formulation changes the chemical parameters by using mild non-ionic surfactant-like molecules (fatty ethoxylated dimeric urethanes) instead of harsh ethanol or ionic surfactants, thereby achieving extended antimicrobial coverage while preserving the stability of lysozyme and ovotransferrin proteins at physiological pH levels.
3Stability of the object's composition
If formulations are designed to be stable at physiological skin pH, then protein stability is maintained, but antimicrobial activity against diverse bacteria is reduced
Solution Approach 1:
The patent creates a composite formulation where lysozyme and ovotransferrin work synergistically at physiological pH. Ovotransferrin's iron-binding capability and antimicrobial activity complement lysozyme's action, allowing the formulation to maintain both protein stability at skin pH and broad-spectrum antimicrobial effectiveness that would not be achievable with either protein alone.
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 formulation effectively inhibits Cutibacterium acnes, Corynebacterium species, and Staphylococcus aureus, maintaining viscosity and enzymatic activity over extended periods, including at elevated temperatures.
Implementation Method 1
Lysozyme C type is a natural protein with a molecular weight of 14,4 kDa extracted from hen eggs white (HEW) endowed with antimicrobial properties. This compound, active mainly on Gram-positive bacteria and on some viruses... Ovotransferrin, which has a molecular weight of 76 kDa, is another natural protein present in the HEW. This protein belongs to the family of transferrins; it possesses antibacterial, antioxidant and immunomodulatory activities due to its ability to bind iron
Implementation Method 2
new stable gel formulations comprising lysozyme, ovotransferrin, fatty ethoxylated dimeric urethanes , a preservative, water and optionally one or more humectants
Implementation Method 3
using a non-ionic thickener to stabilize the proteins at physiological skin pH
Implementation Method 4
The formulation effectively inhibits Cutibacterium acnes, Corynebacterium species, and Staphylococcus aureus, maintaining viscosity and enzymatic activity over extended periods, including at elevated temperatures
Data Source
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AI summary
The present invention relates to compositions and methods for the preparation of a topical gel for the treatment of acne vulgaris and, in particular, to topical gel compositions comprising lysozyme and ovotransferrin as active ingredients and ethoxylated dimeric urethanes as gelling agents.