Liraglutide Microneedle Composition for Denaturation Control
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Solution Overview
Problem
Liraglutide-containing microneedles face issues with denaturation during manufacturing and storage, leading to reduced stability and activity, which are not adequately addressed by existing formulations.
Innovation Solution
A composition comprising liraglutide, a biodegradable polymer (hyaluronic acid or carboxymethyl cellulose), a stabilizer (trehalose or xylitol), and an antioxidant (EDTA or dipotassium glycyrrhizinate) is used to prevent denaturation and enhance stability during manufacturing and storage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If liraglutide is formulated as microneedles for transdermal delivery, then patient convenience and adherence are improved, but liraglutide denaturation occurs during manufacturing and storage, reducing stability and activity
Solution Approach 1:
The patent introduces specific excipients as intermediary substances to protect liraglutide from denaturation. These include hydrophilic polymers (hydroxypropyl cellulose, carboxymethyl cellulose sodium), amino acids (arginine, lysine, histidine, phenylalanine, tyrosine, tryptophan), and sugars (trehalose, sucrose, galactose, lactose, maltose, glucose) that act as stabilizing agents between liraglutide and the microneedle matrix, preventing structural degradation while enabling transdermal delivery formulation
Solution Approach 2:
The patent optimizes formulation parameters including pH control (using citric acid and sodium hydroxide to maintain stable pH), concentration ratios of excipients to liraglutide, and physical conditions during manufacturing to prevent denaturation. By adjusting these parameters, the formulation maintains liraglutide stability throughout the microneedle lifecycle from manufacturing to storage to delivery
2Ease of manufacture
If conventional microneedle manufacturing methods are used, then production is simplified, but liraglutide denaturation occurs leading to reduced activity
Solution Approach 1:
The patent incorporates stabilizing excipients into the formulation before microneedle manufacturing begins. These protective agents are pre-mixed with liraglutide to create a stabilized formulation that is then processed into microneedles, ensuring protection is in place before any potential denaturation can occur during subsequent manufacturing steps
Solution Approach 2:
The patent creates a composite microneedle formulation combining liraglutide with multiple stabilizing excipients (polymers, amino acids, sugars, pH adjusters) in specific compositions. This composite material approach allows the formulation to maintain liraglutide stability while enabling conventional microneedle manufacturing processes without requiring complex additional equipment or procedures
3Duration of action of stationary object
If liraglutide is stored after manufacturing, then treatment can be delayed for future use, but denaturation occurs during storage reducing stability
Solution Approach 1:
The patent builds in protective cushioning by incorporating stabilizing excipients that create a protective environment around liraglutide molecules during storage. These excipients (hydrophilic polymers, amino acids, sugars) form a protective matrix that cushions liraglutide against environmental stressors such as moisture, temperature fluctuations, and physical stress during storage, thereby maintaining stability over extended periods
Solution Approach 2:
The formulation creates an inert-protective microenvironment through the use of stabilizing excipients that minimize liraglutide's exposure to degrading factors during storage. The combination of hydrophilic polymers, amino acids, and sugars creates a protective formulation environment that isolates liraglutide from harmful interactions, effectively creating a chemically protective atmosphere within the microneedle structure
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 composition maintains liraglutide's stability and activity by preventing denaturation, ensuring effective transdermal delivery and treatment efficacy for obesity and type 2 diabetes.
Implementation Method 1
compositions for manufacturing microneedles containing these biodegradable polymers can prevent denaturation of liraglutide during microneedle manufacturing and storage, thereby increasing stability
Implementation Method 2
compositions for manufacturing microneedles containing these stabilizers enable stable manufacturing of microneedles while preventing denaturation of liraglutide during microneedle manufacturing and storage to enhance stability
Implementation Method 3
compositions for manufacturing microneedles containing these antioxidants can prevent denaturation of liraglutide during microneedle manufacturing and storage to enhance stability
Data Source
AI summary
The present invention provides a composition for manufacturing liraglutide-containing microneedles that contains liraglutide as an active ingredient, without denaturation of the active ingredient during manufacture, and maintains stability even after manufacture, and liraglutide-containing microneedles with enhanced stability manufactured using the composition. The composition for manufacturing liraglutide-containing microneedles according to the present invention uses a specific combination of a biodegradable polymer, a stabilizer and an antioxidant to prevent the denaturation of the active ingredient liraglutide during the manufacture of microneedles and to ensure that the stability of liraglutide is maintained after the manufacture of microneedles.