Biodegradable Polymeric Peptide Delivery System
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Solution Overview
Problem
Current peptide delivery systems face challenges due to peptide instability, leading to short circulation half-life and the need for frequent injections, which are painful, costly, and inconvenient. Existing biodegradable polymer-based delivery systems often result in interactions between peptide agents and polymers, causing degradation and stability issues, and require complex manufacturing processes.
Innovation Solution
A stabilized injectable biodegradable polymeric composition using a salt of a peptide agent formed with a strong acid, combined with a biodegradable polymer and a pharmaceutically acceptable organic solvent, to minimize interactions and provide a controlled release of peptides over extended periods, allowing for a single syringe pre-filled configuration with improved stability and convenience.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If peptide agents are administered by injection multiple times per day, then the peptide stability is maintained, but the patient compliance becomes very challenging and the treatment becomes painful and inconvenient
Solution Approach 1:
The peptide delivery system is segmented into biodegradable polymer microparticles that encapsulate the peptide agent, allowing controlled release over extended periods. This segmentation enables the peptide to be delivered continuously at a controlled rate without requiring frequent injections, thereby maintaining stability while improving patient compliance
Solution Approach 2:
The peptide agent is pre-encapsulated within biodegradable polymer matrices before administration. This preliminary action of encapsulation protects the peptide from degradation and enables sustained release, eliminating the need for multiple daily injections while maintaining peptide stability throughout the extended release period
2Duration of action of stationary object
If peptide agents are incorporated in biodegradable polymer matrices, then the controlled release over long period is achieved, but the interaction between peptide and polymer causes degradation
Solution Approach 1:
A coating layer is introduced as an intermediary between the peptide agent and the biodegradable polymer matrix. This coating prevents direct interaction and degradation reactions between the peptide and polymer while allowing controlled release of the peptide over the desired time period, thereby maintaining both release duration and peptide stability
3Duration of action of stationary object
If microparticle suspension forms are used, then the controlled release is achieved, but the large volume of suspending fluids is required
Solution Approach 1:
The invention uses solid rod implant forms with thin biodegradable polymer coatings instead of microparticle suspensions. This approach eliminates the need for large volumes of suspending fluids while maintaining controlled release capabilities, as the solid rod form provides structural integrity and controlled degradation without requiring suspension media
4Duration of action of stationary object
If solid rod implants are used, then the controlled release is achieved, but the surgical insertion is required
Solution Approach 1:
The invention employs biodegradable polymer coatings on solid rod implants that dynamically degrade over time through hydrolysis and enzymolysis. This dynamic degradation process allows the solid rod to be inserted via simple injection rather than surgical implantation, as the polymer gradually breaks down to release the peptide agent, combining the advantages of both solid rod stability and easy administration
5Duration of action of stationary object
If biodegradable polymers are used, then the sustained release is achieved, but the manufacturing process becomes complicated
Solution Approach 1:
The invention merges the peptide agent with biodegradable polymer coatings in a single integrated solid rod implant formulation. This combining of components simplifies the manufacturing process by eliminating the need for complex multi-step encapsulation and assembly procedures required for microparticles, while maintaining sustained release capabilities through the polymer's controlled degradation
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 solution enables a stable, convenient, and cost-effective controlled release of peptide agents, such as LHRH agonists or antagonists, over 1, 3, or 6 months, with enhanced storage stability and tailored release profiles, reducing degradation and manufacturing complexity.
Implementation Method 1
These polyesters are biocompatible and degraded by typical biochemical pathways, such as hydrolysis and enzymolysis
Implementation Method 2
These polyesters are biocompatible and degraded by typical biochemical pathways, such as hydrolysis and enzymolysis
Implementation Method 3
When the liquid composition is injected into the body, the solvent dissipates into the surrounding aqueous environment
Data Source
AI summary
The present invention provides for a stabilized biodegradable polymeric composition useful as a controlled release delivery system for peptide agents. The compositions of the present invention comprise a) a strong acid salt and a weak acid of a LHRH agonist or antagonist; b) a biodegradable polymer of poly(lactide-co-glycolide), wherein the ratio of lactide:glycolide of the copolymer is from 50:50 to about 100:0; and c) N-methyl-2-pyrrolidone (NMP), wherein the composition does not contain excess strong acid in addition to the strong acid used to form the salt of the LHRH agonist or antagonist. The composition, when injected, can provide a controlled release of leuprolide for a period of up to 6 months.