Biodegradable Polymer Matrix for Controlled Prostacyclin Release
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Solution Overview
Problem
Current drug delivery systems face challenges in achieving a steady concentration of drugs in the therapeutic window, leading to inadequate efficacy or side effects due to peak-to-trough variations in blood concentration, and existing methods for prostacyclin drugs like treprostinil are associated with injection site pain and infection risks.
Innovation Solution
Development of a drug release polymer comprising prostacyclin compounds with carboxylic acid and hydroxyl groups that form ester bonds, allowing for controlled release through biodegradation, which can be administered subcutaneously or intramuscularly, avoiding peak-to-trough variations and reducing injection site issues.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If continuous subcutaneous infusion is used to achieve steady drug concentration, then peak-to-trough variation is reduced, but injection site pain and inflammation increase
Solution Approach 1:
The drug is pre-loaded into a biodegradable polymer matrix during manufacturing, creating a controlled-release formulation that maintains steady drug concentration without requiring continuous infusion. The polymer gradually degrades in the body, releasing the drug at a controlled rate over time, thereby eliminating the need for repeated injections and associated pain and inflammation.
2Reliability
If continuous infusion via indwelling catheter is used to maintain therapeutic concentration, then drug delivery is sustained, but risk of infection increases
Solution Approach 1:
The invention extracts the drug from a continuous infusion system and embeds it within a biodegradable polymer matrix that can be administered as a single injection or implant. This eliminates the need for indwelling catheters and continuous external infusion equipment, thereby removing the source of infection risk while maintaining sustained drug delivery through polymer degradation.
3Ease of operation
If conventional sustained release formulations are used, then injection frequency is reduced, but peak-to-trough concentration variation increases
Solution Approach 1:
The invention changes the release kinetics parameters by using a biodegradable polymer matrix with specific degradation characteristics. The polymer's gradual hydrolysis and enzymatic degradation provide a zero-order or near-zero-order release profile, maintaining steady drug concentration in the therapeutic window. This allows for extended dosing intervals (reducing injection frequency) while avoiding the peak-to-trough variations seen in conventional sustained-release formulations.
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 polymer achieves a steady drug concentration profile with minimal peak-to-trough variation, reducing side effects and injection site pain, while maintaining high drug loading and prolonged action, suitable for conditions like pulmonary hypertension.
Implementation Method 1
the active pharmaceutical moieties form monomeric units covalently bonded to each other to form a polymer backbone
Implementation Method 2
the active pharmaceutical moieties are capable of being released at a rate that is dependent on the extent of biodegradation of the polymer backbone
Implementation Method 3
the active pharmaceutical moieties are capable of being released at a rate that is dependent on the extent of biodegradation of the polymer backbone
Data Source
AI summary
Disclosed herein are drug release polymer compounds and compositions comprising prostacyclin compounds of Formula (I), and methods of preparing the same. A preferred polymer has a repeating unit of the following structure: