Thermosensitive Hydrogel for Sustained Anesthetic Release
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Solution Overview
Problem
There is a significant unmet need for effective post-surgical pain management that provides extended pain relief without compromising motor function, as current methods often rely on opioids, which can lead to addiction and inadequate pain control in a substantial number of patients.
Innovation Solution
A thermosensitive hydrogel-based formulation using PLGA-PEG-PLGA triblock copolymers to deliver anesthetic drugs like bupivacaine, lidocaine, and ropivacaine, which forms a gel at body temperature, allowing for controlled release and reducing the need for opioids.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If opioids are used for post-surgical pain management, then pain relief is achieved, but risk of addiction and inadequate pain control increases
Solution Approach 1:
The patent changes the chemical parameters of the anesthetic agents by using amino amide group compounds with specific molecular structures and properties. This substitution transforms the pharmacological profile from opioid-dependent to opioid-sparing mechanisms, achieving reliable pain relief through alternative neurochemical pathways while eliminating addiction risk
Solution Approach 2:
The formulation combines multiple components including anesthetic drugs, adjuvant agents, and excipients into a composite pharmaceutical composition. This composite approach synergistically enhances analgesic effectiveness while reducing reliance on any single agent, particularly opioids, thereby maintaining pain relief reliability without addiction hazards
2Duration of action of moving object
If extended regional analgesia is provided, then duration of pain relief is improved, but motor function may be compromised
Solution Approach 1:
The patent applies local quality by using adjuvant agents that selectively enhance sensory nerve blockade while sparing motor nerve function. These agents are incorporated into the formulation to modify the local pharmacological effects at the injection site, providing extended analgesia through targeted mechanisms that differentiate between sensory and motor fiber sensitivity
Solution Approach 2:
The formulation dynamics are optimized to provide time-dependent release characteristics where the extended analgesic effect is achieved through controlled drug release kinetics. The composition maintains appropriate motor function throughout the extended duration by utilizing adjuvants that progressively enhance sensory blockade without cumulative motor impairment
3Ease of operation
If single injection is used for durable pain relief, then ease of administration is improved, but achieving extended duration of action becomes difficult
Solution Approach 1:
The patent incorporates adjuvant agents into the formulation that act preliminarily to extend the duration of action. These agents are pre-combined with the anesthetic drugs in the composition, creating a synergistic effect that prolongs analgesia from a single injection without requiring multiple administrations or complex delivery systems
Solution Approach 2:
Adjuvant agents serve as intermediaries that bridge the gap between single injection administration and extended duration of action. These mediators enhance and prolong the effects of the primary anesthetic agents, allowing durable pain relief to be achieved through a single dose by facilitating sustained pharmacological activity
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 provides sustained pain relief with minimal impact on motor function, potentially reducing opioid use and facilitating earlier ambulation and physical therapy, while offering a non-opioid sensory blockade with extended regional analgesia.
Implementation Method 1
The triblock copolymer component of the formulations disclosed herein, when dissolved in aqueous media, used forms micelles that allow the polymer to exist in a solution phase at ambient or refrigerated temperatures
Implementation Method 2
forms a soft gel at body temperature
Implementation Method 3
The present invention is exemplified by using the anesthetics bupivacaine, lidocaine, and ropivacaine as active pharmaceutical ingredients (APIs). However, the compositions disclosed herein are based on a hydrogel formulation composed of a triblock copolymer component that comprises one or more of PLGA-PEG-PLGA triblock copolymers, wherein any two PLGA-PEG-PLGA triblock copolymers are non-identical in total MW. The triblock copolymer component of the formulations disclosed herein, when dissolved in aqueous media, used forms micelles that allow the polymer to exist in a solution phase at ambient or refrigerated temperatures but forms a soft gel at body temperature.
Data Source
AI summary
The present disclosure provides compositions comprising a thermosensitive hydrogel formulation of anesthetic drugs and a triblock copolymer component, and methods of use and manufacture of the compositions for management of acute pain or pain associated with surgical procedure.