Injectable Biodegradable Copolymer Sustained Release for Ocular Delivery
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Solution Overview
Problem
Current treatments for ocular disorders, such as age-related macular degeneration, require frequent injections into the eye, which can be painful and require professional training. Additionally, topical treatments like eye drops are ineffective for diseases affecting the posterior segment of the eye due to poor penetration.
Innovation Solution
A sustained-release formulation using an injectable bioabsorbable copolymer composed of trimethylene carbonate (TMC) and polylactide (PLA), combined with a pharmaceutically acceptable excipient, 1,2,3-triacetoxypropane, and a bioactive agent, which forms a solid/gel structure in the tissue site for delayed release of the bioactive agent.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If topical treatments like eye drops are used, then the treatment is easy to apply, but the treatment is ineffective for diseases of the posterior segment of the eye due to poor penetration
Solution Approach 1:
The patent uses an injectable polymer formulation as an intermediary delivery system that bypasses the limitation of topical application. The polymer acts as a carrier that can be directly injected into the vitreous humor, serving as a mediator between the drug and the target tissue in the posterior segment, thereby achieving both effective delivery and sustained release.
Solution Approach 2:
The patent employs injection technology to deliver the polymer formulation directly into the ocular tissue. This hydraulic method allows the treatment to bypass the corneal barrier that prevents effective penetration of topical drops, enabling direct delivery to the posterior segment while maintaining ease of administration through a simple injection procedure.
2Reliability
If direct injection into the eye is performed to deliver bioactive agent to target site, then the treatment effectiveness is improved, but the frequency and number of injections required increases
Solution Approach 1:
The patent incorporates the bioactive agent within the injectable polymer formulation before administration. This preliminary encapsulation allows the drug to be delivered in a sustained-release format, providing therapeutic effects over an extended period and reducing the frequency of repeat injections compared to conventional immediate-release formulations.
Solution Approach 2:
The patent changes the physical and chemical parameters of the drug delivery system by using a biodegradable polymer matrix. This formulation modification alters the release kinetics of the bioactive agent, transforming it from rapid clearance to sustained release, thereby extending the duration of action and reducing injection frequency while maintaining treatment effectiveness.
3Reliability
If conventional needles and syringes are used for injection, then the bioactive agent can be delivered to the target site, but professional training is required and multiple injections are needed
Solution Approach 1:
The patent uses a composite injectable formulation consisting of a polymer matrix combined with the bioactive agent. This composite material provides both structural integrity for controlled release and biocompatibility for safe injection, eliminating the need for complex specialized devices while maintaining delivery accuracy through the formulation's inherent properties.
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 allows for an extended or sustained release of the bioactive agent, reducing the frequency of injections and improving therapeutic efficacy by maintaining effective drug levels at the target site for an extended period.
Implementation Method 1
an injectable bioabsorbable copolymer having repeating units of trimethylene carbonate (TMC) and polylactide (PLA)
Implementation Method 2
forms a solid/gel structure in the tissue site for delayed release of the bioactive agent
Data Source
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AI summary
The present disclosure is directed to injectable formulations that include biodegradable polymers based on trimethylene carbonate (TMC) with mole fractions of polylactic acid (PLA) and/or polyglycolic acid (PGA) that are used to deliver a bioactive agent to a targeted site. Excipients such as polyethylene glycol (PEG) may be added to the formulations to reduce the injection force and/or to modulate the release of the bioactive agent. Suitable biodegradable polymers for use in the injectable formulations include D,L-PLA:TMC, D-PLA:TMC, L-PLA:TMC, TMC:PLA:PGA and variations thereof. Additionally, copolymers of TMC and PLA and terpolymers of TMC:PLA:PGA may be formed into nanoparticles and delivered to the target site with an injectable crosslinkable polyethylene glycol system. In at least one embodiment, the injectable formulations are used to treat ocular diseases.