Ocular Composition for Controlled Therapeutic Release
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Solution Overview
Problem
Current methods for delivering therapeutic agents to the posterior segment of the eye face challenges due to ocular barriers, resulting in low therapeutic agent levels and toxicity, making it difficult to treat chronic retinal diseases effectively.
Innovation Solution
An ocular composition comprising at least 20% w/w of a therapeutic agent, 5 to 75% w/w of a photopolymerizable composition, and 0.1 to 40% w/w of a biodegradable polymer, which forms a crosslinked polymer matrix for controlled release, allowing high loading and reduced implant size without burst releases, enabling administration via narrow needles with minimal tissue trauma.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high concentrations of therapeutic agent are administered to overcome ocular barriers, then therapeutic efficacy is improved, but therapeutic agent-related toxicity increases
Solution Approach 1:
The therapeutic agent is segmented into controlled release units through incorporation into ocular implants or delivery systems with specific release kinetics, allowing the agent to be delivered in controlled amounts over time rather than as a single high-concentration dose, thereby maintaining efficacy while reducing peak toxicity
Solution Approach 2:
The therapeutic agent is pre-loaded into ocular implants or delivery devices at high concentrations during manufacturing, but the actual release to the ocular tissue is controlled and gradual, separating the loading concentration from the release profile to avoid toxicity while ensuring sufficient drug availability
2Adaptability or versatility
If large molecules like proteins and peptides are administered to treat chronic retinal diseases, then therapeutic coverage is improved, but delivery difficulty increases due to ocular barriers
Solution Approach 1:
The delivery system parameters are optimized for large molecules by adjusting implant composition, molecular weight, crosslinking density, and release kinetics to accommodate the slower diffusion and different pharmacokinetics of proteins and peptides compared to small molecules, enabling effective delivery of these versatile therapeutic agents
3Ease of operation
If implant size is reduced to improve patient comfort and tolerability, then patient acceptance is improved, but drug loading capacity decreases
Solution Approach 1:
The ocular implant uses composite material formulations combining multiple polymers, crosslinking agents, and therapeutic agents in optimized ratios, achieving high drug loading density within a compact volume while maintaining structural integrity and controlled release properties, thus providing sufficient drug capacity in a small, comfortable implant size
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 ocular composition and implants achieve controlled release of therapeutic agents, maintaining high bioavailability and efficacy over time, improving patient comfort and tolerability, while allowing for the administration of large molecules like proteins and peptides with reduced implant size and minimal ocular trauma.
Implementation Method 1
5 to 75% w/w of a photopolymerizable composition selected from the group consisting of fragments or monomers of polyalkylene glycol mono-acrylate, polyalkylene glycol diacrylate, polyalkylene glycol methacrylate, polyalkylene glycol dimethacrylate and mixtures, copolymers and block copolymers thereof
Implementation Method 2
0.1 to 40% w/w of a biodegradable polymer selected from the group consisting of lactide/glycolide copolymer (including poly(lactide-co-glycolide) (PLGA)), poly (L-lactide) (PLA), polyhydroxyalkanoates, including polyhydroxybutyrate, polyglycolic acid (PGA), polycaprolactone (PCL)
Data Source
AI summary
The present invention relates to ocular compositions for the controlled release of a therapeutic agent. The ocular composition comprises at least 20% w/w of a therapeutic agent; 5 to 75% w/w of a photopolymerizable composition selected from the group consisting of fragments or monomers of polyalkylene glycol mono-acrylate, polyalkylene glycol diacrylate, polyalkylene glycol methacrylate and polyalkylene glycol dimethacrylate, and mixtures, copolymers, and block copolymers thereof; 0.1 to 40% w/w of a biodegradable polymer selected from the group consisting of lactide/glycolide copolymer (including poly(lactide-co-glycolide) (PLGA)), poly (L-lactide) (PLA), polyhydroxyalkanoates, including polyhydroxybutyrate, polyglycolic acid (PGA), polycaprolactone (PCL), poly (DL-lactide) (PDL), poly (D-lactide), lactide/caprolactone copolymer, poly-L-lactide-co-caprolactone (PLC) and mixtures, copolymers, and block copolymers thereof; and a photoinitiator.