Photopolymerizable Ocular Implants for Sustained Drug Release
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Solution Overview
Problem
Current ocular drug delivery methods, such as topical eye drops, suffer from poor bioavailability and high side effects due to low drug penetration, leading to suboptimal medical management of eye diseases like glaucoma and AMD, with less than 5% drug penetration and excessive waste of costly medications.
Innovation Solution
Development of nanoparticle or microparticle ocular implants made from a photopolymerizable composition of polyalkylene glycol diacrylate or dimethacrylate, combined with biodegradable polymers like PLGA and a photoinitiator, which are crosslinked using UV light to achieve controlled and sustained release of therapeutic agents for extended periods.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If topical eye drops are administered to achieve therapeutic effect, then drug delivery to the eye is attempted, but drug penetration is less than 5% leading to poor bioavailability
Solution Approach 1:
The invention segments the drug delivery system into multiple components: a biodegradable polymer matrix for sustained release, ocular mucin for extended retention on the eye surface, and penetrants to enhance drug penetration through ocular barriers. This segmentation allows each component to address specific limitations of conventional eye drops, collectively improving overall drug penetration and bioavailability.
Solution Approach 2:
The invention employs a composite formulation consisting of the therapeutic agent combined with biodegradable polymer, ocular mucin, and penetrants. This composite material approach enables the system to simultaneously provide sustained release kinetics, extended ocular retention, and enhanced penetration through multiple barriers, achieving greater than 5% drug penetration as stated in the patent.
2Reliability
If high drug doses are administered to compensate for poor penetration, then therapeutic effect may be achieved, but long-term side effects such as allergy and intolerance occur
Solution Approach 1:
The biodegradable polymer matrix performs preliminary action by pre-encapsulating the therapeutic agent and controlling its release kinetics. This sustained release mechanism ensures that the drug is delivered gradually over time rather than all at once, maintaining therapeutic levels while avoiding the peaks that cause side effects like allergy and intolerance.
Solution Approach 2:
The combination of sustained release from the polymer matrix and extended retention on the eye surface due to ocular mucin creates continuous useful action. The drug is released continuously over time and remains on the ocular surface longer, ensuring consistent therapeutic exposure without the need for repeated high-dose administrations that lead to side effects.
3Reliability
If topical eye drops are applied frequently to maintain therapeutic levels, then drug exposure is increased, but patient compliance deteriorates
Solution Approach 1:
The invention introduces dynamics into the drug delivery system through the biodegradable polymer matrix that gradually degrades over time, automatically adjusting the release rate. As the polymer degrades, it sustains drug release without requiring patient intervention, transforming a static dosing regimen into a dynamic, self-regulating system that maintains therapeutic levels while reducing administration frequency.
Solution Approach 2:
The sustained release system performs self-service by automatically maintaining therapeutic drug levels over an extended period without requiring frequent patient administration. The polymer matrix self-regulates the release kinetics, and the ocular mucin self-extends the retention time, collectively reducing the burden on patients and improving compliance.
4Ease of operation
If conventional eye drops are used, then administration is simple, but less than 5% of the drug penetrates the eye resulting in excessive waste of costly medications
Solution Approach 1:
The biodegradable polymer matrix acts as a flexible shell that encapsulates the therapeutic agent and controls its release. This shell structure protects the drug during administration and enables sustained release kinetics, ensuring that a higher proportion of the administered drug actually penetrates the eye rather than being wasted, while still maintaining ease of administration.
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 method provides controlled release of therapeutic agents for 24 hours to 3 months, improving bioavailability and reducing side effects, while allowing flexibility in administering small and large molecules, including proteins and peptides, effectively treating a range of eye conditions.
Implementation Method 1
irradiating the mixture ii) with light at a wavelength of between 230 to 550 nm, between 300 to 525 nm, or between 350 to 490 nm
Data Source
Figure 2~3
Figure 4
Figure 5~6C
AI summary
The invention provides methods of making microparticle and nanoparticle ocular implants from a composition comprising: 99 to 60 % (w/w) of a photopolymerizable composition selected from the group of fragments or monomers consisting of polyalkylene glycol diacrylate and polyalkylene glycol dimethacrylate, wherein the photopolymerizable composition has a molecular weight in the range of 100 to 20,000 Dalton; a biodegradable polymer selected from the group consisting of aliphatic polyester-based polyurethanes, polylactides, polycaprolactones, polyorthoesters and mixtures, copolymers, and block copolymers thereof; a photoinitiator; and a therapeutic agent.