Ocular Composition for Sustained Drug Delivery
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current methods for delivering therapeutic agents to the posterior segment of the eye, such as intravitreal injections, are invasive, cause tissue trauma, and require frequent administration, leading to discomfort, toxicity, and increased costs, while alternative non-invasive methods like iontophoresis have limitations in sustained release and patient compliance.
Innovation Solution
Development of ocular compositions comprising photopolymerizable compositions, biodegradable polymers, and therapeutic agents, which can be administered as implants or coatings to achieve controlled release of small and large molecules, including proteins and peptides, using a combination of polyalkylene glycol diacrylate, aliphatic polyester-based polyurethanes, and PLGA, with photopolymerization for in situ or pre-formed implants.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If intravitreal injections are used to deliver drugs to the posterior segment of the eye, then direct drug delivery to the target site is achieved, but tissue trauma, pain, and risk of infection increase
Solution Approach 1:
The delivery system is segmented into multiple components: a biodegradable polymer matrix for drug incorporation, a photopolymerizable gel former for in-situ implant formation, and a photoinitiator for controlled crosslinking. This segmentation allows separate optimization of drug loading, delivery control, and implant formation, reducing the need for invasive surgical implantation while maintaining reliable drug delivery to the posterior segment
Solution Approach 2:
The patent introduces an intermediary photopolymerizable gel system that can be injected in a liquid state and then transformed in-situ into a solid implant through light-triggered crosslinking. This intermediary state allows minimally invasive injection while achieving the structural integrity of a solid implant, reducing tissue trauma compared to direct surgical implantation of solid devices
2Reliability
If frequent intravitreal injections are administered to maintain therapeutic drug levels, then treatment efficacy is maintained, but patient discomfort and treatment costs increase
Solution Approach 1:
The patent incorporates the full therapeutic dose into the implant matrix during manufacturing, performing the drug loading action in advance. The implant is then injected once and releases the pre-loaded drug over an extended period (months), eliminating the need for frequent re-dosing and reducing patient burden while maintaining therapeutic levels
Solution Approach 2:
The biodegradable polymer matrix provides continuous drug release through sustained diffusion and erosion mechanisms, maintaining therapeutic drug levels continuously over months rather than requiring discrete repeated dosing events. This continuous action reduces patient discomfort and treatment frequency while ensuring reliable therapeutic coverage
3Reliability
If high concentrations of drug are administered to overcome ocular barriers, then drug delivery efficacy is improved, but drug-related toxicity increases
Solution Approach 1:
The patent replaces the mechanical/chemical approach of administering high systemic or topical doses with a targeted localized delivery system. The implant delivers drug directly to the posterior segment at controlled low concentrations, substituting the need for high-dose systemic administration and thereby reducing drug-related toxicity while maintaining delivery efficacy
Solution Approach 2:
The implant provides localized drug delivery with spatially controlled concentration gradients, releasing drug directly at the target site in the posterior segment. This local quality approach ensures high drug concentration where needed while avoiding systemic circulation of high doses, thereby reducing toxicity while maintaining delivery efficacy
4Object-affected harmful factors
If non-invasive delivery methods like iontophoresis are used, then tissue trauma is reduced, but sustained release capability and patient compliance remain limited
Solution Approach 1:
The patent changes the physical state parameter of the delivery system from liquid (injection) to solid gel (in-situ formed implant) through photopolymerization. This parameter change enables the system to remain minimally invasive during administration while achieving sustained release capabilities comparable to surgical implants, extending drug release from hours/days to months
Solution Approach 2:
The patent creates a composite material system combining biodegradable polymers for drug loading, photopolymerizable gel formers for structural integrity, and biodegradable crosslinkers for controlled network formation. This composite approach enables sustained release over months while maintaining minimally invasive injection-based administration, overcoming the limitations of both traditional iontophoresis and surgical implants
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 solution provides a flexible and biocompatible method for sustained drug delivery, reducing the frequency of administration, minimizing tissue trauma, and maintaining therapeutic levels for extended periods, thus improving patient compliance and reducing side effects.
Implementation Method 1
irradiating the mixture with light at a wavelength of between 230 to 550 nm, between 300 to 525 nm, or between 350 to 490 nm for between 1 second and 60 minutes to form the ocular composition
Implementation Method 2
Drug diffusion across the scleral membrane is dependent upon drug's solubility, molecular weight/molecular radius, charge and polarity
Implementation Method 3
a biodegradable polymer selected from the group consisting of aliphatic polyester-based polyurethanes, polylactides, polycaprolactones, polyorthoesters
Data Source
AI summary
The invention provides an ocular 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. The composition can be used to form an ocular implant and an in situ ocular implant.