Surface-Treated Microparticle Aggregation for Sustained Ocular Drug Delivery
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Solution Overview
Problem
Current methods for delivering therapeutic agents to the posterior segment of the eye face challenges such as short-term complications, rapid particle dispersal, immunogenicity, and systemic toxicity, making it difficult to achieve sustained therapeutic levels for effective treatment of ocular diseases.
Innovation Solution
Mildly surface-treated solid biodegradable microparticles that aggregate in vivo to form larger pellets, reducing unwanted side effects and enabling long-term sustained drug delivery, suitable for ocular injection without significantly impairing vision.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If small microparticles are injected into the eye, then high drug concentration can be achieved in the vitreous chamber and retina, but the particles rapidly disperse and are quickly removed from the injection site, causing vision obstruction and immunogenicity
Solution Approach 1:
The patent combines multiple small microparticles into a single aggregated pellet structure in situ within the eye. This merging approach maintains the advantages of small particle injection (high drug concentration, minimal vision obstruction) while achieving long-term retention by forming a larger consolidated structure that resists rapid dispersal and phagocytosis
2Quantity of substance
If small microparticles are injected into the eye, then drug delivery to the posterior segment is achieved, but complications such as retinal detachment, endophthalmitis, and intravitreal hemorrhages occur
Solution Approach 1:
By forming an aggregated pellet from multiple microparticles after injection, the system reduces the number of discrete particle-macaque interactions that could trigger immune responses or mechanical complications. The consolidated structure minimizes individual particle-related adverse events while maintaining therapeutic efficacy
Solution Approach 2:
The aggregated pellet acts as an intermediary structure between the injected microparticles and the ocular environment. This intermediate form factor reduces direct interaction between individual particles and sensitive ocular tissues, thereby minimizing complications while still delivering the therapeutic agent effectively
3Quantity of substance
If microparticles are injected into the eye, then therapeutic agent delivery is achieved, but immunogenicity occurs upon recognition of the microspheres by macrophages and immune system cells
Solution Approach 1:
The aggregation of multiple microparticles into a single pellet reduces the total surface area and number of recognition sites exposed to the immune system. This merging strategy decreases the likelihood of macrophage recognition and subsequent immune response while maintaining the therapeutic payload delivery capability
4Duration of action of moving object
If non-biodegradable particles are used for long-term drug delivery, then sustained therapeutic levels can be maintained, but surgical removal is required to avoid long-term complications
Solution Approach 1:
The patent changes the material parameter of the particles from non-biodegradable to biodegradable composition. This parameter change allows the particles to maintain structural integrity for sustained drug delivery while automatically degrading over time through physiological processes, eliminating the need for surgical removal and associated complications
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 aggregated microparticles provide sustained drug delivery for up to several months, minimizing vision disruption and inflammation, and are biodegradable, avoiding the need for surgical removal.
Implementation Method 1
surface treated solid (e.g., non-porous) microparticle that aggregates in vivo to form a consolidated larger particle
Data Source
AI summary
The present invention is a surface treated drug-loaded solid (e.g., non-porous) microparticle that aggregates in vivo to form a consolidated larger particle for medical therapy. In one embodiment, the particles are used for ocular therapy. Processes for producing the surface treated microparticle and injectable formulations which include the surface treated microparticle are also provided. When used in the eye, long-term consistent intraocular delivery can be achieved without disrupting vision and minimizing undesirable inflammatory responses.