Photoresponsive Nanocarriers for Green-Light Ocular Drug Release
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Solution Overview
Problem
Conventional photoresponsive drug delivery systems face challenges such as complex synthesis, slow drug release, poor light penetration, and phototoxicity, limiting their translational applications, especially for ocular drug delivery.
Innovation Solution
Development of small clathrin-like molecules that self-assemble into nanoparticles, utilizing dicyano group-modified coumarin responsive to green light for rapid drug release, which can penetrate deeper into tissues with reduced phototoxicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If conventional photoresponsive systems use UV light-absorbing coumarin, then phototriggered drug release can be achieved, but light penetration depth is poor and phototoxicity occurs
Solution Approach 1:
The patent changes the absorption wavelength parameter of the coumarin photocleavable group from UV range (300-400 nm) to green light range (500-560 nm). This parameter change enables deeper tissue penetration and reduces phototoxicity, as green light is less harmful to normal tissues such as retina compared to UV or blue light.
Solution Approach 2:
The patent substitutes UV light irradiation with green light irradiation to trigger the photocleavage reaction. This substitution replaces a harmful physical stimulus (UV light) with a safer one (green light) while maintaining the photoresponsive functionality of the coumarin group.
2Productivity
If polymeric photoresponsive nanocarriers are used, then drug delivery can be achieved, but the construction is complicated and drug release is slow
Solution Approach 1:
The patent segments the polymeric structure into small molecular building blocks (clathrin-like three-legged molecules). These small molecules self-assemble into nanoparticles, simplifying the construction process to a single step while enabling rapid drug release when the photocleavable groups are cleaved, as the assembly dissociation is much faster than polymeric skeleton degradation.
Solution Approach 2:
The patent uses small molecular nanocarriers that are designed to be transient and rapidly degrade upon light triggering. These small molecules serve as disposable carriers that dissolve quickly after delivering their cargo, unlike stable polymeric systems that require complex degradation pathways.
3Ease of operation
If intravitreal administration is used for ocular drug delivery, then UV light degradable polymer can achieve drug release, but the administration route is invasive
Solution Approach 1:
The patent uses intravenous injection as an intermediary route to deliver the nanocarriers systemically to the eye. The nanocarriers accumulate in the eye tissues naturally, and then green light irradiation triggers localized drug release. This intermediary approach avoids direct intravitreal injection while maintaining reliable drug delivery to the target site.
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 system enables rapid, spatiotemporally controlled drug release, effectively delivering drugs to the posterior segment of the eye for treatments like retinoblastoma with reduced side effects and improved penetration.
Implementation Method 1
the release of encapsulated cargos upon light triggering can be rapid, since the assembly of small molecules can be readily dissociated upon the photocleavage of the molecules
Implementation Method 2
we designed small clathrin-like (three-legged) molecules that can self-assemble into nanoparticles
Data Source
AI summary
Disclosed herein is a controlled drug release system of photoresponsive nanocarriers. Also provided are methods of making the nanocarriers. Also provided are method of using the nanocarriers for the treatment of diseases.