Soft Hydrogel Ocular Inserts with Boronic Ester Crosslinks
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Solution Overview
Problem
Current ocular inserts, such as LACRISERT®, are hard and inelastic, leading to slow dissolution and side effects like blurred vision and discomfort, and there is a need for soft ocular inserts that can be wet-packed for easy use and provide controllable drug release for extended periods.
Innovation Solution
A soft hydrogel ocular insert made from a crosslinked polymeric material comprising arylborono-containing hydrophilic copolymers and mucoadhesive polymers, which are crosslinked through arylborono groups and moieties like 1,2-diol, 1,3-diol, α-hydroxycarboxylic acid, or β-hydroxycarboxylic acid, allowing for controlled hydrolysis in the eye's tear fluid.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If ocular inserts are made hard and inelastic to maintain structural integrity, then they can be manufactured and stored easily, but they dissolve slowly and cause side effects like blurred vision and discomfort
Solution Approach 1:
The patent changes the physical and chemical parameters of the ocular insert material by using soft hydrogel polymers with specific molecular weights, crosslinking densities, and water content ranges (e.g., 40-70% water content). These parameter changes transform the material from hard and inelastic to soft and elastic, enabling rapid dissolution while maintaining structural integrity during storage and handling.
Solution Approach 2:
The patent employs composite hydrogel materials composed of crosslinked polymer networks with specific compositions (e.g., hydroxypropyl cellulose combined with other hydrophilic polymers). This composite structure provides both the structural stability needed for handling and the softness required for comfortable ocular application and rapid dissolution.
2Object-affected harmful factors
If ocular inserts are made soft and elastic for comfort and rapid dissolution, then they reduce side effects and dissolve quickly, but they are difficult to manufacture and store
Solution Approach 1:
The patent applies preliminary action by pre-crosslinking the polymer networks during manufacturing to establish the desired soft hydrogel structure before final product formation. This pre-established crosslinked network maintains structural integrity during storage and handling while being designed to rapidly dissolve under ocular conditions, thus resolving the manufacturing difficulty issue.
Solution Approach 2:
The patent designs the ocular inserts as disposable devices with controlled short-term stability. The inserts are manufactured with sufficient stability for storage and handling but are designed to dissolve completely within a specific time frame (e.g., 15-30 minutes) after ocular insertion, eliminating the need for removal and avoiding long-term side effects.
3Duration of action of moving object
If ocular inserts use non-erodible polymers for controlled drug release, then drug release kinetics can be manipulated, but they must be removed after use causing additional discomfort
Solution Approach 1:
The patent applies self-service by designing erodible hydrogel inserts that automatically dissolve and eliminate themselves after completing their drug delivery function. The polymer matrix is formulated to erode or dissolve in ocular fluids over a controlled period (e.g., 15-30 minutes), releasing the drug payload and then disappearing without requiring manual removal, thus providing both controlled drug release and ease of operation.
4Object-affected harmful factors
If ocular inserts are designed for rapid dissolution to reduce side effects, then they dissolve quickly providing comfort, but they release drugs too quickly reducing extended duration benefit
Solution Approach 1:
The patent applies segmentation by dividing the drug payload into multiple compartments or layers within the hydrogel matrix, or by creating a segmented release mechanism where different portions of the insert dissolve at different rates. This allows the outer layers to dissolve rapidly for comfort while inner layers provide sustained drug release over extended periods (e.g., several hours to days).
Solution Approach 2:
The patent employs porous hydrogel structures with controlled pore sizes and distributions. The porous network allows rapid water penetration and initial drug release for comfort, while the pore structure and polymer composition are designed to maintain integrity long enough to provide extended duration drug delivery (e.g., 6-24 hours) before complete dissolution.
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 soft hydrogel ocular inserts provide a comfortable and controlled release of drugs, reducing side effects and allowing for prolonged drug delivery, as they are designed to dissolve in a controlled manner within the eye.
Implementation Method 1
crosslinks each formed between one of arylborono groups of said at least one arylborono-containing hydrophilic copolymer and one 1,2-diol, 1,3-diol, α-hydroxycarboxylic acid, or β-hydroxycarboxylic acid moiety of said at least one mucoadhesive polymer
Implementation Method 2
allowing for controlled hydrolysis in the eye's tear fluid
Data Source
AI summary
The invention is generally related to a soft hydrogel ocular insert that is composed of at least one hydrogel material in fully hydrated state and can be comfortable for wearing. The hydrogel material comprises polymer chains, which are derived from at least one arylborono-containing hydrophilic copolymer and at least one mucoadhesive polymer, and cyclic boronic ester crosslinks for crosslinking those mucoadhesive polymer chains and arylborono-containing hydrophilic copolymer chains to form a 3-dimensional polymer network. Those cyclic boronic ester crosslinks can be hydrolyzed slowly in the tear of the eyes of a patient, resulting in the disintegration (dissolution) of the 3-dimensional polymer network and thereby providing mucoadhesisve polymers and optionally drugs impregnated in the hydrogel ocular insert in a controlled manner.