Crosslinked Polyester Particles Sustained Drug Release
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Solution Overview
Problem
Current drug delivery particles face challenges in controlling particle size and morphology for reproducible results, limited drug loading capacity, rapid biodegradation, and a burst effect leading to inconsistent drug release profiles.
Innovation Solution
Development of crosslinked degradable particles with polyester backbones crosslinked via thioethers, allowing for controlled release of drugs through degradation, erosion, or diffusion, with specific methods involving functional groups, crosslinkers, and solvents to achieve uniform size and sustained drug release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If smaller particles are used to improve biodegradation rate, then drug release speed increases, but drug loading capacity decreases and sustained release duration is insufficient
Solution Approach 1:
The patent changes the chemical structure parameter of the particle matrix by incorporating hydrophobic segments and crosslinkable functional groups (allyl, propargyl, epoxide) into the polyester backbone. This structural modification enables the particles to maintain larger sizes with higher drug loading capacity while achieving controlled degradation rates through the hydrophobic effect and crosslinking density, resolving the contradiction between release speed and loading capacity.
Solution Approach 2:
The patent creates composite particle structures by combining polyester backbones with crosslinking agents (dithiols, diamines, etc.) to form crosslinked networks. This composite approach allows the particles to achieve both high drug loading capacity (through larger size) and controlled release rates (through crosslinking density and hydrophobic segments), simultaneously satisfying both requirements.
2Duration of action of stationary object
If crosslinked particles are used to extend drug release duration, then sustained release is achieved, but particle size and morphology control becomes difficult
Solution Approach 1:
The patent incorporates crosslinkable functional groups (allyl, propargyl, epoxide) and crosslinking agents into the particle formulation before final particle formation. The crosslinking reaction is then triggered under controlled conditions (UV irradiation, thermal treatment, or chemical reaction) after particles are formed, allowing precise control of particle size and morphology during formation while subsequently achieving extended drug release through the crosslinked network structure.
3Reliability
If drug is dispersed in particles for delivery, then therapeutic effect is achieved, but burst effect occurs causing inconsistent drug release
Solution Approach 1:
The patent creates local heterogeneity in the particle structure by incorporating hydrophobic segments and crosslinkable functional groups at specific locations within the polyester backbone. This local quality variation creates regions with different drug affinity and degradation rates, preventing the burst effect by ensuring uniform drug distribution and controlled release throughout the particle matrix, thereby achieving consistent therapeutic delivery.
4Quantity of substance
If larger particles are used to increase drug loading capacity, then more drug can be loaded, but biodegradation rate decreases leading to insufficient release duration
Solution Approach 1:
The patent modifies the chemical composition parameters of the particle matrix by incorporating hydrophobic segments and crosslinkable functional groups into the polyester backbone. This structural change enables larger particles to maintain appropriate degradation rates through the hydrophobic effect (which slows water penetration) and controlled crosslinking density, allowing simultaneous achievement of high drug loading capacity and sufficient release duration.
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 crosslinked particles provide reproducible, sustained drug release over an extended period (up to several months) without a burst effect, ensuring consistent therapeutic delivery and improved biocompatibility.
Implementation Method 1
reacting the functional groups with crosslinkers to form a crosslinked degradable particle
Implementation Method 2
The particles can release drug by degradation, erosion, diffusion, or a combination of mechanisms
Data Source
Figure 1A
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AI summary
Disclosed are crosslinked particles (e.g., microparticles) that are capable of storing and releasing drugs. The particles can be macroparticles, microparticles, or nanoparticles and can be composed of polyester backbones. The particles can be loaded with a drug. The particles can degrade in vivo to release the drug. The particles can be prepared by crosslinking functionalized polyester backbones and loaded with a given drug. The particles of the present disclosure can be injected with a syringe. In some embodiments, the particles of the present disclosure are administered in connection with a surgery and release the drug after the site of the surgery for a period of 1-6 months.