Bioorthogonal Payload Compositions for Site-Selective Drug Release
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Solution Overview
Problem
Existing biomaterials for drug delivery exhibit an initial burst of activity after implantation and lack modularity, limiting their application in medical conditions requiring specific dosing regimens or delayed therapeutic agent identification.
Innovation Solution
Bioorthogonal compositions with functionalized payloads and linkers, allowing for selective and controlled delivery of therapeutic agents to specific sites using bioorthogonal conjugation reactions, enhancing aqueous solubility and enabling targeted release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If systemic medications are used for treatment, then therapeutic agents can be delivered to the body, but frequent dosing is required and noxious side effects occur
Solution Approach 1:
The patent segments the therapeutic agent delivery by using a biomaterial depot that releases the agent locally at the implantation site, rather than systemic administration. This localized delivery segmentates the treatment from systemic circulation, reducing side effects while maintaining treatment effectiveness at the target site.
Solution Approach 2:
The biomaterial acts as an intermediary carrier that holds and releases the therapeutic agent at the implantation site. This intermediary depot system allows controlled local release, avoiding the need for frequent systemic dosing and reducing exposure of non-target tissues to the therapeutic agent, thereby reducing side effects.
2Duration of action of moving object
If existing biomaterials are used as depots for therapeutic agents, then agents can be released through diffusion or degradation, but the materials cannot be modulated or modified after implantation and exhibit an initial burst of activity
Solution Approach 1:
The patent introduces dynamic functionality to the biomaterial depot by incorporating bioorthogonal functional groups that allow post-implantation modification. The depot can be dynamically adjusted after implantation through bioorthogonal conjugation reactions, enabling modulation of the therapeutic agent release profile without requiring removal or replacement of the implant.
Solution Approach 2:
The biomaterial is pre-functionalized with bioorthogonal groups before implantation, preparing it for future modification. This preliminary functionalization enables subsequent controlled modification and tuning of the depot's release characteristics after implantation, allowing adaptation to specific dosing requirements.
3Ease of manufacture
If biomaterials are implanted for therapeutic delivery, then agents can be delivered to the body, but doses cannot be administered at different time points or adjusted after implantation
Solution Approach 1:
The patent creates a dynamic dosing system where the implanted biomaterial depot can be modified after implantation to administer doses at different time points. The bioorthogonal functionality allows the depot to be tuned to release therapeutic agents according to specific dosing regimens, providing flexibility in timing and amount of drug delivery while maintaining the simplicity of the initial implantation procedure.
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 bioorthogonal compositions provide controlled and targeted delivery of therapeutic agents, reducing side effects and enabling precise dosing regimens, improving treatment efficacy for conditions like cancer and infections.
Implementation Method 1
Bioorthogonal conjugation or click reactions are selective and orthogonal (non-interacting with) functionalities found in biological systems, and have found use in various applications in the fields of chemistry, chemical biology, molecular diagnostics, and medicine
Implementation Method 2
Bioorthogonal conjugation or click reactions are selective and orthogonal (non-interacting with) functionalities found in biological systems
Implementation Method 3
The functionalized payload comprises a complementary binding agent that selectively binds to the binding agent on the support composition
Implementation Method 4
Existing biomaterials can serve as depots for therapeutic agents, which can be released to the body through diffusion or degradation
Implementation Method 5
Existing biomaterials can serve as depots for therapeutic agents, which can be released to the body through diffusion or degradation
Data Source
AI summary
Cyclooctene conjugates of therapeutic or diagnostic agents have improved aqueous solubility and can release the agents upon contact with a tetrazine-containing biomaterial. The cyclooctene conjugates provide site-selective delivery of agents at the location of the tetrazine-containing biomaterial in a subject. The compositions and methods have applications in the treatment of various diseases or conditions including cancer, tumor growths, and bacterial infections.