Biodegradable Microsphere Formulation for Ischemic Tissue Repair
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Solution Overview
Problem
Current regeneration therapies for ischemic organ diseases, such as arteriosclerosis obliterans and myocardial infarction, face challenges including limited effectiveness, ethical concerns, safety issues, and the need for frequent administration of systemic medications with side effects, particularly in promoting angiogenesis and tissue repair.
Innovation Solution
Development of a pharmaceutical composition comprising a PGI2 agonist, EP2 agonist, or EP4 agonist, which acts as an endogenous repair factor production accelerator, inducing vascular endothelial growth factor and other growth factors to promote angiogenesis and tissue repair, formulated as a persistent release preparation using biodegradable polymers like microspheres or nanospheres for topical administration to ischemic regions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If systemic medications are administered to promote angiogenesis and tissue repair, then therapeutic effectiveness is improved, but side effects increase and administration compliance deteriorates
Solution Approach 1:
The patent segments the medication delivery system into localized microspheres or nanospheres that are administered directly to the ischemic region, rather than systemic administration. This localization segments the therapeutic effect to the target area, reducing exposure of healthy tissues to the medication and thereby reducing side effects while maintaining therapeutic effectiveness in the ischemic region.
Solution Approach 2:
The patent applies local quality by formulating the medication as persistent release preparations (microspheres, nanospheres) that are administered locally to the ischemic region. This creates high concentration of the active ingredient at the target site with gradual release, improving therapeutic effectiveness locally while minimizing systemic side effects.
2Reliability
If systemic medications are administered to promote angiogenesis and tissue repair, then therapeutic effectiveness is improved, but administration compliance deteriorates due to frequent dosing
Solution Approach 1:
The patent employs persistent release preparations (microspheres, nanospheres) that are prepared in advance with embedded active ingredients. These preparations are designed to release the medication gradually over an extended period, so a single administration provides sustained therapeutic effect, eliminating the need for frequent dosing and thereby improving administration compliance while maintaining therapeutic effectiveness.
Solution Approach 2:
The patent achieves continuity of useful action through persistent release formulations that maintain therapeutic drug levels in the ischemic region over an extended period. The microspheres or nanospheres continuously release the active ingredient, ensuring sustained angiogenesis promotion and tissue repair without requiring repeated administrations, thus improving compliance.
3Productivity
If growth factors are released to accelerate angiogenesis, then formation of collateral circulation passage is accelerated, but production cost increases
Solution Approach 1:
The patent extracts and utilizes endogenous repair factors (growth factors like VEGF, HGF, FGF) that are already present in the body, rather than administering large quantities of exogenous growth factors. The agonists stimulate the body's own cells to produce and release these endogenous factors, thereby achieving angiogenesis acceleration while reducing the quantity of external substances needed, thus lowering production costs.
Solution Approach 2:
The patent employs a self-service mechanism where the administered agonists trigger the body's own cells (endothelial cells, smooth muscle cells, fibroblasts) to produce and release endogenous repair factors. This self-service approach leverages the body's natural repair mechanisms, reducing the need for expensive external growth factor administration while maintaining effective angiogenesis acceleration.
Data Source
AI summary
It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) 12 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.