FAPIN Nanoparticles for High-Loading Drug Delivery
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Solution Overview
Problem
Current organic nanodrug delivery systems (NDDS) face limitations in drug loading capacity, leading to high amounts of non-pharmaceutical ingredients, potential toxicity, and lack of traceability, while conventional systems require additional imaging agents for biological disposition visualization.
Innovation Solution
Development of self-indicating full active pharmaceutical ingredients nanoparticles (FAPIN) with 100% API loading capacity, utilizing pheophorbide A and irinotecan conjugates for dual-fluorogenic and near-infrared fluorescence imaging, enabling controllable trimodality therapy and real-time drug release monitoring.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional organic nanodrug delivery systems are used to deliver APIs, then the solubility of APIs is improved and they are protected from degradation, but the drug loading capacity is low (below 20 wt %) leading to high amounts of non-pharmaceutical ingredients
Solution Approach 1:
The patent merges the drug molecule with the carrier structure by conjugating API to peptide-based nanocarriers, creating a unified theranostic agent that eliminates the need for separate drug and carrier components, thereby achieving 100% drug loading capacity
Solution Approach 2:
The patent creates composite theranostic agents by conjugating multiple functional components (API, imaging agent, therapeutic moiety) onto a single peptide nanocarrier platform, forming a multifunctional composite material that simultaneously delivers drug and provides imaging capabilities
2Quantity of substance
If the quantity of non-pharmaceutical ingredients is increased to elevate API amounts for better efficacy, then the therapeutic effect is improved, but the toxicity increases as the quantities surpass the safety threshold
Solution Approach 1:
The peptide nanocarrier is designed to be self-degradable through enzymatic cleavage by proteases in the tumor microenvironment, automatically breaking down into non-toxic amino acids after delivering the API, thereby eliminating the need for external clearance mechanisms and reducing cumulative toxicity
Solution Approach 2:
The patent changes the chemical structure of the carrier from conventional non-degradable polymers to enzymatically cleavable peptide bonds, fundamentally altering the degradation parameter from 'stable' to 'biodegradable' and thereby reducing toxicity while maintaining high API loading
3Loss of information
If conventional NDDS require additional imaging agents to indicate biological dispositions, then the traceability is improved, but the device complexity increases and the imaging agents may leak out giving false information
Solution Approach 1:
The patent combines the imaging function with the therapeutic carrier by conjugating fluorescent or MRI-active moieties directly to the peptide nanocarrier, creating a unified theranostic agent that simultaneously provides both therapy and real-time imaging without separate imaging components
Solution Approach 2:
The integrated imaging agent in the peptide nanocarrier provides real-time feedback on the location and distribution of the theranostic agent in vivo, enabling monitoring of drug delivery and accumulation at the target site, thereby optimizing treatment efficacy and reducing off-target toxicity
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
Achieves high drug loading efficiency, reduced toxicity, and real-time biological disposition visualization, enhancing therapeutic efficacy through precise and spatiotemporal cancer treatment with minimal side effects.
Implementation Method 1
utilizing pheophorbide A and irinotecan conjugates for dual-fluorogenic and near-infrared fluorescence imaging
Implementation Method 2
PTT is realized by transforming photo energy to heat
Implementation Method 3
PDT refers to produce the reactive oxygen species (ROS) in the circumstance
Implementation Method 4
The amphiphilic conjugates self-assemble to form nanoparticles, which aggregate to form nanocarriers
Data Source
AI summary
The present inventions provides drug-drug conjugates, drug-porphyrin conjugates, nanoparticles of the conjugates, as well as modified nanoparticles having PEGylated exteriors or encapsulated by red blood cell vesicles. The conjugates, nanoparticles and nanocarriers are useful for treating cancers and other diseases, as well as for imaging diseased tissue or organs.