Supramolecular Cell-Based Carrier Host-Guest Targeting
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Solution Overview
Problem
Traditional drug formulations face challenges such as quick clearance by the mononuclear phagocytic system, weak penetration through physiological barriers, and low targeting delivery efficiency, limiting their therapeutic efficacy for inflammation-related diseases like cancer and neurological disorders.
Innovation Solution
A supramolecular cell-based carrier system utilizing host-guest interactions between macrocyclic host molecules and guest molecules embedded in cell membranes, allowing for targeted drug delivery without cytotoxicity and specific receptor limitations, using cells like macrophages or stem cells with liposomes for enhanced permeability and targeting.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional drug formulations are used, then the formulation is simple to prepare, but the drug is quickly cleared by the mononuclear phagocytic system during blood circulation
Solution Approach 1:
The patent changes the physical and chemical parameters of the drug formulation by using supramolecular assemblies with specific host-guest interactions. The macrocyclic host molecules (e.g., cyclodextrins, cucurbiturils) and guest molecules form stable complexes that alter the formulation's properties, enabling evasion of the mononuclear phagocytic system while maintaining relatively simple preparation procedures.
Solution Approach 2:
The patent employs composite supramolecular formulations consisting of host molecules, guest molecules, and drug substances. These composite structures combine the advantages of different components to achieve prolonged circulation stability while avoiding rapid clearance by the mononuclear phagocytic system.
2Reliability
If traditional synthetic targeting formulations are used, then the formulation can be designed for targeting, but the penetration ability through physiological barriers is weak
Solution Approach 1:
The patent utilizes supramolecular assemblies with tunable size, shape, and surface properties to optimize penetration through physiological barriers. The host-guest interaction systems allow for precise control of formulation parameters such as hydrodynamic radius and surface charge, enhancing barrier penetration while maintaining design flexibility.
Solution Approach 2:
The supramolecular formulations exhibit porous or cavity-containing structures that facilitate penetration through physiological barriers. The host molecules with cavities (e.g., cyclodextrins, cucurbiturils) create channels or spaces that enable the formulation to navigate through tight barrier structures more effectively.
3Reliability
If traditional formulations are used, then the preparation process is simple, but the targeting delivery efficiency to lesion tissue is low
Solution Approach 1:
The patent employs supramolecular assemblies with adjustable parameters including size, surface chemistry, and stability constants of host-guest complexes. These parameter optimizations enable enhanced targeting delivery efficiency to lesion tissues while maintaining relatively streamlined preparation processes compared to conventional complex formulations.
Solution Approach 2:
The host-guest interaction systems serve as intermediary mechanisms that facilitate targeted delivery. The specific binding between host and guest molecules acts as a mediator to guide the formulation to lesion tissues, improving targeting efficiency without requiring overly complex formulation designs.
4Object-affected harmful factors
If direct drug internalization is used to load drug carriers, then the loading process is simple, but the phagocytized drug carriers are degraded in the intracellular environment causing cytotoxicity
Solution Approach 1:
The patent introduces supramolecular host-guest complexes as intermediary structures between the drug and the delivery system. These complexes protect the drug from degradation in the intracellular environment, preventing cytotoxicity while maintaining relatively simple loading procedures through non-covalent interactions.
Solution Approach 2:
The patent modifies the chemical parameters of the drug delivery system by using stable supramolecular assemblies with high dissociation constants. These parameter changes protect the drug from intracellular degradation, reducing cytotoxicity while keeping the loading process straightforward through self-assembly mechanisms.
5Object-affected harmful factors
If covalent bond or ligand-receptor binding is used to conjugate drug carriers on cell surface, then the conjugation is stable, but it involves complex and multi-step chemical reactions causing cell damage
Solution Approach 1:
The patent replaces complex covalent bonding chemistry with supramolecular host-guest interactions. This substitution eliminates the need for multi-step chemical reactions and harsh conditions that cause cell damage, while maintaining stable conjugation through strong non-covalent binding. The preparation becomes simpler and more cell-friendly.
Solution Approach 2:
The host-guest interaction system serves as an intermediary that simplifies the conjugation process. Instead of direct covalent bonding or ligand-receptor binding, the supramolecular complexes act as mediators that facilitate stable attachment to cell surfaces through benign non-covalent interactions, reducing cell damage and process complexity.
6Adaptability or versatility
If ligand-receptor interaction is used for targeting, then the targeting is specific, but it is limited to specific cells expressing relevant receptors
Solution Approach 1:
The patent employs supramolecular host-guest interactions that can be applied universally across different cell types. The host molecules (e.g., cyclodextrins, cucurbiturils) and guest molecules provide a universal binding platform that is not restricted to specific receptor expressions, thereby expanding cell type applicability while maintaining targeting specificity through appropriate host-guest pair selection.
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 supramolecular cell-based carrier system achieves high biocompatibility, physiological barrier permeability, and targeting efficiency, enabling effective delivery of drugs like anti-inflammatory agents and cancer therapies with minimal cytotoxicity and complex chemical reactions.
Implementation Method 1
A supramolecular cell-based carrier includes a first part and a second part connected to each other through host-guest interaction
Implementation Method 2
The membrane-embedded material is similar to the structural components of cell membrane, and is self-assembled with the phospholipid layer on the membrane surface through hydrophobic forces
Data Source
AI summary
Disclosed is a method for preparing supramolecular cell-based carrier, which relates to the technical fields of supramolecular chemistry, supramolecular materials and cell preparations. Host-guest interactions mediated supramolecular cell-based carriers can achieve targeted delivery based on cell physiological functions, and have high biocompatibility, physiological barrier permeability, and targeting delivery efficiency. It does not require covalent bond modification on the cell surface, and has no effect on the physiological functions of transporting cells. The preparation method of supramolecular cell-based carrier provided by the present application has the advantages of simple and fast construction process, mild conditions and universal applicability, and the method has bio-orthogonality. In addition, a drug loading system is also provided, which can realize drug loading for targeted therapy.