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Supramolecular core-shell compound, supramolecular drug-loaded core-shell compound, and preparation methods and applications of supramolecular core-shell compound and supramolecular drug-loaded core-shell compound

A supramolecular core and complex technology, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc. Water-soluble, strong penetrating power, high photothermal conversion efficiency

Inactive Publication Date: 2021-10-15
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the guest molecule G for constructing supramolecular vesicles has poor water solubility and low solubility in water. Therefore, organic solvents are needed in the process of preparing supramolecular vesicles, and the preparation process is a bit cumbersome.
Moreover, although supramolecular vesicles have explored the photothermal effect in the second near-infrared region, they still use high laser power density (3.0 W / cm 2 )

Method used

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  • Supramolecular core-shell compound, supramolecular drug-loaded core-shell compound, and preparation methods and applications of supramolecular core-shell compound and supramolecular drug-loaded core-shell compound
  • Supramolecular core-shell compound, supramolecular drug-loaded core-shell compound, and preparation methods and applications of supramolecular core-shell compound and supramolecular drug-loaded core-shell compound
  • Supramolecular core-shell compound, supramolecular drug-loaded core-shell compound, and preparation methods and applications of supramolecular core-shell compound and supramolecular drug-loaded core-shell compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Preparation of supramolecular core-shell complex

[0039] Dissolve 7.6mg of WP5 in 10mL of ultrapure water in a sample bottle, add buffer solution to adjust its pH to 6.8. Take 5.0 mg of TAPEG and directly add it to the above aqueous solution of WP5, sonicate for 10 minutes to make it fully mixed, add PBS buffer solution to finally adjust its pH to 7.4, and get Aqueous solutions of supramolecular core-shell complexes.

[0040] 1-1. Microstructure of supramolecular core-shell complexes

[0041] Photographed by transmission electron microscopy, as figure 1 shown, it can be seen The aggregates of TAPEG have a regular core-shell structure, and the aniline tetramer part of TAPEG enters the hydrophobic cavity microenvironment of WP5 to obtain a host-guest complex. The resulting complex has the characteristics of a bola-type surfactant because both ends are hydrophilic and the middle is hydrophobic. , the complex surfactant can form micelles under certain cond...

Embodiment 2

[0049] Example 2: Preparation of supramolecular drug-loaded core-shell complex

[0050] Get 10mL prepared in Example 1 For the aqueous solution of the supramolecular core-shell complex (pH=7.4), a certain amount of doxorubicin (DOX) was weighed according to the molar ratio of the anticancer drug and the supramolecular core-shell complex being 1:2, and added to the supramolecular core-shell The complex solution was stirred for one day to make it loaded into the core of the supramolecular core-shell complex. Use a dialysis bag with a molecular weight cut-off of 14,000 to dialyze the above-prepared supramolecular drug-loaded core-shell complex solution to remove the drug not wrapped in the complex, regularly replace the aqueous solution outside the dialysis bag, and detect its fluorescence intensity until dialysis No DOX can be detected in the solution outside the bag, that is, the supramolecular drug-loaded core-shell complex is obtained.

[0051] After the hydrophobic doxoru...

Embodiment 3

[0064] Example 3: Treatment of colon cancer mice by supramolecular drug-loaded core-shell complex

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Abstract

The invention discloses a supramolecular core-shell compound and a preparation method thereof, a supramolecular drug-loaded core-shell compound and a preparation method and application thereof. Water-soluble column [5] arene (WP5) is used as a subject, amphiphilic aniline tetramer (TAPEG) modified by a polyethylene glycol chain segment is used as a guest molecule, and through subject-guest recognition interaction between the subject and the guest, the supermolecule core-shell compound with the photo-thermal performance is formed through self-assembly. The core of the supramolecular core-shell compound is hydrophobic, the shell layer is hydrophilic, the biocompatibility is good, the hydrophobic core is loaded with an anti-cancer drug doxorubicin (DOX), under the slightly acidic condition of tumor cells, the structure is disintegrated, and the drug is released, so that the effect of chemotherapy treatment is achieved; the constructed supramolecular core-shell compound is relatively good in photo-thermal performance, realizes chemical-photo-thermal combined tumor treatment under the irradiation of low laser power density (1.0 W / cm < 2 >) of a near-infrared second region, and has a very good clinical application prospect.

Description

technical field [0001] The invention belongs to the technical field of nanomedicine, and in particular relates to supramolecular core-shell complexes, supramolecular drug-loaded core-shell complexes, their preparation methods and applications. Background technique [0002] In contemporary society, due to various exogenous and endogenous factors, malignant tumors are increasingly endangering human life and health. The treatment means for malignant tumors is still based on surgical treatment, radiation therapy, and chemical drug therapy, but traditional drug therapy also brings inevitable side effects to the human body due to poor drug targeting when treating malignant tumors. The supramolecular core-shell complex with pH stimulus responsiveness can pack anticancer drugs in its core and release them in the acidic microenvironment of tumors, thereby reducing the toxic and side effects of drugs. As a new treatment method in recent years, photothermal therapy uses laser to irrad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/18A61K47/12A61K41/00A61K31/704A61P35/00
CPCA61K9/127A61K47/18A61K47/12A61K41/0052A61K31/704A61P35/00A61K2300/00
Inventor 韩杰王自遥孙晓环郭荣
Owner YANGZHOU UNIV
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