Dual-targeting co-drug-loading micelle and preparation method thereof

By preparing FA-PEG5K-SS-DTX/CUR dual-targeted co-drug-loading micelles, the procedural release of curcumin and docetaxel was achieved, and the problem of poor water solubility and indiscriminate release in the combined application of docetaxel and curcumin was solved, the targeting and efficacy of tumor cells were improved, and drug resistance was reversed.

CN120242055APending Publication Date: 2025-07-04UNIV OF JINAN
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Patent Information

Application Number
CN202510406409.1
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-04-02
Publication Date
2025-07-04

AI Technical Summary

Technical Problem

In the prior art, docetaxel and curcumin are combined in anti-tumor research and have poor water solubility, low bioavailability and undifferentiated simultaneous drug release patterns, making it difficult to effectively reverse drug resistance.

Method used

Folic acid modified polyethylene glycol is used as a carrier, and docetaxel is coupled through disulfide bonds to form an FA-PEG5K-SS-DTX amphiphilic block polymer with reduction sensitivity and active targeting, and is prepared into a FA-PEG5K-SS-DTX/CUR dual-targeted co-drug-loading micelle to achieve programmed release of the drug, first releasing curcumin to inhibit P-gp, and then docetaxel is released.

Benefits of technology

The targeting and drug release targeting of tumor cells was improved. Curcumin first inhibited P-gp, and docetaxel subsequently acted on tumor cells, reversed drug resistance and enhanced drug efficacy.

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Abstract

The invention discloses a dual-targeting co-drug-loading micelle and a preparation method thereof. Folic acid modified polyethylene glycol (PEG5K) is used as a carrier, and is coupled with docetaxel (DTX) through a disulfide bond to construct an FA-PEG5K-SS-DTX amphiphilic block polymer with reduction sensitivity and active targeting, and the FA-PEG5K-SS-DTX / CUR dual-targeting co-loading micelle is further prepared by taking the FA-PEG5K-SS-DTX / CUR dual-targeting co-loading micelle as the carrier and physically entrapping curcumin (CUR). The micelle disclosed by the invention integrates targeted delivery, programmed drug release and synergistic drug delivery, can fully play the chemosensitization effect of curcumin, enhances the activity of docetaxel on drug-resistant tumor cells, and reverses drug resistance.
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