A preparation method of ROS-responsive microsphere encapsulated mitochondria-targeted nocardicin loaded to Mxene multifunctional composite

By preparing ROS-responsive microspheres to encapsulate mitochondrial-targeting nocaketone and loading it onto Mxene multifunctional composite materials, the problems of poor water solubility and lack of targeting of nocaketone were solved, enabling the targeted release and local hyperthermia of nocaketone and enhancing the therapeutic effect of osteoarthritis.

CN122005487BActive Publication Date: 2026-08-28DONGZHIMEN HOSPITAL OF BEIJING UNIV OF CHINESE MEDICINE
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Patent Information

Application Number
CN202610272325.8
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2026-03-06
Publication Date
2026-08-28
Estimated Expiration
2046-03-06

AI Technical Summary

Technical Problem

Nocaketone has poor water solubility, rapid metabolism in the body, and lack of targeting, which limits its therapeutic effect in treating osteoarthritis.

Method used

A method for preparing a multifunctional composite material of mitochondrial-targeting nocaketone loaded onto Mxene by encapsulating mitochondrial-responsive microspheres was developed. This method involves preparing carboxylated Mxene nanosheets, loading nocaketone onto them, and utilizing hyaluronic acid-modified microspheres to achieve on-demand drug release. Combined with the photothermal conversion properties of Mxene, localized thermotherapy and targeted drug release can be achieved.

Benefits of technology

It improves the targeting and therapeutic effect of nocaketone, achieving targeted release and local thermotherapy of nocaketone, thus enhancing the therapeutic effect on osteoarthritis.

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Abstract

The application discloses a preparation method of ROS response microsphere encapsulated mitochondria targeted nocardicin loaded Mxene multifunctional composite material, relates to the technical field of biological medicine, and prepares carboxylated Mxene nanosheet, dissolves in dimethyl sulfoxide to obtain product MXene-COOH@NK, is dissolved in 2-morpholinoethanesulfonic acid MES solution to obtain product MXene-COOH@NK-Man, and on this basis, ROS response microsphere encapsulated mitochondria targeted Mxene loaded nocardicin is prepared. The ROS response microsphere encapsulated mitochondria targeted Mxene loaded nocardicin prepared by the application has the near-infrared light heat conversion performance of MXene to support light-controlled drug release and local mild thermotherapy, and after the modification of MXene-COOH@NK by mannose, the MXene-COOH@NK can be directly enriched with chondrocyte mitochondria, further inhibit the expression of inflammatory factors, the microsphere contains borate ester bonds, the borate ester bonds are broken under the high ROS environment condition of OA lesion, the site release of the drug nocardicin is realized, and the systemic exposure is reduced.
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