A tetravalent platinum ester alkyne complex, degradable high polymer, nanomicelle and preparation method and application thereof

Degradable polymeric nanomicelles were prepared by click polymerization of tetravalent platinum ester acetylene complexes with diamine and monomethyl ether polyethylene glycol mPEG-NH2, which solved the problems of toxicity and drug resistance of platinum drugs in cancer chemotherapy and achieved efficient and controllable drug release and antitumor activity.

CN116925150BActive Publication Date: 2026-02-10SOUTH CHINA UNIV OF TECH
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Patent Information

Application Number
CN202310870309.5
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-07-14
Publication Date
2026-02-10
Estimated Expiration
2043-07-14

AI Technical Summary

Technical Problem

Existing platinum-based drugs have systemic toxicity and tumor cell resistance in cancer chemotherapy. Traditional nanocarrier systems have drawbacks such as premature release, low drug loading capacity, and uncontrollable release, which limit their clinical application.

Method used

A biodegradable polymer was prepared by a tetravalent platinum ester acetylene complex, diamine, and monomethyl ether polyethylene glycol mPEG-NH2 via acetylene-amine click polymerization. This polymer forms nanomicelles that exhibit reduction and acid environment responsiveness, enabling high drug loading and controlled release.

Benefits of technology

It achieves efficient degradation and release of anticancer active drugs in the tumor microenvironment, exhibiting high antitumor activity and low cytotoxicity, thus improving the therapeutic effect of platinum drugs.

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Abstract

The application discloses a tetravalent platinum ester alkyne complex, a degradable high polymer, a nanomicelle and a preparation method and application thereof; the structural formula of the tetravalent platinum ester alkyne complex is shown as formula (I); the preparation method of the degradable high polymer is as follows: the tetravalent platinum ester alkyne complex is prepared first; then the obtained tetravalent platinum ester alkyne complex and diamine and monomethyl ether polyethylene glycol mPEG-NH2 are clicked to obtain a triblock high polymer. The nanomicelle of the degradable high polymer is also disclosed. The tetravalent platinum ester alkyne complex disclosed by the application can specifically respond to reducing substances in a tumor microenvironment, and the enamine ester structure generated by the reaction of the tetravalent platinum ester alkyne complex with diamine also has the property of responding to an acidic environment; the high polymer has mild and simple preparation conditions, the molecular weight can reach 35200, and the platinum drug loading capacity is as high as 33.91%; the nanomicelle can efficiently degrade and release anticancer active drugs in the tumor microenvironment, and has high antitumor activity and low cytotoxicity.
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