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Cis-platinum carrier with MMP-2 response, preparation method of cis-platinum carrier, cis-platinum complex and preparation method of cis-platinum complex

A technology of MMP-2 and complexes, applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of obvious non-specific effects, toxicity, short blood half-life, etc., to achieve Avoid sudden release and non-specific interactions, reduce toxicity effects

Active Publication Date: 2021-03-12
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although various cisplatin analogues have been developed to reduce toxic side effects and improve therapeutic effects, they still have problems such as short blood half-life and obvious non-specific effects common to small molecule platinum drugs, and bring about problems in the hematopoietic system, digestive system, etc. Systemic and nervous system toxicity

Method used

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  • Cis-platinum carrier with MMP-2 response, preparation method of cis-platinum carrier, cis-platinum complex and preparation method of cis-platinum complex
  • Cis-platinum carrier with MMP-2 response, preparation method of cis-platinum carrier, cis-platinum complex and preparation method of cis-platinum complex
  • Cis-platinum carrier with MMP-2 response, preparation method of cis-platinum carrier, cis-platinum complex and preparation method of cis-platinum complex

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preparation example Construction

[0067] The present invention also provides a method for preparing the MMP-2-responsive cisplatin carrier described in the above technical solution, which is characterized in that it comprises the following steps:

[0068] A) n-hexylamine, N-benzyloxycarbonyl-L-lysine-N-cyclic carboxylic anhydride, γ-benzylglutamic acid-N-cyclic carboxylic anhydride are mixed and reacted to obtain polyamino acid nanoparticles;

[0069] B) dissolving the polyamino acid nanoparticles in haloacetic acid, performing acidolysis to remove the benzyloxycarbonyl group in the presence of hydrobromic acid and acetic acid, to obtain the compound of formula IV;

[0070] C) under the action of a catalyst, the functionalized nano-shell compound and the compound of formula IV are mixed and reacted to obtain the cisplatin carrier with MMP-2 response shown in formula I;

[0071] The functionalized nanoshell compound is a compound of formula II and / or a compound of formula III;

[0072]

[0073] in:

[0074...

Embodiment 1～3

[0140] Embodiment 1~3: the preparation of the polyethylene glycol-PLGLAG (being formula II compound) of different molecular weights

Embodiment 1

[0142] Dissolve 2.0g of mercaptopolyethylene glycol (molecular weight: 5000) and 0.3g of maleimide-based polypeptide (MI-PLGLAG-COOH) in 30mL of dichloromethane, stir and react at 25°C for 36h, and settle with diethyl ether Twice, dry to obtain the compound of formula II.

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Abstract

The invention provides a cis-platinum carrier with MMP2 response, a preparation method of the cis-platinum carrier, a cis-platinum complex and a preparation method of the cis-platinum complex. The cis-platinum carrier provided by the invention has a structure as shown in a formula I, specific branched chain sulfhydrylation polyethylene glycol maleimide polypeptide is grafted on the side chain of polyamino acid, the cis-platinum carrier can be used as a shell of cis-platinum, has certain shielding capability and MMP-2 responsiveness, and is enriched at a tumor tissue part by enhancing an osmotic retention (EPR) effect; under other normal environments of a human body, the toxicity of cis-platinum can be prevented, and under the stimulation of active oxygen conditions of overexpression of a tumor prevention part, cis-platinum can be quickly responded, automatically removed and released, and plays a role in the tumor part. Therefore, sudden release and non-specific interaction in a blood circulation system after intravenous injection can be effectively avoided so that the toxicity is reduced.

Description

technical field [0001] The invention relates to the technical field of polymer drug carriers, in particular to a cisplatin carrier with MMP-2 response and a preparation method thereof, a cisplatin complex and a preparation method thereof. Background technique [0002] Tumor has become one of the most serious diseases threatening human health. Commonly used clinical cancer treatment methods include chemotherapy, radiotherapy and surgery. Among them, chemotherapy is the most commonly used and important treatment approach. However, the clinically used antineoplastic drugs have many defects in application, such as: poor water solubility and stability, and large toxic and side effects of drugs. In order to solve these problems, drugs can be combined with drug carriers to improve the water solubility and stability of drugs, and achieve controlled release of drugs, thereby reducing the side effects of drugs on normal tissues and giving full play to the efficacy of drugs. [0003...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K47/64A61K47/69A61K33/243A61P35/00
CPCC08G81/00A61K47/64A61K47/6929A61K33/243A61P35/00
Inventor 丁建勋姜中雨栗迪庄秀丽陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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