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Platinum-icodextrin-polycaprolactone macromolecular compound, nano drug delivery system and application of nano drug delivery system

A technology of icodextrin and polycaprolactone, applied in the direction of active ingredients of heavy metal compounds, preparations for in vivo tests, medical preparations of non-active ingredients, etc., can solve problems such as poor cycle stability and poor water solubility, and achieve Improved stability, small drug particle size, and stable structure

Active Publication Date: 2021-11-09
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the defects of the prior art, the object of the present invention is to provide a platinum-icodextrin-polycaprolactone macromolecular compound, a nanometer drug-carrying system and its application, by combining carboxylated tetravalent platinum compounds and polycaprolactone The lactones are coupled with icodextrin via ester bonds to obtain a nano-drug loading system, which aims to solve the problems of poor water solubility and poor circulation stability in the blood of existing platinum prodrugs

Method used

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  • Platinum-icodextrin-polycaprolactone macromolecular compound, nano drug delivery system and application of nano drug delivery system
  • Platinum-icodextrin-polycaprolactone macromolecular compound, nano drug delivery system and application of nano drug delivery system
  • Platinum-icodextrin-polycaprolactone macromolecular compound, nano drug delivery system and application of nano drug delivery system

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preparation example Construction

[0073] The present invention also provides a platinum - preparing polycaprolactone macromolecule compound, comprising the steps of - icodextrin:

[0074] S1, oxidizing cisplatin into tetvalent platinum compound with hydrogen peroxide, reacting with an acid anhydride, and purifying the compound PT-COOH after separation.

[0075] S2, the carboxyl group on the polycaprolactone is esterified with the hydroxyl group in the Ai Topylide, and the compound ICO-PCL is obtained after separating purification;

[0076] S3, the carboxyl group on the compound Pt-COOH of step S1 is esterified in the hydroxyl group in which the hydroxyl group in the compound ICO-PCL in step S2 is esterified, and the platinum-Ai Tour is obtained after separating and purification. Ester macromolecular compound.

[0077] In some embodiments, the step S1 is specifically: cisplatin reaction mixture and hydrogen peroxide, divalent platinum oxide cisplatin become tetravalent platinum, isolated and purified tetravalent pl...

Embodiment 1

[0099] Example 1 Compound Preparation and verification and FIP embodiment PtIP

[0100] The embodiment according to the present embodiment figure 1 Preparation of compound represented by the flowchart PtIP, following these steps:

[0101] (1) Weigh 1g Cisplatin (Cisplatin, 3.33mmol) was placed in a 100mL round bottomed flask, and the flask was successively added 35mL 30% hydrogen peroxide (10-fold excess) and 25mL of ultrapure water. 50 ℃ reflux 1h. After completion of the reaction, the ice bath, the product was recrystallized precipitate, the supernatant was collected by centrifugation, and then washed with ethanol, washed three times with ether, and dried in vacuo to give a white solid powder is the oxidation product of cisplatin.

[0102] (2) Weigh accurately Previous cisplatin oxidation product 334mg (1mmol) and succinic anhydride 100mg (1mmol) was added to 50mL round bottom flask, followed by addition of molecular sieve-dried 30mL anhydrous dimethyl sulfoxide in a round botto...

Embodiment 2

[0112] Example 2 DiR embodiment entrapped preparation and characterization of nanoparticles based DPtFIP FIP co-assembled and PtIP

[0113] This embodiment utilizes several different dialysis prepared Pt-ICO-PCL and FA-ICO-PCL ratio nanoparticles, the specific operation is as follows:

[0114] (1) in accordance with the ratio of the Pt-ICO-PCL FA-ICO-PCL mass were 9: 1, 8: 2 and 7: 3 Weigh two samples, so that the total mass of the two samples was 5mg.

[0115] (2) to step (1) the ratio of each was added a solution of dimethylsulfoxide 3mL 3mgDiR dissolution, and then samples were applied to a molecular weight cutoff of the dialysis bag 3500Da. At room temperature, dialyzed in ultrapure water stirring 24h, 2h replaced once every fresh ultrapure water, the dialysis bag was collected after completion of the dialysis. A small amount of ultrafiltration (molecular weight cutoff 10 KDa) and concentrated to a final volume of 5 mL; most lyophilized stand.

[0116] By dynamic light scatter...

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Abstract

The invention belongs to the field of nano drug delivery systems, and discloses a platinum-icodextrin-polycaprolactone macromolecular compound, a nano drug delivery system and application of the nano drug delivery system. The compound is a polycaprolactone modified icodextrin-platinum conjugate, the icodextrin-platinum conjugate is formed by connecting a carboxylated tetravalent platinum compound to icodextrin through an ester bond, and the polycaprolactone is coupled with the icodextrin through the ester bond; the molecular weight of the polycaprolactone is 1 kDa to 10 kDa, and the molecular weight of the icodextrin is 10 kDa to 20 kDa; the grafting rate of the polycaprolactone on the icodextrin is 0.5-1, and the mass percentage of a platinum element in the macromolecular compound is 1%-5%. The compound contains a hydrophilic fragment icodextrin, a hydrophobic fragment polycaprolactone and tetravalent platinum, as a tumor treatment drug, the toxic and side effects of cis-platinum are reduced, the stability of circulation in blood is improved, so that the bioavailability of platinum is improved, and the anti-tumor effect is greatly enhanced.

Description

Technical field [0001] The present invention belongs to the technical field of nano-drug systems, and more particularly to a platinum-Ai Tutinine-polycaprolactone mid-polymer compound, nano-loading system and its application thereof. Background technique [0002] Tumors are the most important factors threaten by human health. Chemotherapy is one of the most effective means of treating tumors. Although many common chemotherapy drugs have certain therapeutic effects, there is still great defect in a large number of chemotherapeutic drugs currently listed. The selectivity of divalent platinum drugs on tumors is mainly derived from tumor's high demand for nutrients, but this selectivity is very weak, other rapidly growing tissue (such as bone marrow, hair follicles, etc.) will also generate toxicity due to increased intake At the same time, PT (II) drugs are often removed by kidney, so hepatotoxicity and nephrotoxicity are also produced. In addition, Pt (II) drugs are unstable, and t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K47/59A61K47/54A61K47/69A61K31/282A61K33/243A61K41/00A61K49/00A61P35/00
CPCA61K47/61A61K47/593A61K47/545A61K47/6939A61K47/6937A61K31/282A61K33/243A61K41/0057A61K49/0054A61K49/0021A61P35/00A61K2300/00Y02A50/30
Inventor 李子福杨祥良官建坤万江陵
Owner HUAZHONG UNIV OF SCI & TECH
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