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A hyperbranched-block co-grafted drug carrier loaded with antitumor drugs and its preparation method and application

An anti-tumor drug and co-grafting technology, which is applied in the field of hyperbranched-block co-grafted drug carrier and its preparation, can solve the problem of low drug utilization, prolong the time of high concentration, and enhance the therapeutic effect of tumors , the effect of structural stability

Active Publication Date: 2022-04-29
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The method provided by the invention improves the physical and chemical stability of the drug; the method provided by the invention endows hyperbranched polyglycidol with pH responsiveness, and can endow the drug with tumor targeting, thereby solving the problem of drug utilization in the process of tumor treatment low problem, while enhancing the therapeutic effect, it reduces the toxic and side effects of drug treatment; the preparation method provided by the invention is simple, and can obtain nano-medicine with high load

Method used

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  • A hyperbranched-block co-grafted drug carrier loaded with antitumor drugs and its preparation method and application
  • A hyperbranched-block co-grafted drug carrier loaded with antitumor drugs and its preparation method and application
  • A hyperbranched-block co-grafted drug carrier loaded with antitumor drugs and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: Preparation of HPG

[0042] First, trimethylolpropane (TMP) was used as the starting agent, and potassium methoxide powder was added to activate TMP under anhydrous and oxygen-free conditions at 75°C to generate active anions. After vacuum removal of the generated methanol, under the protection of nitrogen, the method of slowly adding monomeric glycidol dropwise with a syringe pump for 24 hours, and finally through cation exchange resin treatment and precipitation in 500mL acetone, finally synthesized hyperbranched polyglycidol ( HPG). During the synthesis of HPG, the ratio of the amount of TMP, potassium methoxide and glycidol used is 1:1:50-100, and the number-average relative molecular mass of the obtained HPG is 3000-25000.

Embodiment 2

[0043] Embodiment 2: Preparation of HPG-MA

[0044] Then, hyperbranched polyglycidol (marked as HPG-MA) containing double bonds at the end group was synthesized by transesterification method. The specific method is: take hyperbranched polyglycidol, dissolve and disperse it in 20mL of DMSO, add 4-dimethylaminopyridine in it, pass through nitrogen protection, add glycidyl methacrylate (GMA) drop by drop, at room temperature After stirring for 12 hours, it was poured into 1L of ether and stirred. It was observed that an orange-yellow liquid sank to the lower layer. After washing with ether for 3 times, the upper ether layer was discarded to obtain a viscous liquid. The ether was dried in vacuum at 25°C to obtain the product. During the preparation process, the mass ratio of HPG, 4-dimethylaminopyridine and GMA is controlled to be 1-10:10-50:20-200.

Embodiment 3

[0045] Embodiment 3: Preparation of HPG-SDP

[0046] Using the mercapto-alkenyl click reaction, a pH-responsive hyperbranched-block co-grafted carrier was rapidly synthesized under ultraviolet light conditions: HPG-MA was dissolved in DMSO, and then n-dodecanethiol and Mercapto-polyethylene glycol-hydroxyl (SH-PEG-OH) whose terminal group contains both mercapto and hydroxyl groups. After fully stirring evenly, add an appropriate amount of benzophenone. Under the conditions, after 30min of irradiation, through dialysis in chloroform for 3 days, change the dialysate 3 times every day, after removing the chloroform by rotary evaporation at 40°C, a pH-responsive hyperbranched-block co-grafted carrier can be obtained ( HPG-SDP). Control the number-average relative molecular mass of the SH-PEG-OH used to be 3000 or more, and the mass ratio of HPG-MA, n-dodecanethiol and SH-PEG-OH is: 1-10:10-50:20-200 .

[0047] Among them, the preparation path of HPG-SDP is as follows: figure 1...

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Abstract

The invention discloses a hyperbranched-block co-grafted drug carrier loaded with antitumor drugs: comprising a hyperbranched-block co-grafted carrier and an anti-tumor drug embedded in the hyperbranched-block co-grafted carrier Drug; hyperbranched-block co-grafted carrier is a hydrophilic core-hydrophobic bridge-hydrophilic PEG block co-grafted carrier. The invention also discloses the preparation method of the above-mentioned drug carrier: synthesize HPG-MA by transesterification method; synthesize HPG-SDP by using mercapto-alkenyl click reaction; encapsulate anti-tumor drugs in HPG by two-phase extraction-vacuum freeze-drying method ‑SDP, to obtain the drug carrier. The invention also discloses the application of the above drug carrier in the preparation of anti-tumor therapeutic drugs. The drug carrier improves the physical and chemical stability of the anti-tumor drug and endows the drug with tumor targeting, solves the problem of low utilization rate of the anti-tumor drug in organisms and reduces the toxic and side effects of drug treatment; the preparation method provided by the invention is simple And a drug carrier with a high load of antitumor drugs is obtained.

Description

technical field [0001] The invention relates to a targeting carrier, in particular to a hyperbranched-block co-grafted drug carrier loaded with antitumor drugs, a preparation method and application thereof. Background technique [0002] The clinical treatment effect of malignant tumor is not satisfactory. Research progress in drug combination therapy, nanomedicine and other fields has brought new ideas and methods to tumor treatment. Through the screening of new drug combination schemes and the use of targeted nano-drug carriers, new strategies can be provided for the treatment of malignant tumors and clinical efficacy can be improved. [0003] Hyperbranched polyglycidol (HPG) is a kind of hyperbranched polymer with rich ether bonds inside the molecule and hydroxyl rich on the molecular surface. The starting unit is generally trimethylolpropane, and the repeating unit is glycidol. The special structure and chemical bonds of HPG endow it with excellent water solubility and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/60A61K9/107A61K31/44A61P35/00C08G83/00
CPCA61K47/60A61K9/1075A61K31/44A61P35/00C08G83/006C08G83/005
Inventor 童荣亮何桂金冯孝德李顺胡家挺刘涵清吴健
Owner ZHEJIANG UNIV