Reduction and pH super-sensitive cross-linked polymer prodrug and preparation method and application of polymer prodrug

A technology of cross-linking polymers and polymers, which is used in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problem of capillary hyperplasia, which is difficult to supply sufficient oxygen and nutrients. question

Active Publication Date: 2021-05-18
ANHUI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In addition, based on the characteristics of rapid proliferation of tumor cells, a large amount of oxygen and nutrients are needed to supply the exponential growth of cells, and capillary hyperplasia at the tumor site is difficult to supply sufficient oxygen and nutrients

Method used

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  • Reduction and pH super-sensitive cross-linked polymer prodrug and preparation method and application of polymer prodrug
  • Reduction and pH super-sensitive cross-linked polymer prodrug and preparation method and application of polymer prodrug
  • Reduction and pH super-sensitive cross-linked polymer prodrug and preparation method and application of polymer prodrug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] A reduction and pH ultra-sensitive cross-linked polymer prodrug, its structure is shown in formula III:

[0075]

Embodiment 2

[0077] Preparation of reduction and pH ultra-sensitive cross-linked polymer prodrugs, the synthetic route is as follows:

[0078]

[0079] The preparation steps of reduction and pH ultrasensitive cross-linked polymeric prodrugs are as follows:

[0080] Formula I synthetic steps are as follows:

[0081]

[0082] The compound represented by formula I in this example and the preparation steps of the compound represented by formula I are the same as the synthesis steps in the patent with publication number CN105949467A.

[0083] Formula II synthetic route is as follows:

[0084]

[0085] The specific synthesis steps of formula II are as follows:

[0086] H 2 o 2 Dihydroxycisplatin (500mg, 1.493mmol), norcantharidin (1004mg, 5.972mmol) and triethylamine (catalytic amount) obtained by oxidation of the aqueous solution were dissolved in DMF, stirred at 65°C for 24 hours, and the solvent was distilled off under reduced pressure . Finally, the cisplatin-norcantharidin co...

Embodiment 3

[0091] Preparation of reduction and pH ultra-sensitive cross-linked polymer prodrug micelles and detection of particle size stability and critical micelle concentration:

[0092] After 50 mg of the cross-linked polymer prodrug was added to 0.5 mL of DMSO to fully dissolve, it was added dropwise into phosphate buffer (20 mL, pH 7.4, 0.01 M) and stirred for 6 h. Then, the mixture was dialyzed against deionized water (MWCO 3500Da) for 24 h, and cross-linked micelles were obtained after lyophilization.

[0093] The cross-linked micelles were dispersed in 0.01M pH 7.4 phosphate buffer and 20mg / mL SDS solution, and the particle size was measured by DLS (Malvern, Zeta-sizer Nano-ZS90) at room temperature, once a day , measured for 7 days, the particle size stability is as follows image 3 shown.

[0094] Nile red was used as a probe, and the critical micelle concentration was determined by fluorescence spectrophotometer. Under light-shielded conditions, the cross-linked micelles w...

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Abstract

The invention discloses a reduction and pH super-sensitive cross-linked polymer prodrug, relates to the technical field of controllable cross-linked polymer prodrugs, and the structural formula of the polymer prodrug is shown as a formula III. The invention also provides a preparation method and application of the polymer prodrug. The cross-linked polymer disclosed by the invention has the beneficial effects that the cross-linked polymer is compact in structure and not easy to disintegrate in a blood circulation process; extracellular orthoester is degraded at a tumor part, the particle size is increased, and the retention effect is enhanced; after the cross-linked polymer is taken by cells, the medicine is quickly released in glutathione and a stronger acid environment, and cell apoptosis is triggered; and under the dual influence of acidity / reduction in tumor cells, the medicine is quickly released, so that the treatment effect of the medicine is enhanced.

Description

technical field [0001] The invention relates to the technical field of controllable cross-linked polymer prodrugs, in particular to a reducing and pH ultra-sensitive cross-linked polymer prodrug and its preparation method and application. Background technique [0002] So far, chemotherapy is still the main method of clinical treatment of cancer. However, traditional chemotherapy has disadvantages such as poor therapeutic effect and strong side effects. In order to solve these problems, nano-drug carriers have been developed to improve tumor targeting, maintain blood circulation stability, and achieve controllable drug release. At present, most mainstream nano-drug carriers are loaded with anti-tumor drugs by physically embedding them, such as doxorubicin, paclitaxel, and methotrexate. [0003] As a broad-spectrum anticancer drug, cisplatin has a unique curative effect on reproductive system tumors (such as ovarian cancer and testicular cancer), and can work synergistically...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/59A61K47/69A61K31/365A61K33/243A61K47/55A61P35/00C08G69/48
CPCA61K47/55A61K47/595A61K47/6907A61K33/243A61K31/365A61P35/00C08G69/48
Inventor 唐汝培王石闫国卿王鑫
Owner ANHUI UNIVERSITY
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