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Preparation and application of a reduction-responsive PEGylated drug nanocomposition

A polyethylene glycol and drug compound technology, which can be used in drug combinations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve problems such as adequate release of unfavorable drugs, and achieve good clinical application value. , improve safety, improve efficacy

Active Publication Date: 2016-09-14
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this type of drug delivery system still has shortcomings: when the nanoparticles reach the target site, the outer hydrophilic shell will delay the uptake of the drug by the target cells, which is not conducive to the full release of the drug

Method used

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  • Preparation and application of a reduction-responsive PEGylated drug nanocomposition
  • Preparation and application of a reduction-responsive PEGylated drug nanocomposition
  • Preparation and application of a reduction-responsive PEGylated drug nanocomposition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1, the synthesis of polyethylene glycol-disulfide bond-paclitaxel

[0054] Preparation of Py-SS-COOH:

[0055] Add dithiobipyridine (Py-SS-Py, 2g, 9.06mmol) into 16mL of ethanol (EtOH), add 214μL of acetic acid (AcOH), and add 3-mercaptopropionic acid (0.48g, 4.53mmol) dropwise under vigorous stirring ) in EtOH. After reacting for 2 hours, the EtOH was evaporated under reduced pressure, separated by a neutral alumina column, concentrated, and the solid was precipitated by adding cold water, filtered by suction, and dried in vacuum overnight to obtain the product as a white solid with a yield of 25%. NMR, mass spectrometry detection, the results are as follows figure 1 and figure 2 .

[0056] Preparation of PEG-SS-COOH:

[0057] SH-PEG 5000 (500mg, 0.1mol) was dissolved in 7mL distilled dichloromethane (DCM), 0.5mL AcOH was added, under nitrogen protection, under vigorous stirring, dithiopyralidic acid (Py-SS-COOH, 214mg, 1mol) was added dropwise. Chlo...

Embodiment 2

[0060] Embodiment 2, the synthesis of polyethylene glycol-disulfide bond-docetaxel

[0061] The synthesis method is the same as in Example 1, wherein docetaxel is used instead of paclitaxel to obtain polyethylene glycol derivatives of docetaxel.

Embodiment 3

[0062] Embodiment 3, the synthesis of polyethylene glycol-disulfide bond-paclitaxel

[0063] Synthetic method is the same as embodiment 1, wherein with PEG 2000 -SH instead of PEG 5000 -SH, to obtain polyethylene glycol-disulfide bond-paclitaxel complexes with different molecular weights.

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Abstract

The invention relates to a preparation method and application of a reduction-response-type pegylation (PEG) nanomedicine composition. The nanomedicine composition is characterized by being prepared by coupling the PEG with a medicine via disulfide bonds which are sensitive in reduction. Thus, the water solubility of the medicine is improved; the in-vivo behavior of the medicine is also improved. Meanwhile, the full release and the activity of the medicine are ensured by utilizing the characteristic that the disulfide bonds in the PEG medicine, which are sensitive in reduction, can be specifically degraded in a tumor site. Thus, a good tumor treatment scheme is provided.

Description

technical field [0001] The invention relates to a preparation method of a reduction-responsive nano composition formed by a hydrophobic drug and its polymer derivative, and its application in tumor treatment, belonging to the field of pharmaceutical preparations. Background technique: [0002] Cancer seriously endangers human life and health. In the clinical treatment of tumors, chemotherapy still plays an important role. At present, many chemotherapeutic drugs have problems such as poor water solubility, low selectivity, easy clearance by the reticuloendothelial system, rapid metabolism in the body, and severe side effects, which limit the clinical application. [0003] Paclitaxel drugs have obvious anticancer effects. Paclitaxel (PTX) and docetaxel (Docetaxel) are currently used clinically. The former is a natural diterpenoid extracted from Taxus genus with high anti-tumor activity and strong fat solubility; the latter uses 10-deacetylbaccatin (10-DAB) as the core skele...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K9/14A61K31/704A61K31/337A61P35/00
Inventor 王学清串星星张强张华代文兵宋钦
Owner PEKING UNIV