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A kind of phosphatidyl nano-prodrug released by enzymatic response and its preparation method and application

A technology of phosphatidyl nano and oleoyl phosphatidylcholine, which is applied in the field of biomedicine to achieve the effect of improving tumor targeting, high stability, and ensuring effective drug concentration

Active Publication Date: 2019-08-20
江苏灵鹊生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The purpose of the present invention is to provide a phosphatidyl nano-prodrug released in an enzymatic response and its preparation method and application, thereby solving the problems of safety, stability and effective release of targeted drugs in the prior art

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  • A kind of phosphatidyl nano-prodrug released by enzymatic response and its preparation method and application
  • A kind of phosphatidyl nano-prodrug released by enzymatic response and its preparation method and application
  • A kind of phosphatidyl nano-prodrug released by enzymatic response and its preparation method and application

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Embodiment 1

[0042] The preparation of embodiment 1 phosphatidyl nanometer prodrug

[0043] 1.1 Preparation of phosphatidyl doxorubicin and its micelles

[0044] (1) Dissolve 0.3g of doxorubicin in 7ml of acetic acid-sodium acetate buffer (0.2M) and 1ml of isopropanol; dissolve 0.2g of phosphatidylcholine in 5ml of n-heptane; then mix the above solutions and ultrasonically After dissolving, add 100U phospholipase D enzyme solution;

[0045] (2) React at 45°C for 8 hours in a shaker at 220rmp;

[0046] (3) repeatedly extracting the reaction solution obtained in step (2) with chloroform;

[0047] (4) The mixed solution in step (3) is separated and purified by column chromatography, the mobile phase is chloroform: dehydrated alcohol: triethylamine: water (10:11.3:11.7:2.7), and the stationary phase is silica gel powder (300-400 mesh);

[0048] (5) Rotary evaporation: the solution separated in step (4) was subjected to rotary evaporation under the condition of 30° C. for 2 to 5 hours;

[...

Embodiment 2

[0066] Example 2 Structural identification and micellar property identification of phosphatidyl nanoprodrugs

[0067] 2.1 Confirm the chemical composition of the phosphatidyl doxorubicin and phosphatidyl mitoxantrone prepared by the method of infrared respectively in embodiment 1, the results are respectively as follows Figure 1A with Figure 1B Shown: PC characteristic peak (1) 2924cm -1 , CH on the long chain 2 Stretch vibration (2) 1736.1cm -1 , The stretching peak of -C=O of -CO=O; the characteristic peak diagram of doxorubicin (A) a: (1) 1617.1cm -1 , the peak of -C=O on the benzene ring (2) 1582.6cm -1 , the stretching peak of C=C. From the infrared spectrum of phosphatidyl doxorubicin (A)c, the characteristic peaks of PC and doxorubicin can be found (1) 2924cm -1 (2)1736.1cm -1 (3)1617.1cm -1 (4)1582.6cm -1 . Also for phosphatidyl mitoxantrone, the characteristic peaks of PC and mitoxantrone can also be found.

[0068] 2.2 The molecular weights of phosphatid...

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Abstract

The invention provides a phosphatidyl nanometer prodrug released by enzymatic response and a preparation method and application thereof. The phosphatidyl nanometer prodrug is formed by a hydrophilia antitumor drug containing primary alcohol and a phospholipid compound through bonding of a phosphorus oxygen bond under the catalytic action of phospholipase D. The invention further provides application of the phosphatidyl nanometer prodrug released by enzymatic response for releasing the antitumor drug to tumor tissue in a targeting mode. The hydrolysis / transesterification two-way reaction characteristic of the phospholipase D highly-expressed in tumor tissue is utilized creatively, and the amphipathicity phosphatidyl nanometer prodrug is obtained through biological catalytic synthesis of the phospholipase D in vitro; when the prodrug is accumulated to tumors in a targeting mode for responding to the phospholipase D to trigger hydrolysis, the antitumor drug is specifically released, and meanwhile the purposes of safety, stability and effective release of the targeting medicine are achieved.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a phosphatidyl nanometer prodrug released in response to enzymatic response, its preparation method and application. Background technique [0002] Chemotherapy drugs are usually a class of compounds with significant cytotoxicity. After being distributed throughout the body with the blood circulation, these drugs not only act on tumor cells, but also on normal cells at the same time, thus causing serious toxic and side effects and reducing the risk of death in patients. This is also the dilemma of cancer chemotherapy. How to reduce the toxic and side effects of chemotherapy drugs is an important issue in the research of chemotherapy drugs. In order to solve this bottleneck problem, people are committed to the research of drug delivery systems that can target diseased tissues, allowing chemotherapy drugs to grow "eyes", localize to tumor tissues, and play a role in targeted killing. Targ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/54A61K9/107A61K31/704A61K31/136A61P35/00
Inventor 陶欣艺王风清魏东芝贾宁陈能辉赵明
Owner 江苏灵鹊生物科技有限公司
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