Tree-like polymer nanometer drug delivery carrier targeting doxorubicin and its preparation method

A nano-drug delivery carrier, dendrimer technology, applied in the field of anti-tumor drugs, can solve the problems of inability to concentrate drug administration, difficult targeted drug administration, etc., to avoid multiple drug resistance, tumor volume and load inhibition, improve Treatment-targeted effects

Inactive Publication Date: 2013-06-05
万礼 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing nano-administration of doxorubicin prepared by PAMAM is mainly aimed at solid tumors such as liver cancer, while liquid tumors represented by

Method used

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  • Tree-like polymer nanometer drug delivery carrier targeting doxorubicin and its preparation method
  • Tree-like polymer nanometer drug delivery carrier targeting doxorubicin and its preparation method
  • Tree-like polymer nanometer drug delivery carrier targeting doxorubicin and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] PEG-b-PAMAM-hydrozone-(DOX) 8 method of making

[0064] raw material:

[0065] PEG is polyethylene glycol with a molecular weight of 5000, PAMAM is a third-generation polyamide-amine dendritic polymer, hydrozone is hydrazone, and doxorubicin.

[0066] step:

[0067] a) Polyamide-amine type dendritic polymer reacts with cystamine to obtain intermediate one:

[0068] b) Intermediate 1 is reacted with maleimide-based polyethylene glycol monomethyl ether in tris(2-chloroethyl)phosphate under the condition of pH 7.0 to obtain Intermediate 2:

[0069] c) if Figure 4 The nuclear magnetic spectrum shown shows that the nanometer drug delivery carrier is obtained by inserting a sulfhydryl group on the intermediate two through a polymerization reaction in the liquid phase.

[0070] d) Reaction of doxorubicin DOX with N-maleimido caproic acid hydrazide to obtain activated doxorubicin;

[0071] e) The activated doxorubicin reacts with the carrier to obtain the carrier drug. ...

Embodiment 2

[0082] Example 2 PEG-b-PAMAM-hydrozone-(DOX) 16 method of making

[0083] It is basically the same as Example 1, except that PEG is polyethylene glycol with a molecular weight of 9000, PAMAM is a 4th generation polyamide-amine dendritic polymer, hydrozone is hydrazone, and doxorubicin.

Embodiment 3

[0084] Example 3 PEG-b-PAMAM-hydrozone-(DOX) 4 method of making

[0085] It is basically the same as Example 1, except that PEG is polyethylene glycol with a molecular weight of 2000, PAMAM is a 2nd generation polyamide-amine dendritic polymer, hydrozone is hydrazone, and doxorubicin.

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Abstract

The invention relates to a tree-like polymer nanometer drug delivery carrier targeting doxorubicin. The structural general formula of the targeting doxorubicin is PEG-b-PAMAM-hydrozone-(DOX)n. A tree-like polymer nanometer drug delivery carrier targeting doxorubicin of liquid tumors representative to myeloma is provided in the invention. The acidic environment (pH of 5.5) of myeloma makes a hydrogen bond connecting a carrier with doxorubicin be broken, so complete doxorubicin molecules are released. The release is only carried out under the acidic condition of the myeloma, so the treatment pertinence of the drug is greatly improved. P-glycoprotein will diffuse to doxorubicin monomer elimination cells in cells, so tumor cells generate multiple drug resistances. The carrier drug can avoid the medicine efflux phenomenon caused by the p-glycoprotein and can also avoid the multiple drug resistances.

Description

technical field [0001] The invention belongs to an antitumor drug, in particular to a dendrimer nano drug delivery carrier targeting doxorubicin and a preparation method thereof. Background technique [0002] Nano-drug delivery carriers with targeting effect prepared based on dendrimers (PAMAM) are research hotspots in recent years. Chinese patent CN 102657872A discloses a graphene oxide / PAMAM / DTPA-Gd / PSCA antibody multifunctional material and its preparation method. The material is covalently modified polyamide-amine dendrimers on nano-graphene oxide flakes, The DTPA-Gd and PSCA antibodies were modified with the above amino groups. Chinese patent CN101259284A discloses a dendrimer-based liver-targeting anti-cancer nano-prodrug system, preparation and application. The invention uses polyethylene glycol-modified PAMAM of the distal liver targeting gene (T), uses doxorubicin (DOX) as a therapeutic drug, and a lysosome-degradable covalent bond between the carrier and doxorubi...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61K9/14A61P35/00C08G81/00
Inventor 杨烨顾春艳孙晓泉陆美玲万礼王旭立
Owner 万礼
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