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Passive targeting antitumor prodrug of solid tumor and preparation method thereof

A solid tumor, targeted technology, applied in the field of anti-tumor drugs, can solve the problems of deposition, functional impact, not easy to degrade, etc.

Active Publication Date: 2010-06-09
SICHUAN YINGRUI PHARMA TECH CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since pectin is not easily degraded in the body, it can only be excreted through the kidneys. Excessive macromolecular pectin aggregates in the body may cause deposition in the lungs, kidneys and other tissues and organs, which will affect their functions. The specific consequences have not yet been seen. Related reports

Method used

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  • Passive targeting antitumor prodrug of solid tumor and preparation method thereof
  • Passive targeting antitumor prodrug of solid tumor and preparation method thereof
  • Passive targeting antitumor prodrug of solid tumor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 Solid tumor passive targeting anticancer prodrug P(A) of the present invention n preparation of

[0042] 1. Preparation of small molecule pectin:

[0043] Weigh 13.3g of pectin, add 1L of distilled water and stir to dissolve, adjust the pH with 5M NaOH to make the pH = 13, react at 65°C for 10h, and stop the reaction. Use concentrated hydrochloric acid to adjust the reaction solution to neutrality, filter with a millipore with a molecular weight cut-off of 30,000, and then filter the filtrate through a millipore with a molecular weight cut-off of 10,000, collect the solid with a molecular weight cut-off of 10,000 that does not pass through, and concentrate to dryness under reduced pressure. , vacuum-dried to obtain small molecule pectin with a molecular weight of 10,000 to 30,000.

[0044] 2. Loading of doxorubicin and cross-linking of small molecule pectin:

[0045] Weigh 1g of small molecule pectin doxorubicin with a molecular weight of 10,000 to 30,00...

Embodiment 2

[0056] Embodiment 2 Solid tumor passive targeting anticancer prodrug P(A) of the present invention n preparation of

[0057] 1. Preparation of small molecule pectin:

[0058] Weigh 13.3g of pectin, add 1L of distilled water and stir to dissolve, adjust the pH with 5M NaOH to make the pH = 13, react at 65°C for 10h, and stop the reaction. Use concentrated hydrochloric acid to adjust the reaction solution to neutrality, filter it with a millipore with a molecular weight cut-off of 10,000, and then dialyze the filtrate through a dialysis bag with a molecular weight cut-off of 7,000, collect the dialysate, concentrate it to dryness under reduced pressure, and dry it under vacuum to obtain a molecular weight of 7,000-10,000 small molecule pectin.

[0059] 2. Loading of doxorubicin and cross-linking of small molecule pectin:

[0060] Weigh 1g of small molecule pectin doxorubicin with a molecular weight of 7000-10000 and add it to the reaction bottle, add 100ml of water, stir to d...

Embodiment 3

[0063] Example 3 The solid tumor passive targeting anticancer prodrug P(A) of the present invention n preparation of

[0064] 1. Preparation of small molecule pectin:

[0065] Weigh 13.3g of pectin, add 1L of distilled water and stir to dissolve, adjust the pH with 5M NaOH to make the pH = 13, react at 65°C for 10h, and stop the reaction. The reaction solution was adjusted to neutrality with concentrated hydrochloric acid, filtered using a millipore with a molecular weight cut-off of 50,000, and the filtrate was dialyzed for 48 hours using a dialysis bag with a molecular weight cut-off of 20,000, and the distilled water was changed every 3 hours. The dialysate is concentrated to dryness under reduced pressure, and vacuum-dried to obtain small molecule pectin with a molecular weight of 20,000-50,000.

[0066] 2. Loading of doxorubicin and cross-linking of small molecule pectin:

[0067] Weigh 1g of small molecule pectin with a molecular weight of 20,000-50,000 and add it to ...

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Abstract

The invention relates to a passive targeting antitumor prodrug of solid tumor and a preparation method thereof, belonging to the field of antitumor drugs. The preparation method comprises the steps of: reacting small molecules of pectin with Mw of 5,000-45,0000 with doxorubicin to obtain pectin and doxorubicin conjugate with Mw of 100,000-1,000,0000, preparing a suspension, and processing the suspension by using a nano ultra high pressure homogenizing machine to obtain the passive targeting antitumor prodrug of solid tumor with particle diameter of 100-200 nm and melting point of 220-245 DEG C, wherein the pectin and the doxorubicin are connected by an amide bond, the pectin and the pectin are connected by an ester bond formed by condensing the carboxyl group and the hydroxyl group of pectin molecules. The cell inhibition rate of the antitumor prodrug to humanized lung carcinomas cells NCI-H446 and A549 is equivalent to that of the doxorubicin hydrochloride. In the research of the curative effect of melanoma B16 pulmonary metastasis mode mouse, the life cycle of mouse-borne tumor is 42.3+ / -12.4 days, which is remarkably higher than 23.1+ / -10.2 days of the doxorubicin hydrochloride group.

Description

technical field [0001] The invention relates to a solid tumor passive targeting anticancer prodrug and a preparation method thereof, belonging to the field of antitumor drugs. Background technique [0002] The microvascular endothelial space in normal tissues is dense and structurally complete, and macromolecules and lipid particles are difficult to penetrate through the vessel wall. Compared with microvessels in normal tissues, solid tumor tissues have rich blood vessels, irregular microvessel shape and structure, swelling, lack of vessel wall, loose arrangement of endothelial cells, poor structural integrity, wide junctional gap of endothelial cells, and lack of lymphatic return, resulting in macromolecules. Substances and lipid particles have selective high permeability and retention. This phenomenon is called the high permeability and retention effect of solid tumor tissue, or EPR effect (en-hanced permeability and retention effect) for short. Scanning electron microsco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/704A61P35/00
CPCA61K31/704A61K47/4823A61K47/48923A61K47/61A61K47/6939A61P35/00
Inventor 唐小海邱宇宋鑫
Owner SICHUAN YINGRUI PHARMA TECH CO
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