Multifunctional high-polymer prodrug nano-scale drug delivery system as well as preparation method and use thereof

A nano-drug delivery system and technology of a drug delivery system, applied in the field of polymer anti-tumor drug delivery systems and preparations, can solve the problems of low relaxation rate of MRI contrast agents, overcome unsatisfactory clinical treatment effects, improve water solubility, Effect of enhancing efficacy and bioavailability

Active Publication Date: 2017-01-11
EAST CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to their low molecular weight, conventiona

Method used

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  • Multifunctional high-polymer prodrug nano-scale drug delivery system as well as preparation method and use thereof
  • Multifunctional high-polymer prodrug nano-scale drug delivery system as well as preparation method and use thereof
  • Multifunctional high-polymer prodrug nano-scale drug delivery system as well as preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0043] Example 1

[0044]Preparation of PGG-PTX-DTPA

[0045] Dissolve 4.6 mmol of PGG-PTX sodium salt in deionized water, acidify with 0.2M dilute hydrochloric acid, dialyze with deionized water, and freeze-dry. Dissolve the dried 3.5mmol PGG-PTX in 50mL of anhydrous dimethylformamide, stir for half an hour, then add 6.5mmol N-hydroxysuccinimide and 4.2mmol N-(3-dimethylaminopropyl )-N'-ethylcarbodiimide, stirred for 24 hours. The reaction mixture was poured into absolute ethanol to terminate the reaction, and the formed precipitate was collected by centrifugation, washed three times with cold ethanol, and dried under vacuum, then PGG-PTX-NHS was obtained. Dissolve 2.5 mmol PGG-PTX-NHS in 20 mL of anhydrous dimethylformamide and stir for 10 min to obtain a clear solution, then add 0.05 mmol S-2-(4-aminobenzyl)-diethyltriaminepenta Acetic acid and 0.6 mmol 4-dimethylaminopyridine were stirred for 24 hours. The reaction was terminated by pouring into 0.2M dilute hydrochlori...

Example Embodiment

[0046] Example 2

[0047] Preparation of PGG-PTX-DTPA-Gd

[0048] 0.69 mmol of PGG-PTX-DTPA was added to 0.1 M sodium acetate buffer solution with pH=5.5, and then 0.22 mmol of gadolinium chloride dissolved in 0.1 M sodium acetate solution was added, and the solution was stirred overnight. Add xylenol orange indicator to the solution, and then add dropwise 0.1M ethylenediaminetetraacetic acid disodium salt solution until the pink color disappears. Separation and purification by using G50 Sephadex column to obtain nano drug delivery system.

Example Embodiment

[0049] Example 3

[0050] Dissolve PGG-PTX and PGG-PTX-DTPA-Gd with deuterated water, and perform hydrogen spectrum scanning under Bruker's 400 mega-NMR instrument. The nuclear magnetic spectrum is as follows image 3 Shown, PGG-PTX-DTPA-Gd (II) and PGG-PTX (I) show that the molar ratio of the content of DTPA is about 8%, and the content of Gd in every gram of PGG-PTX-DTPA-Gd is measured by ICP-OES 0.21 mmol-Gd consistent.

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Abstract

The invention discloses a multifunctional high-polymer prodrug nano-scale drug delivery system as well as a preparation method and use thereof. A multifunctional high-polymer is characterized in that polyglutamy sodium glutamate is bonded with an anti-cancer drug, namely paclitaxel, so as to form a high-polymer prodrug PGG-PTX, and then the high-polymer prodrug PGG-PTX is linked with a T1 contrast agent Gd-DTPA through a peptide bond to form PGG-PTX-DTPA-Gd; and the multifunctional high-polymer has a structure represented by the following formula (shown in the description) and is clinically applied to the non-invasive diagnosis of neuclear magnetic resonance imaging on solid tumors. The nano-scale drug delivery system is characterized in that the system is of a sphere with a particle size of 30nm-40nm; free Gd-DTPA and PGG-PTX are linked together through the peptide bond, so that the relaxation rate of free Gd-DTPA is increased from 3.87nM<1>S<1> to 18.98nM<1>S<1> and is increased by 4.9 times; a high-polymer prodrug can form nano-particles in water through self-assembling, so that the water solubility and biocompatibility of the drug are improved, and the treatment effect and bioavailability of the drug are increased; the system can be applied to intravenous injection and can be passively targeted to tumors by virtue of a tumor EPR effect and has an obvious inhibition effect to the growth of lung cancer tumors; and the system can be applied to the integrated diagnosis and treatment of tumors.

Description

technical field [0001] The invention relates to the technical fields of polymer chemistry and nanometer medicine, in particular to a polymer anti-tumor drug delivery system and its preparation and use. Background technique [0002] Cancer is a disease that threatens human life. Available data show that cancer kills more people than AIDS, malaria and tuberculosis combined. Chemotherapy remains one of the most effective ways to treat cancer in the clinic. However, due to the lack of imaging technology, there is no way to trace whether conventional chemotherapy drugs enter the tumor site, resulting in poor chemotherapy effect and missing the optimal treatment time. Thus, integrated medicine provides a simple and practical approach for cancer diagnosis and cancer treatment. [0003] Theranostics integrates cancer diagnosis and cancer treatment. Since John Funkhouser, CEO of PharmaNetics, proposed it in 1998, it has become a trend in cancer treatment. With the rapid developme...

Claims

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Application Information

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IPC IPC(8): A61K49/18A61K49/12A61K47/59A61K31/337A61P35/00
CPCA61K31/337A61K49/085A61K49/128A61K49/1857
Inventor 王依婷高礼鹏周靖娥余静彭婷李奇龙闫志强王镜朱建中俞磊
Owner EAST CHINA NORMAL UNIVERSITY
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