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Pluronic P85-containing polymer as well as preparation method and application thereof

A polymer, FA-P85-PLA technology, applied in the field of biomedicine, can solve the problems of high cost and difficulty, achieve high drug embedding rate and increase the effect of anti-tumor effect

Inactive Publication Date: 2015-07-15
JIANGXI SCI & TECH NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

J.R.Baker Jr.'s research group at the University of Michigan modified the targeting group folic acid on the surface of polyamide-amine (PAMAM) dendrimers. There are specific interactions, which can effectively improve the therapeutic effect of anticancer drugs (Choi, Y. Chemistry & Biology 2005, 12, 35), however, the clinical application of dendrimers largely depends on the controllable preparation, function With the development of chemical and other related research, there are still problems such as difficulty and high cost in the controllable preparation of highly regular monodisperse peptide dendrimers

Method used

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  • Pluronic P85-containing polymer as well as preparation method and application thereof
  • Pluronic P85-containing polymer as well as preparation method and application thereof
  • Pluronic P85-containing polymer as well as preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0024] The preparation method of the FA-P85-PLA copolymer of the present invention is as follows:

[0025] 1. First add 1.67g, 3.78mmol folic acid FA and 0.72g 1,3-dicyclohexylcarbodiimide (DCC) to 100ml anhydrous dimethylsulfoxide (DMSO), stir at room temperature for 24 hours, and then 40g, 8.7mmol Pluronic P85 (PEO 26 -PPO 40 -PEO 26 ,) and 0.39g of 4-dimethylaminopyridine (DMAP) were added to it, and stirring was continued for 48 hours at room temperature. After dialysis with DMSO at 30°C for 24 hours, until the inside of the dialysis bag is clear (the molecular weight cut-off of the dialysis bag is 3500). Then, it was dialyzed with deionized water at 30°C for two days until all DMSO was dialyzed away. Then the product was spin-dried and then put into a vacuum drying oven to dry, and finally FA-P85-OH was prepared. The obtained copolymer weighed 23.6 g, and the yield was 56.6%.

[0026] 2. After the reaction flask is vacuumed and argon gas is used to deoxidize and dehumidify,...

Embodiment 2

[0029] Example 2 The FA-P85-PLA copolymer of the present invention embeds paclitaxel

[0030] 1. Preparation of FA-P85-PLA nanoparticles embedded with paclitaxel

[0031] Weigh 3 mg of FA-P85-PLA polymer and 0.3 mg of paclitaxel (Paclitaxel, PTX) into a test tube with a stopper, and add 3.3 ml of dimethyl sulfoxide (DMSO) to dissolve. Disperse the DMSO solution in 10 g of ultrapure water, pour it into a dialysis bag and dialyze for 24 hours to remove the unencapsulated paclitaxel.

[0032] 2. Determination of paclitaxel embedding rate and drug loading

[0033] Take 4ml of the nanoparticle aqueous solution in step 1 and freeze-dry, then add 4ml of acetonitrile-water (7:3v / v) mixed solution to dissolve, and then use high performance liquid chromatography (HPLC) to test, the test conditions are as follows: C18 column, 1.0 ml·min -1 The flow rate of acetonitrile-water (7:3v / v) is the mobile phase, the peak area is detected at 227nm, and the paclitaxel concentration in the sample is calcu...

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Abstract

The invention discloses a pluronic P85-containing polymer as well as a preparation method and application thereof, belongs to the field of biomedicines and discloses an amphiphilic block polymer with a novel chemical structure, and the amphiphilic block polymer contains a folic acid targeting group, takes polyoxyethylene-propylene oxide-ethylene oxide as a hydrophilic chain segment and takes polylactide as a hydrophobic chain segment, namely folic acid-polyoxyethylene-polypropylene-polyoxyethylene-polylactic acid (FA-P85-PLA) and the preparation method of the compound. The pluronic P85-containing polymer disclosed by the invention has good application prospects.

Description

Technical field [0001] The invention belongs to the field of biomedicine, and relates to a folic acid-containing targeting polymer drug carrier and a preparation method thereof. Background technique [0002] Amphiphilic polymers, especially biocompatible amphiphilic polymers (that is, polymers containing both hydrophilic and hydrophobic segments) have been extensively studied because they can pass through the gap between the hydrophobic segments in water Hydrophobicity and other self-aggregation form nanoparticles with various forms. This property makes amphiphilic polymers have great application prospects in drug release systems, such as controlled release systems and targeted release systems. We know that most of the current drugs (such as anti-cancer drugs) are hydrophobic, that is, they are insoluble in water and are easily excreted by a series of rejection reactions in the human body, such as drug resistance, enzyme degradation, etc., which greatly Limit the effectiveness o...

Claims

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Application Information

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IPC IPC(8): C08G63/685C08G63/85A61K47/34
Inventor 熊向源葛祥军龚妍春李资玲李玉萍
Owner JIANGXI SCI & TECH NORMAL UNIV
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