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A kind of polymer containing pluronic P85 and its preparation method and application

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: 2017-04-12
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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  • A kind of polymer containing pluronic P85 and its preparation method and application
  • A kind of polymer containing pluronic P85 and its preparation method and application
  • A kind of polymer containing pluronic P85 and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The preparation method of 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) into 100ml anhydrous dimethyl sulfoxide (DMSO), stir at room temperature for 24 hours, then 40g, 8.7mmol Pluronic P85 (PEO 26 -PPO 40 -PEO 26 ,) and 0.39 g of 4-dimethylaminopyridine (DMAP) were added thereto, and stirring was continued at room temperature for 48 hours. Then dialyze with DMSO at 30° C. for 24 hours until the inside of the dialysis bag becomes clear (the molecular weight cut-off of the dialysis bag is 3500). Then, it was dialyzed against deionized water at 30° C. for two days until all DMSO was dialyzed. Then the product is spin-dried and then put into a vacuum oven for drying to finally obtain FA-P85-OH. The obtained copolymer weighed 23.6 g and the yield was 56.6%.

[0026] 2. After the reaction bottle is vacuumed and dehumidified by argon, 3g of FA-P85-OH, 3g of la...

Embodiment 2

[0029] Embodiment 2 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 stoppered test tube, add 3.3 ml of dimethyl sulfoxide (DMSO) to dissolve. The DMSO solution was then dispersed in 10 g of ultrapure water, poured into a dialysis bag and dialyzed for 24 hours to remove unencapsulated paclitaxel.

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

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

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Abstract

The invention discloses a Pluronic P85-containing polymer and its preparation method and application, belonging to the field of biomedicine, and discloses a polyoxyethylene-oxypropylene-oxyethylene as a hydrophilic segment, polyoxyethylene-oxypropylene-oxyethylene, polypropylene Lactide is a polymer folic acid-polyoxyethylene-polyoxypropylene-polyoxyethylene-polylactic acid (FA-P85-PLA) with novel chemical structure as the amphiphilic block of the hydrophobic segment, and a preparation method of the compound. The invention has good application prospect.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a targeted polymer drug carrier containing folic acid 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 interactions between hydrophobic segments in water. Self-aggregation such as hydrophobic interaction forms nanoparticles with various morphologies. This property makes amphiphilic polymers have great application prospects in drug delivery systems, such as controllable release systems and targeted release systems. We know that most of the current drugs (such as anticancer drugs) are hydrophobic, that is, 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 Limitin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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