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Targeted polymer medicament carrier and preparation method and application thereof

A polymer and targeted technology, applied in the field of biomedicine

Inactive Publication Date: 2011-04-06
JIANGXI SCI & TECH NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Retrieval shows that so far, there are only literature reports on the synthesis of Biotin-PEO-PLA block copolymers

Method used

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  • Targeted polymer medicament carrier and preparation method and application thereof
  • Targeted polymer medicament carrier and preparation method and application thereof
  • Targeted polymer medicament carrier and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Synthesis of Biotin-Pluronic-PLA-TMRCA.

[0052] a) Synthesis of Biotin-Pluronic-OH: Feed according to Pluronic:Biotin molar ratio 1:1.2, dissolve in dichloromethane, and add 4-dimethylaminopyridine, then add dropwise the solution in dichloromethane under ice-water bath conditions 1,3-Dicyclohexylcarbodiimide. After the dropwise addition, the reaction was continued at room temperature for 38 hours. Then with 10% NaHCO 3 The entire reaction solution was extracted to remove unreacted Biotin. After the extraction, the reaction solution was frozen overnight, and then filtered to remove insoluble matter. Then the reaction solution was concentrated, then dropped into cold anhydrous ether, filtered, and vacuum-dried to obtain Biotin-Pluronic-OH with one end of Biotin modified. It may contain a small amount of Biotin-Pluronic-Biotin with modified Biotin at both ends, and this polymer can be purified and removed in the reaction of step b).

[0053] b) Synthesis of Biotin-Pl...

Embodiment 2

[0056] Application of Biotin-Pluronic-PLA for targeting of cancer cells.

[0057] (1) Biotin-Pluronic-PLA nanoparticles are first prepared by a conventional method, and the nanoparticles can be prepared by dialysis. The operation steps are as follows: first dissolve 10 mg of Biotin-Pluronic-PLA copolymer in tetrahydrofuran (THF), and then add the solution dropwise into 12.5 g of ultrapure water while stirring. The formed Biotin-Pluronic-PLA nanoparticles were dialyzed in water to remove THF;

[0058] (2) Embedding the anticancer drug Paclitaxel in the nanoparticles formed by the copolymer, first dissolve Biotin-Pluronic-PLA-TMRCA 24mg and Paclitaxel 1.5mg in THF, and then add the solution dropwise to 45g of ultrapure water under stirring middle. The formed Paclitaxel-entrapped Biotin-Pluronic-PLA nanoparticles were dialyzed in water to remove THF and non-entrapped paclitaxel.

[0059] (3) The targeting of Biotin-Pluronic-PLA nanoparticles to cancer cells is realized by a th...

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Abstract

The invention relates to a targeted polymer medicament carrier and a preparation method and application thereof. The targeted polymer medicament carrier has a molecular structural formula shown in the graph. The preparation method comprises the following steps of: a) feeding Pluronic and Biotin in a molar ratio of 1:1.1-1.5; dissolving the mixture in dichloromethane; adding 4-dimethylamino pyridine; dropwise adding 1,3-dicyclohexyl carbodiimide in an ice water bath; reacting at room temperature for 24 to 48 hours; extracting reactive fluid with 10 to 15 percent NaHCO3; freezing over night; filtering to remove undissolved substances; concentrating the reactive fluid; dropping the reactive fluid into cold absolute ethyl ether; filtering, and drying in vacuum; and b) dissolving a product with dry toluene, and distilling the product in the presence of argon gas; dehydrating by an azeotropy method; cooling to the room temperature; adding lactide according to 50 to 90 percent of the weight of the product in the presence of the argon gas, and adding stannous octoate according to 0.1 to 0.15 percent of the weight of the lactide; heating to the temperature of between 120 and 140 DEG C; reacting for 6 to 8 hours under stirring; immersing a reactant into the cold ethyl ether, and filtering; and dissolving polymer by using dichloromethane, immersing into methanol, and filtering and drying. The carrier can be used as carriers of medicaments for treating and diagnosing cancers.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to a polymer drug carrier and a preparation method and application thereof. Background technique [0002] Among polymer materials, amphiphilic polymers, especially biocompatible amphiphilic polymers (that is, polymers containing both hydrophilic and hydrophobic segments) have been studied the most, because they can be Nanoparticles with various shapes are formed by self-assembly in water through the hydrophobic interaction between hydrophobic segments. This property makes amphiphilic polymers have great potential in Drug Delivery System (DDS). application prospects. Moreover, compared with small molecule surfactants such as liposomes, the nanoparticles formed by the aggregation of amphiphilic polymers have better stability. [0003] The modification of targeting groups on the surface of polymer nanoparticles can improve the selectivity of drug delivery and the effectiveness of disease tre...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K49/00A61P35/00
Inventor 熊向源李玉萍李资玲龚研春
Owner JIANGXI SCI & TECH NORMAL UNIV
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