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High-stability polyethylene glycol-polyester polymer and application thereof

A polyethylene glycol, high-stability technology, applied in non-active ingredients medical preparations, pharmaceutical formulations, etc., can solve the problems of insufficient polymer excretion, reduced biodegradability, toxicity, etc., to simplify industrial production process, improving targeting, and the effect of high drug loading

Active Publication Date: 2015-05-13
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to do this, the molecular weight or concentration of the polymer should be adjusted, however, as the molecular weight increases, its biodegradability also decreases, so the excretion of the polymer from the body is insufficient and they accumulate in the organs where cause toxic effects

Method used

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  • High-stability polyethylene glycol-polyester polymer and application thereof
  • High-stability polyethylene glycol-polyester polymer and application thereof
  • High-stability polyethylene glycol-polyester polymer and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Synthesis of amphiphilic block copolymer mPEG-PDLLA-CA

[0036] The mPEG-PDLLA diblock copolymer was synthesized by ring-opening polymerization. After the polymer tube is soaked in chromic acid washing solution, it is washed with distilled water and dried for later use. Weigh a certain proportion of polyethylene glycol monomethyl ether (mPEG2000) and lactide monomer into a dry polymerization tube, and then add the catalyst Sn(Oct) 2 (The dosage is 1‰ of the weight of the reactant). After deoxygenation with high-purity nitrogen, the tube was sealed under vacuum and reacted in an oven at 140°C for 6 hours to obtain a light yellow transparent semi-solid product. The obtained crude product was cooled, dissolved with a small amount of dichloromethane and then transferred to a small beaker, precipitated with a large amount of ether in the cold trap, and the crystals were suction filtered. This operation was repeated twice to obtain a relatively pure two-stage pol...

Embodiment 2

[0040] The mensuration of embodiment 2 block copolymer CMC

[0041] (1) Preparation of stock solution

[0042] Preparation of pyrene stock solution: Weigh 6mg of pyrene into a 50mL brown volumetric flask, add acetone to dissolve and dilute to the scale to make 6×10 -4 mol L -1 pyrene solution. Accurately measure 1.0mL into a 25mL volumetric flask, add acetone to constant volume, and obtain a concentration of 2.4×10 -5 mol L -1 Pyrene solution, accurately draw 10mL into a 100mL brown volumetric flask, and dilute with acetone to a final concentration of 2.4×10 -6 mol L -1 , to obtain the stock solution of pyrene.

[0043] Preparation of polymer stock solution: Weigh 20 mg of mPEG-PDLLA-CA block copolymer into a 20 mL volumetric flask, dissolve in distilled water and dilute to the mark to obtain a concentration of 1 mg·mL -1 polymer stock solution.

[0044] (2) Determination of CMC

[0045] Sample preparation: Add 500uL pyrene stock solution to a 10 mL volumetric fla...

Embodiment 3

[0053] Example 3 Preparation and particle size determination of paclitaxel-loaded polymer micelles

[0054] Freeze-drying method: First weigh 7 mg of paclitaxel and dissolve it in tert-butanol, and then mix it with an aqueous solution containing 20 mg of mPEG-PDLLA-CA block copolymer, so that the volume ratio of water / tert-butanol is 70:30. The mixed solution was stirred at 4°C for 3 hours, then sterilized by filtration with a 0.22um microporous membrane, and freeze-dried to obtain the paclitaxel-loaded polymer micelles, which were diluted with water for injection or other solvents before use.

[0055] Dialysis method: Weigh 20mg of mPEG-PDLLA-CA block copolymer and 7mg of paclitaxel, dissolve them in 10mlL DMSO, sonicate for 10min, stir overnight to fully extend the chain segment, drop 20% distilled water in advance, stir for 2h, and use distilled water Dialysis was performed for 24 hours, and the dialysis medium was replaced at regular intervals. Finally, centrifuge at 10...

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Abstract

The invention belongs to the technical field of medicine, relates to a high-stability polyethylene glycol-polyester polymer and its application, in particular to an amphiphilic block copolymer having a hydrophilic block and a hydrophobic block with a terminal hydroxyl group A substance, wherein the terminal hydroxyl group of the hydrophobic block is replaced by a cholic acid group. The hydrophilic A block is selected from any one of polyethylene glycol monomethyl ether, polyethylene glycol, polyvinyl alcohol and polyvinyl pyrrolidone; wherein the hydrophobic B block is selected from polylactide, polylactide-co-glycolide Esters, polyglycolide, polycaprolactone, polylactide-co-caprolactone, polyglycolide-co-caprolactone and polylactide-co-glycolide-cocaprolactone any of the esters. The polymer can spontaneously form micelles with high stability in aqueous medium, and can be used as a carrier of various poorly water-soluble drugs.

Description

technical field [0001] The invention relates to a high-stability polyethylene glycol-polyester polymer and its application, in particular to an amphiphilic block copolymer comprising a hydrophilic A block and a hydrophobic B block with a terminal hydroxyl group and its application. Background technique [0002] As an effective drug delivery carrier, polymer micelles have received extensive attention. Polymer micelles are self-assembled structures formed spontaneously in water by amphiphilic polymer materials, which have a hydrophobic core and a hydrophilic Typical structure of the shell. Among them, the hydrophobic block forms a hydrophobic core for loading drugs, while the hydrophilic block wraps around to form a hydrophilic shell to play a protective role. Compared with other carriers, block copolymer micelles have the following advantages: (1) The particle size is small, so that it is not easy to be phagocytized by reticuloendothelial tissue RES, so it can circulate in t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G63/91C08G63/66A61K47/34
Inventor 乔明曦曾剑夫陈大为朱嘉胡海洋赵秀丽
Owner SHENYANG PHARMA UNIVERSITY
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