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Preparation method of paclitaxel nano micelle

A paclitaxel and micellar technology, applied in the field of biomedicine, can solve the problems of unrealized industrial application, widening of copolymer molecular weight distribution, long ring-opening polymerization time, etc., to avoid cyclization by-products and good targeting , good molecular weight uniformity

Inactive Publication Date: 2012-04-25
上海微丸医药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the ring-opening polymerization time of general lactone is longer (usually more than 12 hours), and the long-term high-temperature polymerization reaction is easy to trigger the cyclization reaction of the active center and the end group, and this by-product increases with the prolongation of the reaction time. , and ultimately broaden the molecular weight distribution of the copolymer (Macromolecules, 2003, 36: 1118-1124)
[0006] So far, there have been a large number of reports on the use of amphiphilic block copolymer micelles to encapsulate fat-soluble drugs in the study of tumor-targeted controlled release systems, but none of them have been able to achieve industrial applications. Beam stability, stealth effect in vivo, tumor targeting effect, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Add 20 g of polyethylene glycol monomethyl ether (molecular weight: 2000) into a well-dried polymerization bottle, and add 1 mL of stannous octoate / dichloromethane solution with a concentration of 0.1 g / mL. Heat the polymerization bottle to 75°C with an oil bath to dissolve polyethylene glycol monomethyl ether, start stirring and vacuumize to remove residual moisture and methylene chloride in the system. After 3 hours, add 20g of D,L-lactide under the protection of nitrogen, heat the polymerization bottle to 75°C with an oil bath to dissolve polyethylene glycol monomethyl ether, and vacuum-dry it again for 2 hours, then vacuum seal the polymerization bottle. The polymerization bottle was placed in an oil bath at 150° C. for 3.5 hours for polymerization. After breaking the polymerization bottle, the product was dissolved in dichloromethane, and the solution was precipitated with a large amount of anhydrous ether, and then vacuum-dried to obtain a block copolymer. Dissol...

Embodiment 2

[0033]10 g of polyethylene glycol (molecular weight 2000) was added to a well-dried polymerization bottle, and 1 mL of stannous octoate / dichloromethane solution with a concentration of 0.1 g / mL was added. Heat the polymerization bottle to 80°C with an oil bath to dissolve polyethylene glycol, start stirring and vacuumize to remove residual water and methylene chloride in the system. After 6 hours, add 20g of D,L-lactide under the protection of nitrogen, heat the polymerization bottle to 80°C with an oil bath to dissolve polyethylene glycol monomethyl ether, dry it in vacuum again for 4 hours, and then vacuum seal the polymerization bottle. Polymerized in an oil bath at 165°C for 3h. After breaking the polymerization bottle, the product was dissolved in dichloromethane, and the solution was precipitated with a large amount of anhydrous ether, and then vacuum-dried to obtain a block copolymer. Dissolve the copolymer in anhydrous dichloromethane, add triethylamine and succinic a...

Embodiment 3

[0035] Add 20 g of polyethylene glycol monomethyl ether (molecular weight: 2000) into a well-dried polymerization bottle, and add 1 mL of stannous octoate / dichloromethane solution with a concentration of 0.1 g / mL. Heat the polymerization bottle to 75°C with an oil bath to dissolve polyethylene glycol monomethyl ether, start stirring and vacuumize to remove residual moisture and methylene chloride in the system. After 12 hours, add 20g of L-lactide under the protection of nitrogen, heat the polymerization bottle to 75°C with an oil bath to dissolve polyethylene glycol monomethyl ether, dry it in vacuum again for 12 hours, and vacuum seal the polymerization bottle, place the polymerization bottle in Polymerize in an oil bath at 160°C for 3h. After breaking the polymerization bottle, the product was dissolved in dichloromethane, and the solution was precipitated with a large amount of anhydrous ether, and then vacuum-dried to obtain a block copolymer. Dissolve the copolymer in a...

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PUM

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Abstract

The invention relates to a preparation method of paclitaxel nano micelle, which comprises the following steps of: taking a block copolymer of polyether and polyester as a medicine supplementary material and paclitaxel as a medicine; and preparing the paclitaxel nano micelle by rotating an evaporation solvent, wherein the medicine supplementary material is prepared through body ring-opening polymerization, and the terminal hydroxyl group of the copolymer is modified into carboxylate so as to increase the stability of the micelle. According to the micelle disclosed by the invention, during the preparation process, no stabilizing agent is added, and the obtained medicine-carrying micelle can stably exist for over 48h under the body fluid environment, is a paclitaxel nano sustained-release carrier with a good application prospect, and has the characteristics of stability and tumour targeted effect.

Description

technical field [0001] The invention relates to biomedicine, in particular to a preparation method of paclitaxel nano micelles. Background technique [0002] Cancer is the number one disease threatening human life today. Cancer treatment is aimed at killing cancer cells. However, due to the high similarity and higher vitality between tumor cells and normal cells, existing non-surgical therapies need to continue to improve the specificity of tumor cells, which requires anticancer drugs to have higher targeting, which is currently the A constant challenge for the pharmaceutical industry and scientists. [0003] Targeted therapy for tumors is to selectively concentrate drugs on tumor tissues, thereby reducing side effects on normal tissues. Anti-tumor targeted drug delivery system is an important part of tumor targeted therapy. It can specifically or selectively deliver effective anti-cancer drugs to tumor tissues, and control the dose of drugs in specific physiological part...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/337A61K47/34A61P35/00C08G63/91C08G63/664
Inventor 蒋健庆
Owner 上海微丸医药开发有限公司
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