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Diblock polymer-loaded micelles of taxanes, preparation method and application thereof

A technology of block polymers and taxanes, applied in the direction of drug combinations, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of poor stability and inconvenient use of micelles, and achieve good stability effects

Active Publication Date: 2017-02-01
GUANGDONG ZHONGSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a diblock polymer-loaded taxane drug micelle, aiming at solving the inconvenience and poor stability of the existing block polymer-loaded taxane drug micelle The problem

Method used

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  • Diblock polymer-loaded micelles of taxanes, preparation method and application thereof
  • Diblock polymer-loaded micelles of taxanes, preparation method and application thereof
  • Diblock polymer-loaded micelles of taxanes, preparation method and application thereof

Examples

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preparation Embodiment 1

[0034] Preparation Example 1: Add 10 g of methoxypolyethylene glycol (molecular weight: 2000) into a 100 mL three-neck round bottom flask, heat to 100° C. in an oil bath, and reduce the pressure to 500 Pa with a vacuum aspirator to carry out 30 minutes to remove moisture. Add 9.45 g of caprolactone into the flask, mix well, and lower the pressure to 500 Pa at 70° C. for 30 minutes to remove water. Then add 61.7mg of stannous octoate as a catalyst, raise the temperature to 145°C, stir for 12 hours, then add 1.1g of D,L-lactide, mix well, and stir for 12 hours. The obtained product was cooled to 40°C and dissolved in absolute ethanol, and then the solution was injected into n-pentane at -20°C to obtain a precipitated diblock polymer, and the dissolution-precipitation process was repeated twice, The mPEG-PCL-PLA diblock polymer (molecular weight 2000-2000, PCL / PLA=9:1) was purified, and the purified product was 18.5 g with a yield of 90%. The schematic diagram of the synthetic ...

preparation Embodiment 2 to 16

[0035] Preparation Examples 2 to 16: Except for controlling according to the feeding amount given in Table 1, the remaining processes obtained the corresponding mPEG-PCL-PLA according to the same steps as in Preparation Example 1, and the molecular weight, yield and yield were listed in Table 1.

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Abstract

The invention is applicable to the technical field of nano-drugs and provides a micelle composed of a taxane drug-loaded di-block polymer and a preparation method and application thereof. The micelle is prepared from a di-block polymer methoxy polyethylene glycol-polycaprolactone / polylactide and a taxane drug and reaches good balance in the aspects of drug loading capacity, an entrapment rate, a particle size, stability and the like.

Description

technical field [0001] The invention belongs to the technical field of nano-medicines, and in particular relates to a diblock polymer-loaded taxane drug micelle, a preparation method and an application thereof. Background technique [0002] Taxane drugs are a large class of natural drugs obtained from plants. They belong to diterpenoids in structural classification, so they are also called taxane diterpenes. Both paclitaxel and docetaxel belong to the taxane class of antineoplastic drugs, which are fat-soluble compounds and hardly soluble in water. They have been widely used clinically as first-line anticancer drugs. The solubility of taxane drugs in water is very low. In order to make these drugs produce the desired therapeutic effect, it is usually necessary to administer drugs in a solubilized form to patients. Polymer-loaded taxane drugs are used to make polymer gels. Bundling is an effective way. [0003] Although some existing block polymers can better realize the lo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K31/337C08G63/08A61K9/10A61K9/19A61P35/00
Inventor 龙超峰钱志勇陈小新张兰谢称石黄爱君魏于全
Owner GUANGDONG ZHONGSHENG PHARMA