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Application of micelles formed by polyethylene glycol derivatives in paclitaxel or derivatives thereof

A polyethylene glycol, polyethylene glycol group technology, applied in non-active ingredients medical preparations, medical preparations containing active ingredients, drug combinations, etc. The distribution and number of hydrophobic chains are difficult to precisely control, reducing tissue penetration and other problems, achieving long-term stability and controllability, overcoming low organic solvent tolerance, and highlighting the effects of biocompatibility

Active Publication Date: 2020-09-04
天津力博生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a large number of lipophilic and hydrophilic groups make the size of the block copolymer polymer micelles larger, and the hydration radius can reach more than 100nm, which reduces the tissue penetration
Moreover, it is difficult to precisely control the distribution and number of hydrophobic chains in the copolymer, which affects the precise adjustment of the release kinetics of hydrophobic compounds.

Method used

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  • Application of micelles formed by polyethylene glycol derivatives in paclitaxel or derivatives thereof
  • Application of micelles formed by polyethylene glycol derivatives in paclitaxel or derivatives thereof
  • Application of micelles formed by polyethylene glycol derivatives in paclitaxel or derivatives thereof

Examples

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preparation example Construction

[0099] The preparation method of above-mentioned polyethylene glycol derivative, described method comprises the steps:

[0100] (a) phospholipid compound, (b) polyethylene glycol PEG-(Y) with Y terminal group n , and optionally (c) fatty chain-containing compound R 4 -X 1 Mix and react to obtain the polyethylene glycol derivative.

[0101] In one embodiment of the present invention, the above raw materials are mixed in a solvent, for example, the solvent is selected from N,N-dimethylformamide.

[0102] In one embodiment of the present invention, described method comprises the steps:

[0103] (1) (a) phospholipid compound and optional (c) fatty chain-containing compound R 4 -X 1 Dissolved in a solvent to obtain a mixed solution A;

[0104] (2) the polyethylene glycol PEG-(Y) whose end group is Y in (b) n Dissolved in a solvent to obtain a mixed solution B;

[0105] (3) Mix the mixed solution A and the mixed solution B, and react at room temperature to prepare the polyet...

preparation example 1 3

[0120] Preparation Example 1 The synthesis of three aliphatic chain-polyethylene glycol derivatives (1DSPE, 1 n-octadecyl mercaptan)

[0121] Weigh 50 mg of DSPE in a 10 mL round-bottom glass flask, dissolve it in 100 μL of N,N-dimethylformamide, and add 12 μL of diisopropylethylamine to obtain a solution (1).

[0122] Take by weighing 334mg end group substituted polyethylene glycol OPSS-PEG5000-SCM (average molecular weight 5000Da, end group is the polyethylene glycol of dithiopyridyl and succinimide carboxymethyl ester respectively with 2 milliliters weighing bottle, (purchased from Beijing Jiankai Technology Co., Ltd., product number A5109), and dissolved in 400 μL DMF to obtain solution (2).

[0123] The solution (2) was added into the round-bottomed flask with the solution (1) for mixing, stirred by magnetic force, and reacted at room temperature for 4 hours under the protection of nitrogen. Thereafter, nitrogen protection was removed, and 100 μL of 0.5 M hydrochloric ac...

preparation example 2 3

[0125] Preparation Example 2 The synthesis of three aliphatic chain-polyethylene glycol derivatives (1DSPE, 1 n-octyl mercaptan)

[0126] Weigh 50 mg of DSPE in a 10 mL round bottom glass flask, dissolve it in 100 μL of DMF, add 12 μL of diisopropylethylamine to obtain solution (1).

[0127] Take by weighing 334mg end group substituted polyethylene glycol MAL-PEG5000-SCM (average molecular weight 5000Da, end group is respectively the polyethylene glycol of maleimide and succinimide carboxymethyl ester) with 2 milliliter weighing bottle , purchased from Beijing Jiankai Technology Co., Ltd., product number A5003), which was dissolved in 400 μL DMF to obtain solution (2).

[0128] Add 15 μL of 1-octanethiol (molecular weight 146, purchased from Beijing Bailingwei Technology) to solution (2), and react for 1 hour under nitrogen protection. The obtained reaction liquid was added into the round bottom flask with solution (1) for mixing, stirred by magnetic force, and reacted under ...

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Abstract

The invention relates to application of micelles formed by polyethylene glycol derivatives in paclitaxel or derivatives thereof, and belongs to the technical field of lipoid molecules. The polyethylene glycol derivative can be dispersed in a solvent to form micelles, and the micelles can be used for efficiently wrapping, delivering and releasing paclitaxel or paclitaxel derivatives. Micelles formed by the polyethylene glycol derivative have high tissue penetrability, long-acting stability and controllable release performance. Particularly, the polyethylene glycol derivative contains a phospholipid structure, so that the polyethylene glycol derivative has outstanding biocompatibility.

Description

technical field [0001] The invention relates to the use of micelles formed by polyethylene glycol derivatives in paclitaxel or its derivatives, and belongs to the technical field of lipid molecules. Background technique [0002] Many drug molecules with clear efficacy are poorly soluble in water, such as paclitaxel (trade name Taxol). Paclitaxel is a diterpenoid compound originally isolated from the bark of Yew brevifolia. It is a representative natural anticancer drug with good anticancer effects. Paclitaxel can lead to the accumulation of a large number of microtubules in cells by promoting microtubule polymerization and stabilizing the polymerized microtubules, so that cell division stops at mitosis and blocks normal cell division. Paclitaxel has a broad-spectrum curative effect on ovarian cancer, breast cancer, lung cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma, brain tumor and other tumors. It has a high cure rate for advanced ovarian cancer and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/24A61K31/337A61P35/00
CPCA61K9/1075A61K47/24A61K31/337A61P35/00
Inventor 王晓
Owner 天津力博生物科技有限公司
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