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Triblock copolymer micelle and freeze-drying preparation loading taxane medicaments, and preparation method and application thereof

A technology of taxanes and freeze-dried preparations, which is applied in the direction of drug combination, drug delivery, and medical preparations of non-active ingredients, etc., which can solve the problem of death, increased toxicity and side effects, and limit the clinical application of taxanes such as paclitaxel and other problems, to achieve the effect of simple preparation process, easy operation of preparation process and good stability

Inactive Publication Date: 2011-09-28
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Docetaxel injection is also a solution composed of docetaxel Tween 80 and ethanol, and the clinical trials are somewhat similar to paclitaxel injection; but EL, Tween 80 and ethanol often cause strong side effects, such as hypersensitivity, hemolysis, nephrotoxicity, neurotoxicity and cardiotoxicity, etc., which may lead to death in severe cases
And with the dose increasing, the side effects tend to increase
Therefore, the clinical application of taxanes such as paclitaxel is greatly limited.
[0003] Those skilled in the art have been working on reducing toxic and side effects, or increasing its drug concentration in target organs, in order to better exert its curative effect, but there is still no effective solution to the problems encountered by taxanes in clinical anti-tumor

Method used

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  • Triblock copolymer micelle and freeze-drying preparation loading taxane medicaments, and preparation method and application thereof
  • Triblock copolymer micelle and freeze-drying preparation loading taxane medicaments, and preparation method and application thereof
  • Triblock copolymer micelle and freeze-drying preparation loading taxane medicaments, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] (1) 92mg poly(ε-caprolactone)-polyethylene glycol-poly(ε-caprolactone) triblock copolymer (PCL 850 -PEG 2000 -PCL 850 ) and 8 mg of paclitaxel were dissolved in 2 ml of absolute ethanol, heated and stirred until completely dissolved to obtain a clear solution A;

[0071] (2) Under heating conditions, the clear solution A is rotary evaporated to remove the organic solvent to make it a transparent gel B;

[0072] (3) Add 5ml of preheated water for injection into gel B, make it clear and transparent under the condition of heating and stirring, and pass through a 0.22 μm filter membrane to obtain micelles C with a particle size of 10nm-100nm;

[0073] (4) Freeze-dry the micelles C to obtain the final stable nano drug freeze-dried powder D.

[0074] The freeze-dried powder is added with water for injection before clinical use, and will automatically form nano-sized micelles under the condition of heating.

[0075] The obtained micelles C, lyophilized powder D and final r...

Embodiment 2

[0077] (1) 92mg poly(ε-caprolactone)-polyethylene glycol-poly(ε-caprolactone) triblock copolymer (PCL 850 -PEG 2000 -PCL 850 ) and 8 mg of docetaxel were dissolved in 2 ml of absolute ethanol, heated and stirred until completely dissolved to obtain a clear solution A;

[0078] (2) Under heating conditions, the clear solution A is rotary evaporated to remove the organic solvent to make it a transparent gel B;

[0079] (3) Add gel B to 5 ml of preheated water for injection, make it clear and transparent under the condition of heating and stirring, and pass through a 0.22 μm filter membrane to obtain micelles C with a particle size of 10 nm-100 nm;

[0080] (4) Freeze-dry the micelles C to obtain the final stable nano drug freeze-dried powder D; the freeze-dried powder will automatically form nano-scale micelles under the condition of heating with water for injection before clinical use.

[0081] The drug loading of the obtained nano-micelle is 8.2%, and the encapsulation effi...

Embodiment 3

[0083] (1) 92mg poly(ε-caprolactone)-polyethylene glycol-poly(ε-caprolactone) triblock copolymer (PCL 850 -PEG 2000 -PCL 850 ) and 15.4mg of docetaxel were dissolved in 2ml of absolute ethanol, heated and stirred until completely dissolved to obtain a clear solution A;

[0084] (2) Under heating conditions, the clear solution A is rotary evaporated to remove the organic solvent to make it a transparent gel B;

[0085] (3) Add gel B to 5 ml of preheated water for injection, make it clear and transparent under the condition of heating and stirring, and pass through a 0.22 μm filter membrane to obtain micelles C with a particle size of 10 nm-100 nm;

[0086] (4) Freeze-dry the micelles C to obtain the final stable nano drug freeze-dried powder D; the freeze-dried powder will automatically form nano-scale micelles under the condition of heating with water for injection before clinical use.

[0087] The drug loading of the obtained nano-micelle was 15.1%, and the encapsulation eff...

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Abstract

The invention belongs to the technical fields of medicament forms and preparation of nano medicaments, and relates to a triblock copolymer micelle and freeze-drying preparation loading taxane medicaments, and a preparation method and application thereof. In order to enable the micelle provided by the invention to be used clinically, the loading capacity, entrapment rate and stability of the preparation need to be guaranteed. The micelle is prepared from the following components in parts by weight: 1 part of taxane medicament and 1.5-99 parts of triblock copolymer polycaprolactone-polyethylene glycol-polycaprolactone, wherein the molecular weight ratio of polycaprolactone to polyethylene glycol in the triblock copolymer is 0.5-3. The micelle or freeze-drying preparation loading taxane medicaments can be used for treating patients with cancer, tumors, Kaposi sarcoma, malignant tumors, tissue dysfunction or hyperplasia secondary to tissue damage and any other disease capable of reacting with the taxane medicaments, and has especially obvious curative effects on hepatoma, liver metastasis, ovarian cancer and breast cancer.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical dosage forms and nano-medicines, and in particular relates to micelles and freeze-dried preparations of tri-block polymers loaded with taxanes, as well as a preparation method and application thereof. Background technique [0002] Taxane compounds are a large class of natural products obtained from plants, and belong to diterpenoids in terms of structural classification, so they are also called taxane diterpenes. Paclitaxel, the star molecule in this class of compounds, is an important anticancer drug used clinically. Paclitaxel (trade name: Taxol) is a natural anti-cancer raw material extracted from yew or yew tree. It is a white crystalline powder, insoluble in water, and easily soluble in organic solvents such as chloroform and acetone. Docetaxel (trade name: Taxotere) is a compound synthesized from the needle leaf extract of berry yew (Taxusbaccata, Europeyew), which is ...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61P35/00A61K31/337A61P35/04A61K9/00
Inventor 钱志勇魏于全王成赵霞
Owner SICHUAN UNIV
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