Mixed micelle freeze-dried preparation loaded with docetaxel and preparation method thereof

A technology of docetaxel and mixed micelles, which is applied in the direction of freeze-dried delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of low encapsulation efficiency of hydrophobic drugs and stable micelles Poor drug resistance, easy leakage of drugs and other problems, to achieve the effect of increased accumulation, high encapsulation rate and good stability

Inactive Publication Date: 2014-04-02
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the small proportion of the hydrophobic segment of Pluronic, the encapsulation efficiency of hydrophobic drugs is low, and the stability of the micelles formed is poor, and the drugs are easily leaked, resulting in inactivation.

Method used

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  • Mixed micelle freeze-dried preparation loaded with docetaxel and preparation method thereof
  • Mixed micelle freeze-dried preparation loaded with docetaxel and preparation method thereof
  • Mixed micelle freeze-dried preparation loaded with docetaxel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1: Preparation of docetaxel mixed micelle formulation

[0024] Accurately weigh 5.0mg of docetaxel, PEG-PLA62.5mg, and 137.5mg of Pluronic P123, fully dissolve and mix with 15ml of acetonitrile, remove the organic solvent by rotary evaporation in a water bath at 40°C, and dry in vacuum for 12 hours to obtain a dry and transparent drug. For the membrane, heat it in a water bath to 40°C to melt the solid skeleton, add 6mL of water at the same temperature, stir at a constant speed of 1,000rpm for 1h, cool to room temperature, and pass through a 0.22μm microporous membrane to obtain a transparent mixed micellar solution of docetaxel , the average particle size is 19.9nm, and the dispersion coefficient is 0.102.

Embodiment 2

[0025] Example 2: Preparation of docetaxel mixed micellar lyophilized formulation

[0026] Accurately weigh 6.0 mg of docetaxel, 25 mg of PEG-PLA, and 175 mg of Pluronic P123, fully dissolve and mix with 15 ml of acetonitrile, remove the organic solvent by rotary evaporation in a water bath at 40°C, and dry in vacuum for 10 hours to obtain a dry and transparent drug film. After heating to 50°C to melt the solid skeleton, add 9 mL of water at the same temperature, stir at a constant speed of 1,000 rpm for 1 h, and cool to room temperature to obtain a transparent mixed micellar solution of docetaxel. Add 2% mannitol as a freeze-drying protective agent, pass through a 0.22 μm microporous membrane to sterilize, divide the solution into sterile vials, 3 mL per bottle, and obtain white loose docetaxel mixed micelles after freeze-drying Freeze-dried formulations. Take an appropriate amount of the freeze-dried preparation, redissolve it in double distilled water, and observe it under...

Embodiment 3

[0027] Example 3: Preparation of docetaxel mixed micellar lyophilized formulation

[0028] Accurately weigh 5.0 mg of docetaxel, 62.5 mg of PEG-PLA, and 37.5 mg of Pluronic P123, fully dissolve and mix with 15 ml of acetonitrile, remove the organic solvent by rotary evaporation in a water bath at 40°C, and dry in vacuum for 8 hours to obtain a dry and transparent drug. For the membrane, heat it in a water bath to 60°C to melt the solid skeleton, add 12 mL of water at the same temperature, stir at a constant speed of 1,000 rpm for 1 hour, and cool to room temperature to obtain a transparent mixed micellar solution of docetaxel. Add 2% mannitol as a freeze-drying protective agent, pass through a 0.22 μm microporous membrane to sterilize, divide the solution into sterile vials, 3 mL per bottle, and obtain white loose docetaxel mixed micelles after freeze-drying Freeze-dried formulations. After 3 months of dry storage at room temperature, 2 mL of double-distilled water was added ...

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Abstract

The invention discloses a mixed micelle freeze-dried preparation loaded with docetaxel. A preparation method of the mixed micelle freeze-dried preparation loaded with docetaxel comprises the following steps of: dissolving docetaxel, a Pluronic surfactant and a diblock copolymer into an organic solvent, rotationally evaporating the organic solvent out under reduced pressure under a water bath condition, and standing in vacuum to obtain a dry and transparent medicament film; heating the medicament film in a water bath, melting a solid framework, adding water of the same temperature for hydrating, and cooling to the room temperature to obtain a transparent docetaxel mixed micelle solution; and adding a freeze-drying protecting agent into the docetaxel mixed micelle solution, degerming with a microporous filtering film, and performing freeze drying to obtain a mixed micelle freeze-dried preparation of docetaxel, wherein the average particle diameter of the mixed micelle freeze-dried preparation is 17-25 nanometers. According to the mixed micelle freeze-dried preparation loaded with docetaxel disclosed by the invention, the solubility of docetaxel is increased greatly; and a prepared micelle has small particle diameter and high envelop rate, has the characteristics of passive targeting, long circulation and the like, and has a very good application prospect.

Description

technical field [0001] The invention relates to a freeze-dried preparation of mixed micelles loaded with docetaxel and a preparation method thereof. Background technique [0002] Docetaxel is a second-generation taxane antitumor compound obtained by semi-synthesizing natural prodrugs extracted from Taxus chinensis. Its mechanism of action is similar to paclitaxel, and it is a broad-spectrum anti-tumor drug that has cytotoxic effects on a variety of tumor cell lines. It mainly binds to tubulin, promotes tubulin polymerization to form stable microtubules and inhibits microtubules. Splitting, thereby interfering with the mitosis of tumor cells and inhibiting the differentiation of tumor cells. At present, docetaxel has become a first-line treatment drug that can effectively treat solid tumors such as breast cancer, non-small cell lung cancer, and ovarian cancer. [0003] Docetaxel molecular formula: C 43 h 53 NO 14 , the molecular weight is 807.88, and the structural formu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/337A61K47/34A61P35/00
Inventor 邵伟徐洪燕
Owner SHANDONG UNIV
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