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Docetaxel-loading mixed micelle preparation and preparation method thereof

A technology for loading docetaxel and docetaxel, which is applied in the field of docetaxel-loaded mixed micelles and its preparation, can solve the problems of low bioavailability, increase drug loading, solve poor water solubility, and promote penetration The effect of retention

Inactive Publication Date: 2013-11-20
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main problem with oral docetaxel is the low bioavailability caused by p-glycoprotein (p-gp)

Method used

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  • Docetaxel-loading mixed micelle preparation and preparation method thereof
  • Docetaxel-loading mixed micelle preparation and preparation method thereof
  • Docetaxel-loading mixed micelle preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Weigh 4mg docetaxel, 40mg MPEG 3000 -PLA 2000 Copolymer, 20mg TPGS, add 4mL acetonitrile, ultrasonically dissolve the carrier material and drug completely, and remove the organic solvent acetonitrile by rotary evaporation, so that the material (MPEG-PLA copolymer and TPGS) and drug form a uniform film on the vessel wall. Weigh 10mg of CSO with amino substitution degree 50% 5000 -SA was dissolved in 2mL of water to form an aqueous solution, and the aqueous solution was transferred to a film-forming container. The aqueous solution was magnetically stirred to disperse the film at a temperature of 30°C. After stirring for 30 minutes, the resulting solution was centrifuged to obtain the supernatant docetaxel mixed micelle preparation , 4 ℃ airtight storage.

[0036] Results: The prepared docetaxel mixed micelles had a drug loading capacity of 4.2% and an encapsulation efficiency of 77.1%.

[0037] The particle size distribution figure of the prepared loaded docetaxel mixe...

Embodiment 2

[0039]Weigh 4mg docetaxel, 20mg MPEG 3000 -PLA 10000 Copolymer, 40mg TPGS, add 4mL chloroform, ultrasonically dissolve the carrier material and drug completely, and remove the organic solvent by rotary evaporation, so that the material and drug form a uniform film on the vessel wall. Weigh 10mg of CSO with amino substitution degree 50% 10000 -SA was dissolved in 2mL of water to form an aqueous solution, and the aqueous solution was transferred to a film-forming container, and the aqueous solution was used to disperse the organic film under magnetic stirring at a temperature of 40°C. After stirring for 50 minutes, the resulting solution was centrifuged to obtain the supernatant docetaxel Mixed micellar preparations, sealed and stored at 4°C.

[0040] Results: The prepared docetaxel mixed micelles had a drug loading capacity of 3.1% and an encapsulation efficiency of 54.4%.

Embodiment 3

[0042] Weigh 4mg docetaxel, 20mg MPEG 1000 -PLA 8000 Copolymer, 40mg TPGS, add 3mL ethyl acetate, ultrasonically dissolve the carrier material and drug completely, and remove the organic solvent by rotary evaporation, so that the material and drug form a uniform film on the vessel wall. Weigh 10 mg of CSO with a substitution degree of 50% 8000 -SA was dissolved in 5mL water to form an aqueous solution, and the aqueous solution was transferred to a film-forming container. The aqueous solution was magnetically stirred to disperse the film at a temperature of 25°C. After stirring for 40 minutes, the resulting solution was centrifuged to obtain the supernatant docetaxel mixed micelles Preparations, sealed and stored at 4°C.

[0043] Results: The prepared docetaxel mixed micelles had a drug loading capacity of 5.2% and an encapsulation efficiency of 83.6%.

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Abstract

The invention discloses a docetaxel-loading mixed micelle preparation and a preparation method thereof. The mixed micelle preparation is prepared by the following steps of: preparing docetaxel mixed micelle by using a thin-film dehydration method; and coating the docetaxel with hydrophobic nuclei by taking amphiphilic TPGS, MPEG-PLA and CSO-SA as carrier materials of the mixed micelle. The docetaxel-loading mixed micelle preparation is prepared by using the amphiohilic materials of TPGS, MPEG-PLA and CSO-SA, so that drug-loading rate is increased, solubility and oral bioavailability are improved, and the problems of poor water solubility, low medicine release speed, improper particle size and the like when hydrophilic medicines are prepared are solved.

Description

technical field [0001] The invention relates to a docetaxel-loaded mixed micelle preparation and a preparation method thereof. Background technique [0002] Docetaxel (DTX), also known as docetaxel, is a new type of antineoplastic drug developed in recent years, and it is the second-generation synthetic drug of paclitaxel. The mechanism of action of docetaxel is similar to that of paclitaxel, and its anti-tumor activity is 1.3-12 times that of paclitaxel. It plays an anti-tumor effect by interfering with the microtubule network necessary for cell function during cell mitosis and division. Docetaxel can bind to free tubulin, promote the assembly of tubulin into stable microtubules, and inhibit its depolymerization, resulting in the loss of normal function of microtubule bundles and the fixation of microtubules, thereby inhibiting cell mitosis . It is clinically used in breast cancer, pancreatic cancer, non-small cell lung cancer, soft tissue sarcoma, head and neck cancer, g...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/337A61K47/36A61K47/34A61P35/00
Inventor 翟光喜窦金凤张海群刘秀菊
Owner SHANDONG UNIV
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