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Docetaxel solid lipid nanoparticle and preparation method thereof

A technology of solid lipid nano and docetaxel, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve problems such as poor fat solubility, and achieve increased stability, small particle size, Improve the effect of curative effect

Inactive Publication Date: 2012-07-18
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Docetaxel is poorly fat-soluble, so it is difficult to prepare it into docetaxel solid lipid nanoparticles, which has not been well solved

Method used

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  • Docetaxel solid lipid nanoparticle and preparation method thereof
  • Docetaxel solid lipid nanoparticle and preparation method thereof
  • Docetaxel solid lipid nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Take 600 mg of docetaxel, 10.0 g of glyceryl monostearate, 8.0 g of MCT, 2.0 g of Tween 80, 1.0 g of folic acid-pegylated polyhexadecyl cyanoacrylate (molecular weight 4000) and add appropriate amount Dissolve in absolute ethanol, evaporate the organic solvent to dryness under reduced pressure, and heat to dissolve at 70°C as the oil phase. Take 4.0g of Poloxamer 188, dissolve in 100ml of water for injection, and heat to 70°C as the water phase. The water phase was dropped into the oil phase under stirring at 70°C, the obtained colostrum was processed by a high-pressure homogenization method at 70°C, the docetaxel solid lipid nanoparticles were sealed and stored at 4°C. After diluting with normal saline, measure the average diameter particle size with a COULTER LS230 particle size analyzer, see figure 1 .

[0062] Average particle diameter = 126nm, SD = 17nm, encapsulation efficiency = 90.3 wt%.

Embodiment 2

[0064] Take 60mg of docetaxel, 1.0g of glyceryl monostearate, 0.8g of MCT, 0.4g of phospholipids, 0.2g of folic acid-pegylated polyhexadecyl cyanoacrylate (molecular weight: 4000), add appropriate amount of chloroform to dissolve , rotary evaporated to dry organic solvent, heated at 70°C to dissolve as oil phase. Dissolve 0.3g of Poloxamer 188 in 10ml of water for injection and heat to 70°C as the water phase. The water phase was dropped into the oil phase under stirring at 70°C, the obtained colostrum was sonicated with a 500W probe at 70°C for 2 minutes, the solid lipid nanoparticles of docetaxel were sealed and stored at 4°C. After diluting with normal saline, measure the average diameter particle size with a COULTER LS230 particle size analyzer, see figure 2 .

[0065] Average particle size = 129nm, SD = 18nm, encapsulation efficiency = 87.5 wt%.

Embodiment 3

[0067] Take 500 mg of docetaxel, 8.0 g of glyceryl behenate, 5.0 g of soybean oil, take 1.5 g of Tween 80 and add an appropriate amount of chloroform to dissolve, evaporate the organic solvent under reduced pressure, and heat to dissolve at 80°C to form the oil phase. Dissolve 5.0 g of PEG 400 and 2.0 g of Poloxamer in 100 ml of water for injection, and heat to 80°C as the water phase. The water phase is dripped into the oil phase under stirring at 80°C, the obtained colostrum is homogenized under high pressure at 70°C, the docetaxel solid lipid nanoparticles are sealed and stored at 4°C. The drug release was determined by dialysis: 1000ml of phosphate buffered saline (PBS) with a pH value of 7.4 containing 1% Tween was used as the release medium, the stirring speed was 100 revolutions per minute, and the temperature was 37±0.5°C. After sampling, inject 20 μl of sample for HPLC determination, and calculate the cumulative drug release percentage, see image 3 .

[0068] Avera...

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Abstract

The invention belongs to the field of medicine preparation and particularly relates to a docetaxel solid lipid nanoparticle and a preparation method thereof. The docetaxel solid lipid nanoparticle consists of an effective curative dose of docetaxel, solid lipid materials, liquid lipid materials, an emulsifying agent, additives, long-circulating auxiliary materials and water for injection. The docetaxel solid lipid nanoparticle provided by the invention has the characteristics of stable docetaxel structure, phagocytosis prevention of an in-vivo reticuloendothelial system and active tumor targeting, and can be stably stored.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a docetaxel solid lipid nanoparticle and a preparation method thereof. Background technique [0002] Docetaxel (docetaxel) is a new generation of taxane anti-tumor drugs developed in recent years. It is a mitosis inhibitor. In vitro experiments suggested that docetaxel could inhibit the growth of SPC Al lung adenocarcinoma cells, and the inhibitory effect was enhanced with the increase of the dose, which was related to the GZM phase arrest induced by the drug. Studies on Lewis lung cancer in vivo have shown that docetaxel inhibits the growth of tumor tissue by inducing G2 M phase arrest and apoptosis in Lewis lung cancer cells. The mechanism of action of docetaxel is similar to that of paclitaxel, but its antitumor activity is 1.3-12 times that of paclitaxel, and it has obvious curative effects on breast cancer, non-small cell lung cancer and other cancers....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/14A61K31/337A61K47/26A61K47/28A61K47/32A61K47/34A61K47/36A61P35/00
Inventor 王东凯李翔薛晓
Owner SHENYANG PHARMA UNIVERSITY
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