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Long-circulating solid lipid docetaxel nanoparticles and preparation method thereof

A solid lipid nanometer and docetaxel technology, which is applied in the field of pharmacy, can solve the problems of short drug retention time, leakage, and rupture of drugs, and achieve the effects of improving bioavailability, prolonging circulation time, and reducing toxicity.

Inactive Publication Date: 2011-07-20
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Under the action of proteins and opsonins in the blood, traditional solid lipid nanoparticles are prone to rupture and drug leakage, and are easily phagocytized by macrophages of the reticuloendothelial system and quickly cleared in the blood circulation. The residence time of drugs in the body is short

Method used

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  • Long-circulating solid lipid docetaxel nanoparticles and preparation method thereof
  • Long-circulating solid lipid docetaxel nanoparticles and preparation method thereof
  • Long-circulating solid lipid docetaxel nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Weigh 100mg docetaxel, 800mg stearic acid, 400mg lecithin, 100mg polyethylene glycol-distearoylphosphatidylethanolamine (PEG 2000 -DSPE) was dissolved in 20ml of dichloromethane, evaporated to dryness under reduced pressure at 50°C to form a lipid film, added 25ml of Tween-80 (0.5%), ultrasonically dispersed for 30min (ultrasonic power 600W), and obtained Circulate the solid lipid nanoparticle suspension and store it at 2°C for later use. Its average particle size is 245nm, 90% of the particles are below 500nm, and the particle size distribution is narrow, indicating that the size of the long-circulation solid lipid nanoparticles is relatively uniform.

Embodiment 2

[0044] Weigh 100mg docetaxel, 2000mg soybean lecithin, 200mg hydrogenated lecithin, 400mg polyethylene glycol-dipalmitoylphosphatidylethanolamine (PEG 5000 -DPPE) into a 50ml Erlenmeyer flask with a stopper, add 10ml of ethanol: acetone (1:10) mixed solvent, ultrasonically dissolve it fully and heat to 75°C to form an organic phase. Another 150mg of Poloxamer-188 was dissolved in 30ml of double distilled water to form the water phase. Use a syringe to slowly inject the organic phase into the 75°C aqueous phase stirred at 1000r / min, and continue stirring until a translucent system is formed. The organic solvent was evaporated under reduced pressure at 40° C., the system was concentrated to 25 ml, and cooled to room temperature to obtain a long-circulation solid lipid nanoparticle suspension.

Embodiment 3

[0046] Take 100mg docetaxel, 1000mg dipalmitoylphosphatidylcholine, 100mg distearoylphosphatidylethanolamine, 100mg polyethylene glycol (molecular weight is 3350)-polycaprolactone and dissolve in chloroform:methanol (v / v, 1:1) 10ml, ultrasonically dissolved and heated to (50±2)°C to form the organic phase. Another 200mg of Myrj 53 was added into 30ml of double-distilled water, and ultrasonically dissolved to form an aqueous phase. Slowly inject the organic phase into the water phase at constant temperature of (50±2)°C stirred at 1000r / min to form colostrum, and continue to stir for about 2-3 hours to completely evaporate the organic solvent and concentrate the system to about 5ml. Quickly mix the translucent emulsion obtained in another 20ml of ice water stirred at 1000r / min at 0-2°C, continue to stir for 2 hours, and then homogenize it for 5 times in a high-pressure homogenizer (homogeneous pressure is 15000psi), namely A long-circulating solid lipid nanoparticle suspension ...

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Abstract

The invention discloses long-circulating solid lipid docetaxel nanoparticles and a preparation method thereof. The long-circulating solid lipid docetaxel nanoparticles comprise the following materials in therapeutic effective dose: docetaxel, lipid materials, long-circulating auxiliary materials and an emulsifier. The long-circulating solid lipid docetaxel nanoparticles have small particle size, high encapsulation rate and good stability, and not only improve the solubility and the stability of the docetaxel, reduce the toxicity of the docetaxel, but also prolong the circulating time of a medicament in blood, and improve the therapeutic index of the medicament, so that the preparation has the characteristics of low toxicity, low allergy, high efficiency and targeting in clinical application.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a long-circulation solid lipid nanoparticle containing an antitumor active ingredient docetaxel and a preparation method thereof. Background technique [0002] Docetaxel (DOCETAXEL), whose trade name is Taxotere, is a taxane drug that promotes the assembly of microtubule dimers into microtubules, and at the same time stabilizes microtubules by preventing the process of depolymerization, thereby blocking cells from G2 and M phase, thereby inhibiting the mitosis and proliferation of cancer cells. The pharmacological effect of docetaxel is stronger than that of paclitaxel, its intracellular concentration is 3 times higher than that of paclitaxel, and its residence time in cells is longer, its affinity for microtubules is 2 times that of paclitaxel; as a microtubule stabilizer and assembly promoter, The activity is 2 times greater than paclitaxel; as a microtubule depolymerizatio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/337A61P35/00
Inventor 李亚平陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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