Preparation and Application of Docetaxel Lipid Nanoparticles

A technology of lipid nanoparticles and docetaxel, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, powder delivery, etc., can solve the problems of difficult clinical use, low solubility, non-absorption, etc., and achieve prolonged circulatory retention Time and material cost are low, and the effect of improving stability

Inactive Publication Date: 2014-10-08
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The solubility of docetaxel in water is very low, and it is not absorbed when taken orally, which causes difficulties in clinical use. The current marketed dosage form is only injection

Method used

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  • Preparation and Application of Docetaxel Lipid Nanoparticles
  • Preparation and Application of Docetaxel Lipid Nanoparticles
  • Preparation and Application of Docetaxel Lipid Nanoparticles

Examples

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example 1

[0059] Weigh 87.5mg cetyl palmitate, 37.5mg caprylic capric triglyceride, 5mg docetaxel, add a small amount of absolute ethanol to dissolve, heat and melt at (60±2)°C, and use it as the oil phase. Weigh 60 mg of soybean lecithin and 90 mg of polyethylene glycol 15 hydroxystearate, add 5 mL of physiological saline for injection to dissolve it ultrasonically, and rapidly heat to the same temperature as the oil phase as the water phase. Under magnetic stirring at 400r / min, the water phase was added dropwise to the oil phase where the ethanol was evaporated while hot, to prepare O / W type colostrum. The prepared colostrum was rapidly dispersed with a probe-type ultrasonic cell pulverizer, with a power of 100W, ultrasonication for 1s, interval of 1s, ultrasonication time for 4min, cooling in an ice-water bath, and passing through a 0.22μm microporous membrane. The measured particle size is 33.83nm, the PDI is 0.089, and the encapsulation efficiency is 98.26%.

example 2

[0061] Weigh 120mg glyceryl behenate, 30mg caprylic capric triglyceride, 5mg docetaxel, add a small amount of methanol to dissolve, heat and melt at (80±2)°C, and use it as the oil phase. Weigh 50 mg of soybean lecithin and 90 mg of polyethylene glycol 15 hydroxystearate, add 5 mL of physiological saline for injection to dissolve it ultrasonically, and rapidly heat to the same temperature as the oil phase as the water phase. Under magnetic stirring at 500r / min, the water phase was added dropwise to the oil phase where the methanol was evaporated while hot to prepare O / W colostrum. The prepared colostrum was quickly dispersed with a probe-type ultrasonic cell pulverizer, with a power of 200W, ultrasonication for 1s, interval of 1s, ultrasonication time for 5min, cooling in an ice-water bath, and passing through a 0.45μm microporous membrane. The measured particle size is 182.52 nm, the PDI is 0.052, and the encapsulation efficiency is 97.59%.

example 3

[0063] Weigh 120mg glyceryl palmitostearate, 30mg caprylic capric triglyceride, 6mg docetaxel, add a small amount of acetone to dissolve, heat and melt at (70±2)°C, and use it as the oil phase. Weigh 50 mg of soybean lecithin, 150 mg of polyethylene glycol 15 hydroxystearate, add 5 mL of physiological saline for ultrasonic dissolution, and rapidly heat to the same temperature as the oil phase as the water phase. Under magnetic stirring at 500r / min, the water phase was added dropwise to the oil phase evaporated from the acetone while hot to prepare O / W colostrum. The prepared colostrum was quickly dispersed with a probe-type ultrasonic cell pulverizer, with a power of 140W, ultrasonic for 1s, intermittent for 1s, ultrasonic time for 7min, cooled in an ice-water bath, and passed through a 0.22μm microporous membrane. The measured particle size is 131.6nm, the PDI is 0.211, and the encapsulation efficiency is 96.50%.

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Abstract

The invention discloses preparation and application of a docetaxel lipid nanoparticle. The docetaxel lipid nanoparticle mainly consists of docetaxel, a solid-state lipid material, a liquid-state lipid material, an emulsifying agent and normal saline for injection with treatment effective dose. The docetaxel lipid nanoparticle is proper in grain size, uniform in distribution and high in packaging ratio, can be stably stored, and has good biocompatibility and degradability; and moreover, the docetaxel is carried in the lipid nanoparticle, so that the targeting property and endocytosis of cancer cells can be improved, the antineoplastic curative effect is improved, and the toxic and side effects are reduced.

Description

technical field [0001] The invention belongs to the field of medicines and pharmaceutical preparations thereof, and in particular relates to a docetaxel lipid nanoparticle and a preparation method and application thereof. Background technique [0002] Docetaxel (also known as docetaxel, Docetaxel, DTX), as a new generation of anti-tumor drugs, is extracted from the needles of the berry yew and then semi-synthesized. Docetaxel was originally developed by the French company Rhône-Polancrele, and is used as a chemotherapy drug for breast cancer and non-small cell lung cancer. It was approved by the FDA in May 1996, and the trade name was Taxotere. It is used for the treatment of metastatic breast cancer failed in chemotherapy and metastatic non-small cell lung cancer failed in platinum-based therapy, and has been marketed in 33 countries including Britain, the United States, France, Italy, Germany and Japan. The drug has a broad anti-tumor spectrum and is the most effective s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/337A61P35/00
Inventor 齐宪荣高玮
Owner PEKING UNIV
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