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Long-circulating taxol nanoparticles and preparation method thereof

A paclitaxel and nanoparticle technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as increased cycle time, inability to exert drug efficacy, and short cycle time, and achieve Effect of reducing conditioning effect, prolonging administration time, and convenient administration

Inactive Publication Date: 2011-11-23
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] However, because PLA and PLGA nanoparticles are easily recognized and phagocytized by macrophages, the circulation time in the body is short, and they cannot exert sufficient drug effects.
The use of polyethylene glycol (polyethylene glycol, PEG) to modify nanoparticles to escape the opsonization in vivo to increase the circulation time in nanoparticles has become a hot spot in the preparation of long-circulating nanoparticles in recent years, but the current technology in this area is not yet available. Mature, there is no mature preparation process that can prepare ideal (long residence time in the body, good effect) nanoparticles, and can be used for large-scale production

Method used

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  • Long-circulating taxol nanoparticles and preparation method thereof
  • Long-circulating taxol nanoparticles and preparation method thereof
  • Long-circulating taxol nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of Long Circulating Paclitaxel Nanoparticles

[0025] 540mg PLA-PEG and 27mg paclitaxel were dissolved together in 10mL dichloromethane as the oil phase, 2g F68 was dissolved in 100mL double distilled water as the water phase; the oil phase was mixed with the water phase (the ratio of oil phase to water was 1:10), 20000rpm High-speed shearing for 10 minutes to obtain milky white colostrum; use a high-pressure milk homogenizer at 300bar for 5 times, 600bar for 10 times, and 1000bar for 20 times to obtain the milky liquid; use a magnetic stirrer at 300rpm for 3 hours to make the milk homogenate. The organic solvent was completely volatilized, and long-circulating paclitaxel nanoparticles were obtained. The transmission electron microscope photo was as follows figure 1 As shown, its particle size distribution is shown in figure 2 shown.

Embodiment 2

[0026] Example 2: Preparation of Long Circulating Paclitaxel Nanoparticles

[0027] 5.4, ​​LA-PEG and 270mg paclitaxel were dissolved together in 100mL dichloromethane as the oil phase, 20g F68 was dissolved in 1000mL double distilled water as the water phase; the oil phase was mixed with the water phase (the ratio of oil phase to water is 1:10) , 33000rpm high-speed shearing for 10min to obtain milky white colostrum; use the high-pressure milk homogenizer 300bar milking 5 times, 600bar milking 10 times, 1200bar milking 5 times, 1500bar milking 20 times to obtain the liquid after milking; use Magnetic stirring was performed at 500 rpm for 5 hours to completely volatilize the organic solvent to obtain long-circulating paclitaxel nanoparticles.

Embodiment 3

[0028] Example 3: Preparation of Long Circulating Paclitaxel Nanoparticles

[0029] 540mg PLA-PEG and 54mg paclitaxel were dissolved in 5mL of dichloromethane as the oil phase, and 5g of F68 was dissolved in 100mL of double distilled water as the water phase; the oil phase was mixed with the water phase (the ratio of oil phase to water was 1:20), 14000rpm High-speed shearing for 5 minutes to obtain milky white colostrum; use a high-pressure milk homogenizer at 300bar for 5 times, 600bar for 10 times, 1000bar for 15 times, and 1500bar for 20 times to obtain the liquid after milking; use magnetic stirring Stir at 700 rpm for 3 hours to completely volatilize the organic solvent to obtain long-circulating paclitaxel nanoparticles.

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Abstract

The invention discloses long-circulating taxol nanoparticles which have strong and lasting effect, high curative effect and low toxic side effect and can be administered through intravenous injection or intravenous drip. The long-circulating taxol nanoparticles are prepared from the following raw materials in parts by weight: 1 part of taxol, 5-20 parts of carrier material and 34-132 parts of emulsifier; the nanoparticles have a particle size range of 50-450nm; and the carrier material is PLA-PEG (polylactic acid-polyethylene glycol) or PLGA-PEG (poly(lactic-co-glycolic acid)-polyethylene glycol). The preparation method comprises the following steps of: dissolving the carrier material and the taxol in an organic solvent to be used as an oil phase, dissolving the emulsifier in double-distilled water to be used as a water phase; then mixing the oil phase with the water phase in a certain proportion, shearing at high speed to obtain a milky white primary emulsion; homogenizing the primary emulsion by a high pressure homogenizer to obtain homogenized liquid; and stirring at low speed for 3-5 hours to fully volatilize the organic solvent, thus obtaining the long-circulating taxol nanoparticles.

Description

technical field [0001] The invention relates to a long-circulating paclitaxel nanoparticle and a preparation method thereof. Background technique [0002] Paclitaxel is a complex secondary metabolite in Taxus genus, and it is one of the first-line drugs in clinical application. It is mainly suitable for ovarian cancer and breast cancer, and also has certain curative effect on lung cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma and brain tumor. However, traditional taxane drugs are difficult to be administered clinically due to their low solubility, and auxiliary solvents are required. However, most auxiliary solvents have toxic and side effects. For example, polyoxyethylene castor oil has been reported to produce hypersensitivity reactions, nephrotoxicity, neurotoxicity and cardiotoxicity. side effect. This obviously increases the toxicity of the drug and severely limits the efficacy improvement and safe application of this type of drug. [0003] In r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/337A61K47/34A61P35/00
Inventor 张娜刘永军张鹏
Owner SHANDONG UNIV
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