Paclitaxel nanoparticles and preparation method thereof

A paclitaxel and nanoparticle technology, which is applied in the field of polymer nanoparticle preparation, can solve the problems of changing shape and particle size, increasing gastrointestinal irritation, and difficult storage, so as to reduce dosage, reduce toxic and side effects, and encapsulate high rate effect

Active Publication Date: 2017-01-04
SHANDONG UNIV QILU HOSPITAL
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] At present, the preparation method of nano-paclitaxel particles generally has the following problems: in order to obtain the suspension of paclitaxel polymer nanoparticles, repeated high-speed centrifugation-resuspension is required, and the steps are cumbersome; in the process of preparing the aqueous phase, surfactants need to be added , the addition of surfactants will increase the irritat

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  • Paclitaxel nanoparticles and preparation method thereof
  • Paclitaxel nanoparticles and preparation method thereof
  • Paclitaxel nanoparticles and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0044] Embodiment 1: Optimization of preparation conditions of paclitaxel nanoparticles

[0045] 1. Investigation of preparation method

[0046] Nanoparticles can be prepared by rotary evaporation, dialysis and rotary evaporation dialysis. The rotary evaporation method is to drop the solution mixed with the drug and nanomaterials into water, and stir at a certain speed to obtain a micellar solution. In the dialysis method, the drug and nano-blocks are directly loaded into the dialysis bag, and the nano-micelle solution is obtained through dialysis. The rotary evaporation dialysis method is to combine the two, the rotary evaporation method is the same as the above, the solution obtained by the rotary evaporation is put into a dialysis bag, and dialyzed in water to obtain a micellar solution. The advantage of the rotary evaporation method is that the reaction is more thorough and purer nanoparticles are obtained.

[0047] The nanoparticles prepared by different methods were o...

Embodiment 2

[0069] Embodiment 2: Preparation of folate-free paclitaxel nanoparticles

[0070] Accurately weigh 300 mg of PEG-PLA polymer, dissolve in 1 ml of tetrahydrofuran, and prepare a 300 mg / ml organic solution. Weigh 50 mg of paclitaxel in the dark, dissolve it in 1 ml of dichloromethane, and prepare an organic solution with a concentration of 50 mg / ml. Fully mix the two solutions to make a uniform solution, add 3ml polyvinyl alcohol to the mixed solution, 30-40W ultrasonic 10min, make the drug polymer solution fully mixed, mix the organic solution with 20-30 drops / Add dropwise to 30ml ultrapure water at a speed of 1 minute, and ultrasonicate for 20 minutes at 300W in an ice bath. The obtained emulsion was stirred in a water bath at normal temperature and pressure for 4 hours, the organic solvent was volatilized, centrifuged (14000r / min) for 30 minutes, the precipitate was collected, washed 4 times with distilled water, and rehydrated. Put the rehydrated micellar solution into a ...

Embodiment 3

[0072] Embodiment 3: Preparation of paclitaxel folate nanoparticles

[0073] Weigh 270mg of polymer PEG-PLA, weigh 30mg of polymer polate-PEG-PLA, make the polymer with folic acid account for 10% of the total polymer, dissolve in 1ml tetrahydrofuran, and prepare an organic solution of 300mg / ml. Weigh 50 mg of paclitaxel in the dark, dissolve it in 1 ml of dichloromethane, and prepare an organic solution with a concentration of 50 mg / ml. Fully mix the two solutions to make a uniform solution, add 3ml polyvinyl alcohol to the mixed solution, 30-40W ultrasonic 10min, make the drug polymer solution fully mixed, mix the organic solution with 20-30 drops / Add dropwise to 30ml ultrapure water at a speed of 1 minute, and ultrasonicate for 20 minutes at 300W in an ice bath. The obtained emulsion was stirred in a water bath at normal temperature and pressure for 4 hours, the organic solvent was volatilized, centrifuged (14000r / min) for 30 minutes, the precipitate was collected, washed ...

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Abstract

The invention discloses a preparation method of paclitaxel nanoparticles. The preparation method comprises the following steps of dissolving PEG-PLA or PEG-PLA and folate-PEG-PLA mixed polymer with tetrahydrofuran; dissolving paclitaxel with dichloromethane; uniformly mixing the solutions; adding 2% polyvinyl alcohol of which the volume is 1.5 times of that of the mixed solution, and performing ultrasonic mixing; dropwise adding the mixed solution into water at a speed of 20-30drop/min, and performing ultrasonic treatment in an ice bath; stirring the obtained emulsion in a water bath at a room temperature under normal pressure, volatilizing an organic solvent, performing centrifugation, collecting precipitates, washing with water, and performing re-hydration; dialyzing a hydration obtained by the re-hydration; adding 2.5wt% of a freeze-drying protective agent F-68 into the dialyzed nano micelle, and performing cryopreservation, thereby obtaining the paclitaxel nanoparticles. The method is simple in operation steps and easy to operate; after the medicament micellar solution is placed at a room temperature for one week, no medicament is released, which further proves that the medicament is wrapped in cores of the nanoparticles and the properties are relatively stable.

Description

technical field [0001] The invention relates to a preparation method of polymer nanoparticles, in particular to a paclitaxel nanoparticle and a preparation method thereof. Background technique [0002] Paclitaxel is a diterpenoid compound extracted from the bark of Pacific yew (Taxus brevifolia). However, multidrug resistance, poor solubility and chemotherapy toxicity limit its clinical efficacy. [0003] Most paclitaxel injections used clinically are paclitaxel solubilized in polyoxyethylene castor oil (CremophorEL) absolute ethanol (1:1), and diluted to the administration concentration before use. However, polyoxyethylene castor oil can cause severe allergic reactions, and patients should take antiallergic drugs before administration to reduce adverse reactions. Limiting its clinical application. In order to improve the solubility of paclitaxel, there are currently two main methods, one is chemical modification, and the other is physical encapsulation; among them, chemi...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/337A61K47/34A61K47/32A61K47/10A61P35/00
CPCA61K9/1075A61K31/337A61K47/10A61K47/32A61K47/34
Inventor 宋坤鲁在君孔北华姚舒苑存忠
Owner SHANDONG UNIV QILU HOSPITAL
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