Paclitaxel nanoparticles and preparation method thereof

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...

AI Technical Summary

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 irritation of the gastrointestinal tract during the use of nanoparticles; after the drug is successfully prepared, it will be directly injected into the body without freezing to remove the organic solvent. The organic solvent will cause damage to the body and is not easy to store. ; The reconstitution of frozen nanoparticles has disadvantages such as poor solubility, changes in shape and particle size, etc.

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