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Taxol nanometer particle and preparation method and application thereof

A nanoparticle and paclitaxel technology, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of functional modification of chitosan, and avoid modification steps and operation processes Convenience and the effect of improving curative effect

Inactive Publication Date: 2008-04-30
SHANGHAI TENTH PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by this invention is to provide a kind of paclitaxel nanoparticle and its preparation method and application, to overcome the related technology that existing chitosan derivatives need to carry out functional modification to chitosan in advance as the drug carrier of paclitaxel defect

Method used

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  • Taxol nanometer particle and preparation method and application thereof
  • Taxol nanometer particle and preparation method and application thereof
  • Taxol nanometer particle and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Adopt solvent volatilization method and emulsion cross-linking method, paclitaxel nano-particle is wrapped with chitosan, obtain the spherical particle that particle size is about 80 ± 30nm, specific implementation method is as follows:

[0035] (1) 30mg paclitaxel 0.5mL ethanol solution was added dropwise to 50mL water containing 50mg surfactant sodium dodecyl sulfate (SDS), at room temperature, with the volatilization of ethanol solvent, paclitaxel nanoparticles (PTX NPs);

[0036] (2) Mix 100 mg of chitosan, PTX NPs and 0.5 mL of 0.5% dilute acetic acid solution (mass ratio), add to 80 mL of liquid paraffin, and stir at a constant temperature of 25 ° C for 4 hours;

[0037] (3) Add 0.5 mL of 2% trisodium citrate to the mixture, and react for 30 minutes to solidify and precipitate particles; wash the obtained particles with petroleum ether and isopropanol respectively, and dry and store the particles in vacuum. Particle characterization was carried out with testing i...

Embodiment 2

[0039] (1) Add 50 mg of paclitaxel and 0.5 mL of ethanol solution dropwise to 50 mL of water containing 50 mg of sodium lauryl sulfate, and at room temperature, as the ethanol solvent volatilizes, paclitaxel nanoparticles (PTX NPs) are prepared;

[0040] (2) Mix 100 mg of chitosan, PTX NPs, and 2 mL of 0.5% dilute acetic acid solution (mass ratio), add to 70 mL of liquid paraffin, and stir at a constant temperature of 35 ° C for 1 hour;

[0041] (3) Add 0.5 mL of 2% trisodium citrate to the mixture, and react for 30 minutes to solidify and precipitate particles; wash the obtained particles with petroleum ether and isopropanol respectively, and dry and store the particles in vacuum.

Embodiment 3

[0043]Ovarian cancer cells A2780 in logarithmic growth were adjusted to 1×10 4 cells / mL were inoculated in a 96-well culture plate, 100 μL per well. Three different concentrations of chitosan drug-loaded nanoparticles (25 μg / mL, 2.5 μg / mL, 0.25 μg / mL) were added, and each concentration was paralleled to 4 wells. Give 10% bovine serum 1640 culture solution, add 100 μL to each hole, culture for 24h, 48h, 72h and 96h respectively, and observe the effect of the prepared particles on the cells for promoting apoptosis. The experimental results are shown in Figure 1.

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Abstract

The invention relates to paclitaxel nanometer particles, which can be made by the following preparation process: putting the paclitaxel alcoholic solution containing surface activator under the room temperature, by which paclitaxel nanometer particles are gained as the volatilization of alcoholic solution, dissolving the paclitaxel nanometer particles in chitose solution as aqueous phase, mixing the aqueous phase with the oil phase under the temperature of 25-35 DEG C, and chuning for 1-4 hours, by which emulsion is prepared, solidifying and precipitating chitose nanometer particles of paclitaxel from the emulsion by cross linking agent, washing the particles by organic solvent, by which the nanometer particles carrying paclitaxel is made after vacuum drying. The process doesn't need any chemical modification to the chitose. The prepared nanometer particles carrying medicament has explicit slow-release effect on the death of tumour cell.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a paclitaxel nano particle and a preparation method and application thereof. Background technique [0002] Paclitaxel (PTX) is a diterpenoid compound with anticancer activity extracted from Taxus genus plants. As one of the best anti-tumor drugs at present, it has been widely used clinically, especially for the treatment of breast cancer and ovarian cancer. But its water solubility is extremely poor, in order to increase its solubility, be convenient to clinical administration, paclitaxel preparations both at home and abroad all adopt the same formula at present, promptly added a kind of surfactant---polyoxyethyl castor oil (polyoxyethyl castor oil) in paclitaxel ethanol injection. CremophorEL). However, polyoxyethyl castor oil can promote the release of histamine, which often causes severe allergic reactions and produces adverse reactions such as hypersensitivity,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K9/14A61K47/36A61P35/00
Inventor 李芳朱怀仕沈鹤柏于永春马经纬李佳咛童晓文
Owner SHANGHAI TENTH PEOPLES HOSPITAL
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