Preparation method and application of paclitaxel albumin nanoparticles

A technology of albumin nanoparticles and paclitaxel, which is applied in the field of biomedical preparations, can solve the problems of consumption of yew trees, limited extraction of paclitaxel, low solubility of paclitaxel, etc., and achieves improved drug solubility, reduced toxicity or immune response, organic Reagent volume without residue effect

Inactive Publication Date: 2018-09-14
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The semi-synthetic method can maximize the utilization of plant resources, but it is not fundamentally different from the method of directly extracting paclitaxel. It needs to consume a large amount of yew trees, and still cannot fundamentally solve the problem of scarcity of plant sources.
Apparently the extraction of paclitaxel from yew plant tissue is extremely limited
While paclitaxel raw material drug resources are tight, paclitaxel has low solubility in water and poor biocompatibility, making its bioavailability low

Method used

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  • Preparation method and application of paclitaxel albumin nanoparticles
  • Preparation method and application of paclitaxel albumin nanoparticles
  • Preparation method and application of paclitaxel albumin nanoparticles

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preparation example Construction

[0034] A preparation method of paclitaxel albumin nanoparticles, comprising the steps of:

[0035] 1) Weigh 50 mg of paclitaxel raw material, dissolve it in 1 mL of organic solvent, and sonicate for 30 min to obtain an oil phase. The organic solvent is dichloromethane, or acetone, or a mixture of dichloromethane and acetone (v:v=1:1).

[0036] 2) Weigh bovine serum albumin and dissolve it in water, stir and heat to make it fully dissolved to obtain a bovine serum albumin aqueous solution with a mass volume percentage of 5% (m / v), and add 1mol / L hydrochloric acid dropwise to adjust the albumin aqueous solution pH to 6.0, adding 1% organic solvent to the total volume of the bovine serum albumin aqueous solution, pre-saturation, to obtain the aqueous phase. The organic solvent is dichloromethane, or acetone, or a mixture of dichloromethane and acetone (v:v=1:1).

[0037] 3) Under the action of high-speed shear (rotating speed 10000r), add the oil phase to the water phase drop b...

Embodiment 1

[0040] (1) Orthogonal experiment design

[0041] It can be known from experiments that the type of organic solvent (A), the volume ratio of the oil phase to the water phase (B), and the number of homogenizations (C) are the key factors affecting the particle size of the nanoparticles.

[0042] Type A of organic solvent: 1. Dichloromethane; 2. Acetone; 3. Dichloromethane-acetone (v:v=1:1);

[0043] Volume ratio B of oil phase and water phase: 1, 1:4; 2, 1:7; 3, 1:10;

[0044] Homogenization times C: 1, 5 times; 2, 10 times; 3, 15 times, the experimental design is shown in Table 1:

[0045] Table 1 Orthogonal experiment design table

[0046]

[0047]

[0048] Table 2 Orthogonal test results

[0049]

[0050] Orthogonal design analysis form is shown in Table 2, K in the table 1 、K 2 、K 3 R is the average value of the experimental results (particle size) under the three levels of the corresponding factor, and the R value is the range of each factor, that is, the dif...

Embodiment 2

[0063] (1) a preparation method of paclitaxel albumin nanoparticles, comprising the steps of:

[0064] 1) Weigh 50 mg of the paclitaxel raw material, dissolve it in 1 mL of acetone, and sonicate for 30 min to obtain an oil phase.

[0065] 2) Weigh bovine serum albumin and dissolve it in water, stir and heat to make it fully dissolved to obtain a bovine serum albumin aqueous solution with a mass volume percentage of 5% (m / v), and add 1mol / L hydrochloric acid dropwise to adjust the albumin aqueous solution To bring the pH to 6.0, add 1% acetone to the total volume of the bovine serum albumin solution.

[0066] 3) Under the action of high-speed shear (rotating speed 10000r), add the oil phase to the water phase drop by drop to make an oil-in-water emulsion. By volume, oil phase: water phase = 1:10.

[0067] 4) Transfer the oil-in-water emulsion to a high-pressure micro-fluidic nanodisperser for high-pressure homogenization, the homogenization pressure is 1000 bar, and the homog...

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Abstract

The invention relates to a preparation method and application of paclitaxel albumin nanoparticles and belongs to the field of medicinal preparations. The preparation method includes: weighing paclitaxel active pharmaceutical ingredient, and dissolving in a proper amount of organic solvent to obtain an oil phase; weighing albumin, dissolving in water, stirring, heating to enable the albumin to be fully dissolved to obtain an albumin water solution, adjusting pH of the albumin water solution to 6.0, and adding the organic solvent to obtain an aqueous phase; under action of high-speed shearing, dropwise adding the oil phase into the aqueous phase to obtain an oil-in-water emulsion; transferring the oil-in-water emulsion into a high-pressure microjet nano dispersing instrument for high-pressure homogenizing, and removing the organic solvent from a system after homogenizing is completed through rotary evaporation to obtain a water solution of the paclitaxel albumin nanoparticles. Particle size of the paclitaxel albumin nanoparticles can be controlled by changing proportion of the oil phase and is 100-200nm. The preparation method is simple, controllable and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of biomedical preparations, in particular to the preparation and application of paclitaxel albumin nanoparticles. Background technique [0002] Paclitaxel is a natural secondary metabolite isolated and purified from the bark of the gymnosperm Taxus chinensis. It has been clinically proven to have good anti-tumor effects, especially for ovarian cancer, uterine cancer and breast cancer, which have a high incidence of cancer Wait for special effects. Paclitaxel is the most popular anticancer drug on the international market in recent years, and is considered to be one of the most effective anticancer drugs for humans in the next 20 years. Now the semi-synthetic method of paclitaxel is relatively mature, and it is considered to be an effective way to expand the source of paclitaxel besides artificial planting. The semi-synthetic method can maximize the utilization of plant resources, but it is not fundamentally differen...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/51A61K31/337A61K47/42A61K47/64A61P35/00
CPCA61K31/337A61K9/146A61K9/5169A61K47/643A61P35/00
Inventor 陈立江马徵薇王朝勃张金凤
Owner LIAONING UNIVERSITY
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