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
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[0034] A preparation method of paclitaxel albumin nanoparticles includes the following steps:
[0035] 1) Weigh 50 mg of paclitaxel bulk drug, dissolve it in 1 mL of organic solvent, and sonicate for 30 minutes 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 fully dissolve it to obtain a bovine serum albumin aqueous solution with a mass volume percentage of 5% (m / v), and add 1mol / L hydrochloric acid to adjust the albumin aqueous solution. When the pH reaches 6.0, 1% of the total volume of the bovine serum albumin aqueous solution is added with an organic solvent to pre-saturate to obtain an 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 (rotational speed 10000r), the oil phase is added dropwise to ...
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[0039] Example 1
[0040] (1) Design of orthogonal experiment
[0041] Through experiments, it can be known that the type of organic solvent (A), the volume ratio of the oil phase to the water phase (B), and the number of homogenization (C) are the key factors influencing the particle size of the nanoparticles.
[0042] Type A of organic solvent: 1. Dichloromethane; 2. Acetone; 3. Dichloromethane-acetone (v:v=1:1);
[0043] The volume ratio of oil phase to water phase B: 1, 1:4; 2, 1:7; 3, 1:10;
[0044] The number of homogenization C: 1, 5 times; 2, 10 times; 3, 15 times, the experimental design is shown in Table 1:
[0045] Table 1 Orthogonal test design table
[0046]
[0047]
[0048] Table 2 Orthogonal test results
[0049]
[0050] Orthogonal design analysis table is shown in Table 2, in the table K 1 , K 2 , K 3 It is the average value of the experimental results (particle size) under the three levels of the corresponding factors, and the R value is the extreme difference of each fa...
Example Embodiment
[0062] Example 2
[0063] (1) A method for preparing paclitaxel albumin nanoparticles, including the following steps:
[0064] 1) Weigh 50 mg of paclitaxel bulk drug, dissolve it in 1 mL of acetone, and sonicate for 30 minutes to obtain an oil phase.
[0065] 2) Weigh bovine serum albumin and dissolve it in water, stir and heat to fully dissolve it to obtain an aqueous solution of bovine serum albumin with a mass volume percentage of 5% (m / v), and add 1mol / L hydrochloric acid to adjust the albumin aqueous solution. PH to 6.0, add 1% acetone of the total volume of the bovine serum albumin aqueous solution.
[0066] 3) Under the action of high-speed shear (rotating speed 10000r), the oil phase is added dropwise to the water phase to make an oil-in-water emulsion. According to the volume ratio, oil phase: water phase=1:10.
[0067] 4) Transfer the oil-in-water emulsion to a high-pressure micro-jet nano-disperser for high-pressure homogenization, the homogenization pressure is 1000 bar, a...
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