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Docetaxel polydroxybutyrate nanoparticle, manufacturing method and pisum sativum agglutinin modification method and application

A paclitaxel polyhydroxybutyrate, polyhydroxybutyrate technology, applied in the field of medicine, can solve the problems of low solubility and poor targeting of paclitaxel

Active Publication Date: 2013-12-18
上海市第八人民医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the defects of low solubility and poor targeting of docetaxel in the prior art, and provide docetaxel-loaded polyhydroxybutyrate nanoparticles and pea lectin-loaded docetaxel Polyhydroxybutyrate nanoparticles and their preparation method and application

Method used

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  • Docetaxel polydroxybutyrate nanoparticle, manufacturing method and pisum sativum agglutinin modification method and application
  • Docetaxel polydroxybutyrate nanoparticle, manufacturing method and pisum sativum agglutinin modification method and application
  • Docetaxel polydroxybutyrate nanoparticle, manufacturing method and pisum sativum agglutinin modification method and application

Examples

Experimental program
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Embodiment 1

[0067] Preparation method of docetaxel-loaded polyhydroxybutyrate nanoparticles. The instruments used in Example 1 are shown in Table 1.

[0068] The instrument used in Table 1 Example 1 and its purchaser and model

[0069] operate

instrument

buy manufacturers

Magnetic stirring

S10-3 constant temperature magnetic stirrer

Shanghai Silo Instrument Co., Ltd.

Sonication

VCX130 Probe Type Ultrasonic Crusher

Sonics&materials, USA

centrifugal

RJ-TGL-16G desktop high-speed centrifuge

Wuxi Ruijiang Analytical Instrument Co., Ltd.

Sample weighing

AL204 electronic balance

METTLER TOLEDO, Switzerland

heat reflux

DK-8D type electric heating constant temperature water tank

Shanghai Jinghong Experimental Equipment Co., Ltd.

[0070] Its preparation process steps and conditions are:

[0071] (1) Mix 1.6 mg of docetaxel and 0.4 mL of poly[(R)-3-hydroxybutyric acid] in chloroform to obtain a mi...

Embodiment 2

[0075] Preparation method of docetaxel-loaded polyhydroxybutyrate nanoparticles. The instrument used in embodiment 2 is with embodiment 1; Its preparation process step and condition are:

[0076] (1) Mix docetaxel and poly[(R)-3-hydroxybutyric acid] in chloroform to obtain a mixed solution; the poly[(R)-3-hydroxybutyric acid] in chloroform The concentration of the solution is 0.02g / mL;

[0077](2) ultrasonically treat the aqueous solution of polyvinyl alcohol for 1 min, and add the mixed solution described in step (1) dropwise to the aqueous solution of polyvinyl alcohol under stirring conditions; the stirring speed is 1000rpm, The concentration of the aqueous solution of polyvinyl alcohol (PVA) is 0.005g / mL;

[0078] (3) Ultrasonic emulsification under ice bath conditions for 5 minutes, the amplitude of ultrasonic emulsification is 40%, the pulse is 5s\5s, magnetic stirring is solidified, the stirring speed is 500rpm, the stirring time is 6h, and the organic solvent is vola...

Embodiment 3

[0081] Preparation method of docetaxel-loaded polyhydroxybutyrate nanoparticles. The instrument used in embodiment 3 is with embodiment 1; Its preparation process step and condition are:

[0082] (1) Vortex and mix docetaxel and 0.005 g / mL polyhydroxybutyrate in chloroform to obtain a mixed solution; wherein, the preparation method of polyhydroxybutyrate in chloroform For: mix polyhydroxybutyrate and chloroform solution, heat in a water bath at 70°C, condense for 4 hours, and filter through No. 3 sand core suction filter funnel (the leak size is 35mL-3#);

[0083] (2) Use VCX130 probe-type ultrasonic breaker to ultrasonically treat the aqueous solution of polyvinyl alcohol to make it evenly dispersed; the ultrasonic treatment time is 2min, the amplitude is 40%, and the pulse is 5s\5s;

[0084] Mix the mixed solution with 0.01 g / mL of the above-mentioned polyvinyl alcohol aqueous solution; add the mixed solution dropwise to the above-mentioned aqueous solution of polyvinyl alc...

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Abstract

The invention discloses a docetaxel polydroxybutyrate nanoparticle, a manufacturing method and apisum sativum agglutinin modification method and application. The manufacturing method of the docetaxel polydroxybutyrate nanoparticle includes the steps that docetaxel and thichloromethane and / or dichloromethane of polyhydroxybutyrate are uniformly mixed and then mixed with an aqueous solution of polyvinyl alcohol, then ultrasonic emulsification is carried out for 3-10 min, curing is carried out, and organic solvents are removed; the mass ratio of the docetaxel to the polyhydroxybutyrate to the polyvinyl alcohol is (0.8-2): (4-10): (20-50). The solubility of the docetaxel is improved, distribution of particle sizes of manufactured products is even, the quantity of carried drugs is large, the packing rate is high, drug release is quick, drugs are released in a controlled mode out of the body, and the bioavailability is high. The docetaxel polydroxybutyrate nanoparticle undergoing apisum sativum agglutinin modification improves drug targeting performance and treatment indexes, and lays a foundation for development of a tumor targeting drug delivery system mediated by specific sugar.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to docetaxel-loaded polyhydroxybutyrate nanoparticles and pea agglutinin-loaded docetaxel-loaded polyhydroxybutyrate nanoparticles, as well as their preparation methods and applications. Background technique [0002] Docetaxel (DTX) is a new type of taxane anti-tumor drug, which blocks cell mitosis by inhibiting tubulin depolymerization, thereby inhibiting the proliferation of tumor cells and exerting anti-tumor activity. Clinical studies have confirmed that docetaxel has good curative effects on breast cancer, ovarian cancer, lung cancer, head and neck cancer, and gastric cancer, and is a first-line drug for ovarian cancer. [0003] However, the water solubility of docetaxel is extremely low, and the bioavailability of oral administration is almost zero. Its injection is now used clinically. Severe adverse reactions will occur after taking the medicine, and at the same time, it i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/337A61K47/42A61K47/34A61P35/00
Inventor 李凤前董文凤李菲杜丽
Owner 上海市第八人民医院
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