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A kind of hydrophobic drug nanoparticle, its preparation method and application

A technology of nanoparticles and drug molecules, applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of low bioavailability and low drug loading in nano drug-loading systems, and achieve long cycle time and high bioavailability Improvement, the effect of small particle size

Active Publication Date: 2016-06-08
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to overcome the problems of low bioavailability of anti-tumor hydrophobic drug molecules and low drug loading capacity of nano-drug loading systems, the invention provides a hydrophobic drug nanoparticle and a preparation method thereof. The hydrophobic drug nanoparticle has biological With the characteristics of high utilization and high drug loading, the method is simple to operate, has a wide range of applications and strong universality

Method used

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  • A kind of hydrophobic drug nanoparticle, its preparation method and application
  • A kind of hydrophobic drug nanoparticle, its preparation method and application
  • A kind of hydrophobic drug nanoparticle, its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Embodiment 1: the preparation of curcumin nanoparticles

[0046] The chemical name of the curcumin drug molecule used in this embodiment is (1E,6E)-1,7-bis(4-hydroxyl-3-methoxyphenyl)-1,6-heptadiene-3,5- Diketone, its structural formula is as follows:

[0047]

[0048] Prepare 10 mL of curcumin drug molecule-acetone solution with a concentration of 1.5 mM, add 200 μL of the curcumin drug molecule solution into 4 mL of deionized water, stir magnetically at 25° C. for 5 min, and then let stand to obtain a precursor nanoparticle suspoemulsion.

[0049] Polymaleic anhydride 18 carbene-polyethylene glycol was prepared as a 5 mg / mL aqueous solution.

[0050] Add 300 μL of 5 mg / mL polymaleic anhydride 18 carbene-polyethylene glycol aqueous solution into the precursor nanoparticle suspoemulsion, ultrasonically disperse for 5 minutes, and let stand for 6 hours to prepare water-dispersed hydrophobic curcumin nanoparticles. .

Embodiment 2

[0051] Embodiment 2: Preparation of docetaxel nanoparticles

[0052] The chemical name of the docetaxel drug molecule used in this example is 2aR-(2aα, 4β, 4aβ, 6β, 9α, (αR′, βS′), 11α, 12α, 12aα, 12bα)-β-1,1 -Dimethylethoxycarbonylamino-α-carbonylphenylpropanoic acid 12b-Acetoxy-12-benzoyloxy-2a,3,4,4a,5,6,9,10,11,12,12a, 12b-Dodecahydro-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methylene-1H-cyclodecapenta-3,4 Benzo 1,2-b oxetan-9-yl ester, its structural formula is as follows:

[0053]

[0054] Prepare 10 mL of docetaxel drug molecule-acetone solution with a concentration of 2.0 mM, take 300 μL of the docetaxel drug molecule solution and add it to 8 mL of deionized water, stir magnetically at 25 °C for 5 min, and then let stand to obtain the suspension of precursor nanoparticles. lotion.

[0055] Polymaleic anhydride 18 carbene-polyethylene glycol was prepared as a 1 mg / mL aqueous solution.

[0056] Add 800 μL of 1 mg / mL polymaleic anhydride 18 carbene-polye...

Embodiment 3

[0057] Embodiment 3: Preparation of 10-hydroxycamptothecin nanoparticles

[0058] The chemical name of the 10-hydroxycamptothecin drug molecule used in this example is 4-ethyl-4,10-dihydroxy-1H-pyrano[3',4':6,7]indole[1,2 -b] quinoline-3,14(4H,12H)-dione, its structural formula is as follows:

[0059]

[0060] Prepare 5 mL of 10-hydroxycamptothecin drug molecule-ethanol solution with a concentration of 1.0 mM, take 200 μL of the 10-hydroxycamptothecin drug molecule solution and add it to 3 mL of deionized water, stir magnetically at 25 ° C for 5 min and let stand to obtain Precursor nanoparticle suspoemulsion.

[0061] Polymaleic anhydride 18 carbene-polyethylene glycol was prepared as a 5 mg / mL aqueous solution.

[0062] Add 300 μL of 5 mg / mL polymaleic anhydride 18 carbene-polyethylene glycol aqueous solution into the precursor nanoparticle suspoemulsion, ultrasonically disperse for 5 minutes, and let it stand for 6 hours to prepare a water-phase dispersed hydrophobic 1...

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Abstract

The invention discloses a hydrophobic drug nanoparticle, its preparation method and application. The hydrophobic drug nanoparticle is spherical or approximately spherical, and the hydrophobic drug nanoparticle is prepared from hydrophobic drug molecules through a solvent exchange method. Precursor nanoparticle suspoemulsion, adding amphiphilic surfactant aqueous solution to the precursor nanoparticle suspoemulsion, and ultrasonically treating the obtained nanoparticles coated with amphiphilic surfactant. The hydrophobic drug nanoparticle has the characteristics of high bioavailability and high drug loading capacity, and the method is simple to operate, has a wide application range and strong universality. The invention can be applied to the fields of biomedicine and pharmaceutical preparations.

Description

technical field [0001] The invention relates to the technical field of nanoparticle drug preparations, in particular to a hydrophobic drug nanoparticle, its preparation method and application. Background technique [0002] Hydrophobic organic small molecule drugs still occupy a pivotal position in tumor treatment, but their insoluble problems lead to a series of problems such as the decrease of drug bioavailability, which greatly hinders their clinical application. The current micro-nano drug carriers have improved the bioavailability of hydrophobic drugs to a certain extent, but the biocompatibility and cytotoxicity brought by the carrier itself have attracted widespread attention, which has become a thorny problem that hinders the further clinical application of micro-nano carriers. question. Therefore, how to improve the bioavailability of hydrophobic drugs while increasing drug loading has become a major challenge in tumor treatment. It is urgent to develop a nano-prepa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K9/10A61K47/34A61P35/00
Inventor 梁兴杰张晓宏李盛亮张金凤曹伟鹏李峰
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA