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A preparation method of star-shaped drug delivery nanoparticles with enzyme targeting

A nanoparticle and targeted technology, which is applied in the field of preparation of star-shaped drug delivery nanoparticles, can solve the problem that drug selectivity cannot be guaranteed.

Active Publication Date: 2020-06-30
ZHEJIANG UNIV OF TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, passive drug delivery systems do not guarantee good drug selectivity due to multidrug resistance

Method used

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  • A preparation method of star-shaped drug delivery nanoparticles with enzyme targeting
  • A preparation method of star-shaped drug delivery nanoparticles with enzyme targeting
  • A preparation method of star-shaped drug delivery nanoparticles with enzyme targeting

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Put 1,2,3-propanetricarboxylic acid (0.1765g, 1mmol), ε-caprolactone (3.4245g, 30mmol) and stannous octoate (120μL, 0.37mmol) into a 50mL three-necked flask, N 2 Under protection, the reaction was carried out at 120°C for 24 hours. The product was dissolved in 10ml of DCM and slowly dropped into glacial ether (1:15) to precipitate. The obtained precipitate was filtered and dried in vacuum at 25°C for 24h to obtain 1.4343g of Tri-CL.

[0071] Dissolve Tri-CL (1.0530 g, 0.1 mmol) in 10 mL of toluene, and add N-(tert-butoxycarbonyl)ethanolamine (0.0645 g, 0.4 mmol). Under the protection of nitrogen, add triethylamine (94μL, 0.68mmol), seal it, and react at 40°C for 48h. The reaction solution is added dropwise to 200mL ice methanol, centrifuged at 6000r / min for 30min, and the supernatant is removed. After vacuum drying at ℃ for 24 hours, 0.7542 g of Tri-CL-NHBoc was obtained.

[0072] Tri-CL-NHBoc (0.6576g, 0.06mmol) was dissolved in 10mL of dichloromethane, TFA (0.0274g, ...

Embodiment 2

[0079] Investigating the Effect of Surfactants on the Granulation of Nanoparticles

[0080] Dilute 6mg of curcumin to 10mL with acetone, and prepare a 0.6mg / mL curcumin acetone solution, take 24mg of the prepared MePEG-Peptide-Tri-CL and dissolve it in 2mL curcumin acetone solution to form a lipid phase; P-188, PVA, Tween-80 and sodium dodecylsulfonate were dissolved in 100mL water to form a water phase, and the obtained lipid phase was added dropwise to the high-speed stirring water phase, and stirred for 0.5h after the addition was completed , evacuated for 1 hour, removed acetone, and centrifuged at 6000 r / min for 20 minutes, the supernatant obtained was the curcumin-loaded star nanoparticle solution.

[0081] The effect of surfactant types on the granulation of nanoparticles is shown in Table 1.

[0082] Table 1 Effect of surfactant types on the granulation of nanoparticles

[0083]

[0084] P-188 is preferred.

Embodiment 3

[0086] To investigate the effect of curcumin concentration on the granulation of nanoparticles

[0087] 6mg, 8mg, 10mg, 12mg, 14mg and 16mg of curcumin were fixed to 10mL with acetone respectively, and prepared into 0.6mg / mL, 0.8mg / mL, 1.0mg / mL, 1.2mg / mL, 1.4mg / mL and 1.6 mg / mL curcumin acetone solution, respectively take six prepared MePEG-Peptide-Tri-CL 24mg and dissolve in 2mL curcumin acetone solution to form a lipid phase; respectively dissolve 500mg P-188 in 250mL water to form a water phase , add the obtained fat phase dropwise to the water phase stirred at high speed, stir for 0.5h after the dropwise addition, vacuumize for 1h, remove acetone, and centrifuge at 6000r / min for 20min, the obtained supernatant is the curcumin-loaded star nanoparticle solution.

[0088] Table 2 Effect of curcumin concentration on the granulation of nanoparticles

[0089]

[0090] The preferred range of curcumin concentration is 0.8-1.2 mg / mL.

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Abstract

The invention relates to a preparation method of star shaped drug administration nanoparticles having enzyme targeting property, wherein the preparation method comprises the following steps: a first step, preparation of MPEG-Peptide-Tri-CL; and a second step, preparation of the nanoparticles: with curcumin as a model drug, dissolving the MPEG-Peptide-Tri-CL and curcumin in acetone to be used as alipid phase solution, dissolving a surfactant in water to be used as an aqueous phase, slowly dropwise adding the lipid phase into the aqueous phase according to different lipid phase / aqueous phase ratios, and continuously stirring, to form a curcumin-loaded-star shaped nanoparticle original solution; and carrying out vacuum suction filtration of the prepared nanoparticle solution for 1 h to remove an organic solvent, and centrifuging for 20 min at the speed of 6000 r / min, to obtain a solution namely a nanoparticle solution. The solubility of curcumin in water is improved, at the same time, the star shaped drug administration nanoparticles have the sustained or controlled release and targeting characteristics in the anti-tumor treatment process, and is suitable for intravenous injection, oral administration and other drug administration modes.

Description

Technical field: [0001] The invention relates to the technical field of preparation of pharmaceutical polymer carriers and pharmaceutical nano-preparations, in particular to a preparation method of star-shaped drug delivery nanoparticles with enzyme targeting. Background technique: [0002] Degradable bio-targeting nanomaterials have good biocompatibility and are often used as effective carriers of hydrophobic anticancer drugs, but the problem of low drug loading often limits the further development of amphiphilic polymer drug-loading systems . Recent studies have shown that compared with linear polymers, star polymers have more reactive functional groups and can form a wider loading cavity, which is conducive to the optimization of nanocarriers and the improvement of drug loading. Nanocarriers increase drug accumulation in tumor sites by improving drug penetration and retention. However, passive drug delivery systems cannot guarantee good drug selectivity due to multi-dru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/42A61K47/10A61K31/12A61P35/00
CPCA61K9/0002A61K9/5146A61K9/5169A61K31/12
Inventor 郭钫元杨根生吴文超吴江青黄冬雪张逸菲
Owner ZHEJIANG UNIV OF TECH
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