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Composition, preparation method and application of cisplatin microparticles

A technology of microparticles and cisplatin, applied in the field of microparticle composition and preparation, can solve the problems of poor tumor curative effect, etc., achieve high drug loading, good biocompatibility, protein shielding effect, and good blocking effect of macrophage phagocytosis.

Active Publication Date: 2022-07-01
SHANDONG HUBBLE KISEN BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Kataoka and colleagues reported that particles larger than 30 nm have poor efficacy on poorly permeable tumors (Nat Nanotechnol, 2011), and Jain et al. also confirmed that nanoformulations with a particle size of 12 nm have better penetration on poorly permeable tumors Sex (Nat Nanotechnol, 2012)

Method used

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  • Composition, preparation method and application of cisplatin microparticles
  • Composition, preparation method and application of cisplatin microparticles
  • Composition, preparation method and application of cisplatin microparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] MPEG 2000 -P(GluNa) 2000 About 38.85mg, silver nitrate 48mg, put in a 100m round-bottom flask, add 30ml of distilled water, and shake in a water bath at 40°C for 10 hours; centrifuge to remove the supernatant, collect the precipitate, and then disperse the precipitate with 30ml of purified water, add cisplatin 45 mg of raw material was placed in a water bath at 40 °C for 96 hours of shaking reaction; after the precipitate was completely dissolved, the solution was taken and centrifuged with 10KDa ultrafiltration, and concentrated.

Embodiment 2

[0034] Weigh 45 mg of cisplatin raw material, 48 mg of silver nitrate, add 30 ml of distilled water, and shake in a water bath at 37 °C for 4 hours; centrifuge to take the supernatant, and then add MPEG 2000 -P(GluNa) 2000 About 38.85mg, placed in a round-bottomed flask, shaken to dissolve, and placed in a 37°C water bath for 72 hours of reaction; then 10KDa ultrafiltration centrifugation, concentrated, washed the concentrated solution for several times, combined the concentrated liquid, and passed 0.22μm Filtered and lyophilized.

Embodiment 3

[0036] Weigh 149 mg of cisplatin raw material, 161.5 mg of silver nitrate, MPEG 2000 -P(GluNa)2000 298mg was placed in a 100m round-bottom flask, 50ml of distilled water was added, and the reaction was shaken in a water bath at 37°C for 4 to 10 hours; filtered to remove silver chloride, and the 10KDa filtrate was collected by ultrafiltration and centrifugation for concentration; the concentrated liquid was packaged and lyophilized.

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Abstract

The invention relates to the composition and preparation method of a cisplatin microparticle system with lower cost, higher cisplatin drug loading amount and the effect of shielding macrophage phagocytosis. methoxypolyethylene glycol 2000 ‑Sodium polyglutamate copolymer (MPEG 2000 ‑P(GluNa) 2000 ) as the carrier and cisplatin. Under the conditions of the preparation method required by the patent, the prepared cisplatin nanoparticles have a higher drug loading capacity, and can better shield the phagocytosis of macrophages during the blood circulation process in the body, and have better tumor tissue distribution.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a composition and preparation method of microparticles with lower cost, higher drug loading of cisplatin and the effect of shielding macrophage phagocytosis. Background technique [0002] Cisplatin (cis-dichlorodiammine platinum, CISP) is the first metal complex with anticancer activity discovered by American scientists Rosenborg et al. Cisplatin, as a broad-spectrum anticancer drug, has the characteristics of precise curative effect and high anticancer activity in many cancers, such as breast cancer, ovarian cancer, cervical cancer, esophageal cancer, non-small cell lung cancer and gastric cancer. However, its severe nephrotoxicity, auditory attenuation and other toxic side effects limit the wide clinical application of cisplatin and its platinum compounds. The clearance threshold of the human kidneys for the particle size of foreign bodies is around 5.5nm, and part...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/60A61K33/243A61P35/00
CPCA61K47/6935A61K47/60A61K33/243A61P35/00
Inventor 王成张震李军王维剑牛冲董朋伟
Owner SHANDONG HUBBLE KISEN BIOLOGICAL TECH CO LTD
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