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Sorafenib nano particle and application thereof

A sorafenib nanometer and nanoparticle technology, applied in the direction of non-active ingredient medical preparations, powder delivery, antineoplastic drugs, etc., can solve intestinal, systemic or skin lesions, diarrhea, weight loss, hand- Foot skin reaction and other problems to achieve the effect of avoiding excessive drug release, good ball formation, and avoiding drug side effects

Inactive Publication Date: 2013-08-28
SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, sorafenib directly inhibits VEGFR-2, 3 and PDGFR-β by blocking the RAF-MEK-ERK pathway signal transmission. While inhibiting the proliferation of tumor cells, it also affects other cells in the body. There are drugs in the clinical application process. Treatment-related adverse events, with an overall incidence rate of 80%, were mainly grade 1 or 2, mainly gastrointestinal, systemic or skin lesions, diarrhea, weight loss, hand-foot skin reactions, hair loss, decreased appetite, and voice changes Wait

Method used

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  • Sorafenib nano particle and application thereof
  • Sorafenib nano particle and application thereof
  • Sorafenib nano particle and application thereof

Examples

Experimental program
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Embodiment 1

[0042] The preparation of embodiment 1 mPEG-PDLLA

[0043] First, put polyethylene glycol monomethyl ether (Methoxypolyethylene glycols, mPEG for short) into the schlenk tube, and remove water under vacuum in the molten state; then add the previously refined racemic lactide (DLLA) and the catalyst stannous octoate The reaction tube was evacuated repeatedly, nitrogen was ventilated, and finally the tube was vacuum-sealed and placed in an oil bath at 140°C for 10 h. After the reaction, the product was dissolved with dichloromethane, then precipitated in cold ether, and the target product was obtained after vacuum drying. Among them, the polymer material (mPEG-PDLLA) is a polyethylene glycol monomethyl ether and racemic lactide copolymerized at a weight ratio of 1:1.1~2 (preferably 1.5:2.5). Methyl ether-polylactic acid block copolymer; its general formula is mPEG-PDLLA, its molecular weight range is 40-45kD, and its reaction route is as follows:

[0044]

[0045] Wherein, t...

Embodiment 2

[0046] Example 2 Preparation method of polyethylene glycol monomethyl ether-polylactic acid block copolymer Sorafenib nanoparticles

[0047] The raw material formula is as follows:

[0048] Tetrahydrofuran (C 4 h 8 O) 12ml

[0049] Polymer material (mPEG-PDLLA) 0.25g

[0050] Sorafenib 12.5mg

[0051] Methanol (CH 3 OH) 6ml

[0052] Make 18ml Sorafenib Nanoemulsion

[0053] Stir the above mixture to form a clear and transparent solution, then vacuum rotary evaporate at 60°C, remove the organic solvent, add 50 mL of distilled water at 60°C, rotate at normal pressure for 10 minutes, centrifuge for 10 minutes (4000 r / min), Get the supernatant and be the required Sorafenib nanoparticle solution, 60 Co irradiated and sterilized, and stored in a 4°C refrigerator for later use.

[0054] The detection results of Sorafenib nanoparticles show that the particle size is uniform and the shape is round, such as Figure 1a , Figure 1b As shown, the particle size is 127.3±2.0 nm,...

Embodiment 3

[0055] Example 3 In vitro drug release test of polyethylene glycol monomethyl ether-polylactic acid block copolymer sorafenib nanoparticles

[0056] Prepare a solution of phosphate buffered saline (PBS) (pH7.4, 0.01M) of sorafenib drug-loaded nanoparticles with a concentration of 0.5 wt%, then measure 5 ml and put it into a dialysis bag (molecular weight cut-off 3500). Put the dialysis bag into a 50 ml volumetric flask, add 35 ml of PBS, seal it and place it in a constant temperature air bath shaker (37°C, 75 rpm). At 2, 4, 8, 16, 24, 48, 72, 96, 120, 144, and 168 hours after the release, 20 ml of the release solution was sampled, and an equal amount of fresh PBS solution was added. The UV absorption value of the sample was measured at a wavelength of 263nm, and the concentration and cumulative release percentage of Sorafenib in the release medium were calculated.

[0057] In addition, a sorafenib PBS solution with a concentration of 0.5 wt% was prepared, 5.0ml of the solutio...

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Abstract

The invention relates to a sorafenib nano particle and an application thereof. The nano particle is a dual-target nano medicine made by taking sorafenib as an active ingredient and methoxy polyethylene glycol-poly (lactic acid) block copolymer as a medicine coating auxiliary material. The preparation method of the sorafenib nano particle has the advantages of simple process, high encapsulation efficiency, stable medicine release and good spheronization and can be used for preparing an anti-tumour targeted medicine; the sorafenib nano particle medicine can be used for anti-hepatoma targeted therapy, a methoxy polyethylene glycol-poly (lactic acid) block copolymer nano carrier can promote aggregation of sorafenib on hepatoma carcinoma cells after peripheral vein administration, so that the medicine is slowly released in a local part, action time of the medicine on the tumour cells is prolonged, local medicine concentration is improved, and toxic and side effects of sorafenib on the whole body are reduced; and the sorafenib nano particle medicine has the advantages of accurate target on tumour tissues and cell level, stable medicine aggregation and release, good anti-cancer effect and safety.

Description

technical field [0001] The present invention relates to a Sorafenib nanoparticle and its use, in particular to a liver cancer-specific targeted therapy drug—polyethylene glycol monomethyl ether-racemic polylactic acid block copolymer Sorafenib nanoparticles. Background technique [0002] Sorafenib is a silk, threonine protein kinase (RAF) and tyrosine kinase inhibitor, molecular formula: C28H24ClF3N4O6S, molecular weight: 637.0266, and its chemical structure is as follows: [0003] [0004] The Sorafenib is a weakly alkaline synthetic preparation with poor water solubility. As a new type of multi-target anti-tumor drug, it has dual anti-tumor effects, not only by inhibiting Raf kinase / mitogen extracellular kinase / extracellular regulatory protein Kinase (RAF / MEK / ERK) signaling pathway directly inhibits tumor growth, and blocks tumor angiogenesis by inhibiting vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR), and indir...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/44A61K47/34A61P35/00
Inventor 秦建民盛霞殷佩浩李琦黄涛撒忠秋杨林张敏
Owner SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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