Drug carrier, micelle, drug as well as preparation methods and application thereof

A carrier and drug technology, applied in the fields of drug carriers, micelles, medicaments and their preparation, can solve problems such as difficult to effectively control postoperative metastasis and recurrence process

Pending Publication Date: 2020-11-20
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the strategy of regulating the above factors at a single site is difficult

Method used

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  • Drug carrier, micelle, drug as well as preparation methods and application thereof
  • Drug carrier, micelle, drug as well as preparation methods and application thereof
  • Drug carrier, micelle, drug as well as preparation methods and application thereof

Examples

Experimental program
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Example Embodiment

[0091] Synthesis Example 1 low molecular weight heparin and hydrophobic carotenoid Copolymer

[0092] Object of the present embodiment is an exemplary embodiment of the method of synthesis of low molecular weight heparin and hydrophobic carotenoid copolymer, and characterization of low molecular weight heparin and a copolymer of a hydrophobic carotenoid FIG.

[0093] 1. Heparin and astaxanthin Eno copolymers prepared:

[0094] Accurately weighed astaxanthin 25.0mg, at room temperature, dissolved in 24.0mLN, N- dimethylformamide (DMF) in. Another accurately weighed low molecular weight heparin (heparin Eno) 50.0 mg, at heating at 60 ℃ was dissolved in 3.0mL formamide, was added 1- (3-dimethylaminopropyl) -3-ethylcarbodiimide carbodiimide hydrochloride (EDC) 60.0mg, N- hydroxysuccinimide (NHS) 36.0mg and 4-dimethylaminopyridine (DMAP) 10.0mg, 25 deg.] C in dark activated stirred 3h. After activation is completed in 2 drops / s (about 40μL / s) rate, stirring rate at 600rpm dropwise ...

Example Embodiment

[0099] Example 2 Structural Characterization of low molecular weight heparin and a hydrophobic carotenoid embodiments copolymer (copolymer in Example 1 Embodiment Example)

[0100] 1.LMWH-AST copolymer hydrogen spectra, respectively:

[0101] LMWH-AST 6.0mg sample powder after lyophilization taken, accurately weighed, were dissolved in 0.5mL of D2O and in DMSO-d6. LMWH were weighed and the AST 3.0mg 3.0mg respectively dissolved in D2O and 0.5mL 0.5mL of DMSO-d6 as reference sample. H NMR 400MHz performed in (1H-NMR) analysis.

[0102] Such as figure 2 Shown by comparison of LMWH and AST map, LMWH-AST in the sample in D2O micelles formed forward, atlas, δ 3.5-5.5ppm = a series of peaks between the peaks of the LMWH is hydrogen carbon chain backbone, [delta] = 6.5ppm peak of AST hydrogen on the carbon chain backbone. In summary, 1H-NMR results confirmed the successful synthesis of LANPs.

[0103] Infrared spectroscopy confirmed copolymer 2.LMWH-AST:

[0104] LMWH-AST structure of th...

Example Embodiment

[0112] Example 3 Synthesis of fondaparinux sodium and astaxanthin decanoic Copolymer

[0113] Accurately weighed astaxanthin 25.0mg, at room temperature, dissolved in 24.0mLN, N- dimethylformamide (DMF) in. Another accurately weighed 50.0 mg fondaparinux sodium decyl, at heating at 60 ℃ was dissolved in 3.0mL formamide, was added 1- (3-dimethylaminopropyl) -3-ethylcarbodiimide salt salt (EDC) 60.0mg, N- hydroxysuccinimide (NHS) 36.0mg and 4-dimethylaminopyridine (DMAP) 10.0mg, 25 deg.] C in dark activated stirred 3h. After activation is completed in 2 drops / s (about 40μL / s) rate, stirring rate at 600rpm dropwise added to the above solution astaxanthin, argon (Ar) at protection, 30 deg.] C the dark reaction was 48h. After completion of the reaction, the reaction solution was added 3 volumes of acetone 0 ℃, thoroughly shaken, 4000rpm, to centrifugation at normal temperature. After boiling 25mL was added after cooling After discarding the supernatant, the resulting precipitate wa...

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Abstract

The invention relates to the field of drug preparations, and discloses a drug carrier, a micelle, a drug as well as preparation methods and application thereof. The drug carrier and the micelle comprise: A) a hydrophilic part comprising a hydrophilic heparin compound; and B) a hydrophobic part comprising one of hydrophobic carotenoid and vitamin A compounds, wherein the hydrophilic part and the hydrophobic part are linked in a specific manner. The drug carrier and the micelle not only have functions of blocking activation of an NF-[kappa]B signal pathway and an STAT3 signal pathway in an initial step in an inflammation feedforward loop, inhibiting recruitment of myeloid-derived suppressor cells in tumor parts and remote organs, inhibiting implantation of tumor cells in the remote organs and improving local immunosuppression microenvironments so as to inhibit tumor related inflammations, premetastatic niche reconstruction, tumor cell immune escape and strangle circulating tumor cells, but also can realize the best tumor and tumor metastasis inhabitation effects by further entrapping an anti-tumor drug.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical carrier, micelles, medicaments and their preparation methods and applications. Background technique [0002] Cancer is a serious threat to the health of modern humans. According to statistics from the National Cancer Center, about 3.929 million people were diagnosed with cancer in 2015 in my country, with an average of 7.5 people diagnosed every minute, and the trend is increasing year by year. At present, the treatment methods for cancer mainly include chemical drug therapy (chemotherapy), tumor radiation therapy (radiotherapy) and surgical resection. Among them, although chemotherapy can directly kill tumor cells and has a certain degree of tumor inhibition, it has a large toxic side effect and a single mechanism of action, so the therapeutic effect needs to be further improved. Therefore, if tumors can be inhibited from different mechanisms during c...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K9/107A61K31/704A61P35/00A61P35/04
CPCA61K47/36A61K9/1075A61K31/704A61P35/00A61P35/04Y02A50/30
Inventor 何勤卢正则龙洋李曼
Owner SICHUAN UNIV
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