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Erlotinib-Cy7-chitosan polymer with tumor targeting

A chitosan polymer and tumor-targeting technology, applied in the field of biomedicine, can solve the problem of incompatibility, achieve the effects of overcoming poor solubility, improving therapeutic effect, and reducing drug dosage and cost

Inactive Publication Date: 2017-06-13
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are strong hydrogen bonds between chitosan molecules and molecules, and it is incompatible with water and common organic solvents.

Method used

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  • Erlotinib-Cy7-chitosan polymer with tumor targeting
  • Erlotinib-Cy7-chitosan polymer with tumor targeting
  • Erlotinib-Cy7-chitosan polymer with tumor targeting

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Synthesis of Erlotinib-Cy7-Chitosan Polymer (CE7):

[0040] Step a: Weigh 200 mg of chitosan Cs (chitosan was purchased from Shanghai Boao Biotechnology Co., Ltd., with a molecular weight of 60 kilodaltons and a deacetylation degree of 90%) and dissolve it in 20 mL of anhydrous DMF, and then Add 800 mg of 4-bromophthalic anhydride, nitrogen protection, and heat with stirring in an oil bath at 125°C. When the reaction solution became clear and the solution was yellow, the reaction was terminated. Filter while hot, then directly pour the hot filtrate into 200mL ice water, and a white solid is precipitated. Suction filtration, the solid was washed three times with ether and acetone respectively to remove excess 4-bromophthalic anhydride, and dried in a ventilated place to obtain product 2 (Cs-Br).

[0041] Step b: Weigh 60 mg of product 2, add 6 mL of N-methylpyrrolidone (NMP), heat and stir to dissolve completely, add 100 mg of sodium azide (NaN 3 ), under nitrogen pro...

Embodiment 2

[0044] Synthesis of Chitosan-Cy7 Polymer:

[0045] Weigh 30 mg of product 3, dissolve it in 3 mL of dimethyl sulfoxide, add to the flask, and then add 5 mg of Cy7. The flask was sealed with a rubber stopper. After vacuuming, under nitrogen protection, 4 mg of copper sulfate pentahydrate (dissolved in 200 μL of secondary water) was first added dropwise to the flask with a 1 mL syringe, and then 3 mg of sodium ascorbate (dissolved in 200 μL of secondary water) was added dropwise to the flask. secondary water). The reactants were reacted at 50 °C for 72 h in the dark. After the reaction, the reaction solution was dialyzed in secondary water for 72 hours with a 10,000 gauge dialysis bag. After dialysis, the product was lyophilized to yield polymer C7. C7 was dissolved in dimethyl sulfoxide, the excitation wavelength was 633nm, and the fluorescence intensity was measured. Such as figure 2 As shown, C7 has the characteristic peak of Cy7 at 790-810nm, indicating that Cy7 has be...

Embodiment 3

[0047] Synthesis of chitosan-erlotinib polymer:

[0048] Weigh 30 mg of product 3, dissolve in 3 mL dimethyl sulfoxide, add to the flask, and then add 25 mg Erlotinib. The flask was sealed with a rubber stopper. After vacuuming, under nitrogen protection, 4 mg of copper sulfate pentahydrate (dissolved in 200 μL of secondary water) was first added dropwise to the flask with a 1 mL syringe, and then 3 mg of sodium ascorbate (dissolved in 200 μL of secondary water) was added dropwise to the flask. secondary water). The reactants were reacted at 50 °C for 72 h in the dark. After the reaction, the reaction solution was dialyzed in secondary water for 72 hours with a 10,000 gauge dialysis bag. After dialysis, the product was lyophilized to obtain polymer CE. The product was dissolved in dimethyl sulfoxide to measure the ultraviolet absorption, such as image 3 As shown, Erlotinib has a characteristic absorption peak at 330-350nm, and CE has ultraviolet absorption at 340nm, indic...

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Abstract

The invention discloses an Erlotinib-Cy7-chitosan polymer with tumor targeting. According to the Erlotinib-Cy7-chitosan polymer, lung-cancer molecular targeted medicine Erlotinib and the heptamethine cyanine dye Cy7 are connected to chitosan modified by the chemical structure through click chemistry, and a chitosan derivative (CE7) is obtained. According to the Erlotinib-Cy7-chitosan polymer, chemical synthesis is simple and easy to carry out, the polymer CE7 can be self assembled to form nanometer particle CE7Ns, the nontoxic and high-biocompatibility characteristics of chitosan are reserved, the water solubility and the bioavailability of the Erlotinib are greatly improved, the toxic and side effects of medicine are reduced, near-infrared fluorescence imaging and photodynamic therapy can also be carried out, and the therapy effect is improved.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to an erlotinib-Cy7-chitosan polymer. Background technique [0002] Cancer is a major disease that threatens human health and life, and lung cancer is one of the cancers that cause the most deaths among all cancers. In recent years, the rapid development of molecular biology has brought cancer treatment into the era of molecular targeted therapy (Molecular Targeted Therapy), bringing new hope to cancer patients. Due to the advantages of molecular targeted drugs such as high efficiency, low toxicity, and strong specificity, targeted therapy has become a key direction in the research and development of anticancer drugs. [0003] EGFR tyrosine kinase inhibitor (EGFR-TKI) is one of the first anticancer drugs successfully developed as targeted therapy. EGFR tyrosine kinase regulates cell growth, differentiation and apoptosis inhibition, and this signal transduction play...

Claims

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Application Information

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IPC IPC(8): C08B37/08A61K49/00A61K41/00A61K47/61A61K31/517A61P35/00
CPCA61K31/517A61K41/0057A61K49/0032C08B37/003
Inventor 高瑜张慧娟张英英陈海军贾力
Owner FUZHOU UNIV
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