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Novel water-soluble targeted nano drug carrier based on carboxymethyl chitosan, and preparation method of novel water-soluble targeted nano drug carrier

A technology of carboxymethyl chitosan and nano-drug carrier, which is applied in the field of novel water-soluble targeted nano-drug carrier and its preparation, can solve the problems of poor water solubility, short circulation time, lack of targeting, etc., and achieve enhanced water solubility. , the preparation process is simple, easy to operate

Inactive Publication Date: 2018-09-25
BEIJING FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ursolic acid (UA) and hydroxycamptothecin (HCPT) are antitumor drugs, but due to their poor water solubility, lack of targeting, and short circulation time in the body, their clinical applications are largely limited. application

Method used

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  • Novel water-soluble targeted nano drug carrier based on carboxymethyl chitosan, and preparation method of novel water-soluble targeted nano drug carrier
  • Novel water-soluble targeted nano drug carrier based on carboxymethyl chitosan, and preparation method of novel water-soluble targeted nano drug carrier
  • Novel water-soluble targeted nano drug carrier based on carboxymethyl chitosan, and preparation method of novel water-soluble targeted nano drug carrier

Examples

Experimental program
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Effect test

Embodiment 1

[0028] (1) Preparation of folic acid-polyethylene glycol conjugate: Dissolve 440 mg of folic acid in 20 mL of dimethyl sulfoxide and heat to 50° C., add 383 mg of EDC and 230 mg of NHS to react for 6 h. After the activated folic acid-NHS was reacted with 781mg ethylenediamine and 500mg acetone overnight at room temperature, excess acetonitrile was added to obtain a precipitate, which was filtered and vacuum-dried to obtain folic acid active ester. The obtained folic acid active ester was mixed with 1.60g NH 2 -PEG-COOH was dissolved in 20 mL of acetonitrile, 0.38 g of EDC and 0.23 g of NHS were added, and 0.024 g of DMAP was reacted for 8 h. Dialyzed for 24 hours to remove unreacted folic acid active ester. Obtain folic acid-polyethylene glycol conjugate.

[0029] (2) Synthesis of folic acid-polyethylene glycol-carboxymethyl chitosan polymer: Weigh 0.04g folic acid-polyethylene glycol conjugate and dissolve it in 20mL dimethyl sulfoxide, add 0.46g EDC and 0.28g NHS, 0.03g D...

Embodiment 2

[0033] (1) Preparation of folic acid-polyethylene glycol conjugate: Dissolve 440 mg of folic acid in 20 mL of dimethyl sulfoxide and heat to 50° C., add 383 mg of EDC and 230 mg of NHS to react for 6 h. After the activated folic acid-NHS was reacted with 781mg ethylenediamine and 500mg acetone overnight at room temperature, excess acetonitrile was added to obtain a precipitate, which was filtered and vacuum-dried to obtain folic acid active ester. The obtained folic acid active ester was mixed with 3.20g NH 2 -PEG-COOH was dissolved in 40 mL of acetonitrile, 0.76 g of EDC and 0.46 g of NHS were added, and 0.048 g of DMAP was reacted for 8 h. Dialyzed for 24 hours to remove unreacted folic acid active ester. Obtain folic acid-polyethylene glycol conjugate.

[0034] (2) Synthesis of folic acid-polyethylene glycol-carboxymethyl chitosan polymer: Weigh 0.08g folic acid-polyethylene glycol conjugate and dissolve it in 20mL dimethyl sulfoxide, add 0.92g EDC and 0.56g NHS, 0.06g D...

Embodiment 3

[0038] (1) Preparation of folic acid-polyethylene glycol conjugate: Dissolve 440 mg of folic acid in 20 mL of dimethyl sulfoxide and heat to 50° C., add 383 mg of EDC and 230 mg of NHS to react for 6 h. After the activated folic acid-NHS was reacted with 781mg ethylenediamine and 500mg acetone overnight at room temperature, excess acetonitrile was added to obtain a precipitate, which was filtered and vacuum-dried to obtain folic acid active ester. The obtained folic acid active ester was mixed with 2.40g NH 2 -PEG-COOH was dissolved in 20 mL of acetonitrile, 0.57 g of EDC and 0.345 g of NHS were added, and 0.036 g of DMAP was reacted for 8 h. Dialyzed for 24 hours to remove unreacted folic acid active ester. Obtain folic acid-polyethylene glycol conjugate.

[0039](2) Synthesis of folic acid-polyethylene glycol-carboxymethyl chitosan polymer: Weigh 0.06g folic acid-polyethylene glycol conjugate and dissolve it in 30mL dimethyl sulfoxide, add 0.69g EDC and 0.42g NHS, 0.045g ...

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Abstract

The invention discloses a novel water-soluble targeted nano drug carrier based on carboxymethyl chitosan, and a preparation method of the novel water-soluble targeted nano drug carrier. The method comprises the following steps: linking targeted molecular folic acid with polyethylene glycol by using an amido bond; coupling the obtained folic acid-polyethylene glycol conjugate with the carboxymethylchitosan by means of an amidation reaction; enabling the product to be subjected to an esterification reaction with ursolic acid; enabling the prepared folic acid-polyethylene glycol-carboxymethyl chitosan-ursolic acid conjugate to be wrapped with another medicine, i.e., 10-hydroxycamptothecine by means of self-assembling in water so as to obtain nanoparticles loaded with two anticancer medicines. The nanoparticles have two-layer structures, the outer layer is hydrophilic carboxymethyl chitosan-polyethylene glycol, and the inner layer is the hydrophobic drug ursolic acid and the 10-hydroxycamptothecine. The novel water-soluble targeted nano drug carrier has the advantages that the nano drug carrier improves the water solubility, stability and half-life period of the ursolic acid and the 10-hydroxycamptothecine, so that the drug loading capacity is greatly increased; the folic acid is linked for enhancing the targeting effect of the medicines on tumor sites; the method is simple in preparation process and easy to operate.

Description

[0001] manual technical field [0002] The invention relates to a novel water-soluble targeting nano-medicine carrier based on carboxymethyl chitosan and a preparation method thereof, belonging to the technical field of medicine and nano-medicine. Background technique [0003] Cancer has become a major disease that endangers human health. One of the important methods to treat cancer is chemical drug therapy. However, many anticancer drugs have defects such as insoluble in water and poor stability. In addition, poor selectivity of anticancer drugs, large adverse reactions, and drug resistance of tumors have greatly affected the efficacy of cancer treatment. Therefore, how to solubilize insoluble anticancer drugs and improve the selectivity to cancer cells is very important. [0004] Drug delivery systems (DDS) solve the shortcomings of anticancer drugs such as poor water solubility and poor selectivity. It has enhanced permeability and retention effects, and nanocarriers can...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/36A61K47/22A61K47/10A61K47/61A61K47/60A61K47/69A61K47/54A61K31/4745A61K31/56A61P35/00
CPCA61K9/5161A61K9/5123A61K9/5146A61K31/4745A61K31/56A61K47/545A61K47/60A61K47/61A61K47/6935A61K47/6939A61P35/00A61K2300/00
Inventor 李桂亮何静张依诺朱蓬勃王英飒雷建都
Owner BEIJING FORESTRY UNIVERSITY
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