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Sodium alginate liver-targeted nanometer drug delivery system and preparing method thereof

A technology of sodium alginate and drug delivery system, which is applied in the field of biomedicine to achieve the effects of reducing drug side effects, reducing drug dosage and administration times, and improving drug efficacy

Inactive Publication Date: 2009-10-07
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, the sodium alginate liver-targeting nano drug delivery system technology has active liver targeting and can simultaneously encapsulate hydrophilic anticancer drugs and hydrophobic anticancer drugs or only encapsulate a single anticancer drug. Have not seen related literature reports

Method used

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  • Sodium alginate liver-targeted nanometer drug delivery system and preparing method thereof
  • Sodium alginate liver-targeted nanometer drug delivery system and preparing method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0023] 1) Dissolve glycyrrhetinic acid in tetrahydrofuran, the solution concentration is 300mg / mL, add N,N'-dicyclohexylcarbodiimide, glycyrrhetinic acid and N,N'-dicyclohexylcarbodiimide to the solution The molar ratio of glycyrrhetinic acid and N-hydroxysuccinimide is 1:1, after stirring for 0.5h, add N-hydroxysuccinimide, the molar ratio of glycyrrhetinic acid and N-hydroxysuccinimide is 1:1, continue to stir for 20h, filter and add the filtrate dropwise In 70 mL of tetrahydrofuran solution of ethylenediamine, the molar ratio of glycyrrhetinic acid to ethylenediamine is 1:20, react for 24 hours, precipitate with water, separate the solid and dry it in vacuum, separate and purify the product by column chromatography, and put it in the column chromatography liquid The volume ratio of ethyl acetate to methanol is 1:2 to obtain glycyrrhetinic acid-ethylenediamine which is a single-end modified liver targeting compound.

[0024] 2) Dissolve sodium alginate in water, the solution...

Embodiment 2

[0027] 1) Dissolve glycyrrhetinic acid in tetrahydrofuran, the solution concentration is 50mg / mL, add N,N'-dicyclohexylcarbodiimide, glycyrrhetinic acid and N,N'-dicyclohexylcarbodiimide to the solution The molar ratio of glycyrrhetinic acid and N-hydroxysuccinimide is 1:2, after stirring for 1h, add N-hydroxysuccinimide, the molar ratio of glycyrrhetinic acid and N-hydroxysuccinimide is 1:2, continue to stir for 20h, filter, and drop the filtrate into 70mL In the tetrahydrofuran solution of ethylenediamine, the molar ratio of glycyrrhetinic acid to ethylenediamine is 1:40, react for 12 hours, precipitate with water, collect the solid, and dry it in vacuum. The volume ratio of ethyl acetate to methanol in the column chromatography liquid is 1 : 2, to obtain the glycyrrhetinic acid-ethylenediamine of the single-end modified liver targeting compound.

[0028] 2) Sodium alginate was dissolved in water, the solution concentration was 40mg / mL, after stirring for 1 hour, 1-(3-dimeth...

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Abstract

A sodium alginate liver-targeted nanometer drug delivery system uses sodium alginate as carrier material and uses glycyrrhetic acid as liver-targeted compound. The single-end-modified glycyrrhetic acid-ethylene diamine is prepared through the reacting between the carboxy group of glycyrrhetic acid and the ethylene diamine. The glycyrrhetic acid-sodium alginate is prepared through the reacting between the carboxy group of sodium alginate and the amino group of glycyrrhetic acid-ethylene diamine. Finally the sodium alginate liver-targeted drug delivery nanometer particles are prepared through crosslinking the glycyrrhetic acid-sodium alginate through calcium ions. The invention has a beneficial effect that the liver-targeted nanometer drug delivery system prepared by the invention has high liver targeting property. The hydrophilic anticancer drug and hydrophobic anticancer drug can be packaged simultaneously or a single anticancer drug is packaged. The sodium alginate liver-targeted nanometer drug delivery system of the invention has the advantages of sustained-releasing function of drug, reduced drug dosage, reduced drug taking times, reduced toxic-side effect of drug, increased drug effect, simple and practical preparing method, and excellent application prospect.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a sodium alginate liver-targeted nano drug delivery system and a preparation method thereof. Background technique [0002] Malignant tumor is a common and frequently-occurring disease that seriously threatens human health. At present, there is no effective prevention and control measure. According to the United Nations website, the main types of cancers that cause death are: lung cancer, stomach cancer, liver cancer, colon cancer and so on. In 2007, the number of deaths due to liver cancer was as high as 653,000. At present, the main method of clinical treatment of cancer is chemotherapy, but the antitumor drugs used in chemotherapy have serious toxic and side effects on normal organs of the human body. Therefore, serious adverse reactions often occur during chemotherapy. The liver-targeted drug delivery system has the advantages of strong specificity, reduced toxic and side effects,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K47/28A61K47/18A61K9/14A61K31/704A61K31/513A61K31/337A61P35/00
Inventor 袁直王蔚张闯年黄微田秦
Owner NANKAI UNIV
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