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Application of ursolic-acid nano medicine-carrying microspheres for treating tumors and preparation

A nano-loaded drug and ursolic acid technology, which is applied in the direction of antineoplastic drugs, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of limited application, easy formation of embolism, high cost, etc., and achieve cycle time extension and preparation The method is simple and easy, and the effect of superior anti-tumor drug effect

Inactive Publication Date: 2012-09-19
李晓林
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the nano-microspheres prepared by this method need to go through multiple steps such as dissolving, heating, mixing, emulsifying, cooling, and filling. , will limit its further application in clinical

Method used

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  • Application of ursolic-acid nano medicine-carrying microspheres for treating tumors and preparation
  • Application of ursolic-acid nano medicine-carrying microspheres for treating tumors and preparation
  • Application of ursolic-acid nano medicine-carrying microspheres for treating tumors and preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Step 1, dispensing: take by weighing 60g ursolic acid and 940g drug-loaded material respectively according to the weight ratio of raw material components, wherein, the drug-loaded material is the amphiphilic block copolymer polymer polycaprolactone and polyethylene glycol synthesis. Caprolactone-polyethylene glycol (mPEG-PCL), wherein: mPEG molecular weight 4000, PCL molecular weight 20000;

[0041] Step 2, drug dissolving: under normal temperature conditions, raw material components such as 60g ursolic acid and 940g drug-loaded material taken in step 1 are dissolved in a certain amount of acetone solvent (by weight ratio of components, raw material group points 80%, acetone solvent 20%);

[0042] Step 3, dilution: Slowly add the acetone solution obtained in step 2 to a certain amount of distilled water under stirring conditions (the volume ratio of acetone solution to distilled water is 1:4), and then obtain light blue ursolic acid microspheres acetone and water mixed...

Embodiment 2

[0047] Step 1, dispensing: weigh 200g ursolic acid and 800g drug-loaded material according to the weight ratio of the raw material components, wherein the drug-loaded material is an amphiphilic block copolymer polylactic acid- Polyethylene glycol (mPEG-PLA), in which: mPEG molecular weight 4000, PLA molecular weight 40000;

[0048] Step 2, drug dissolving: under normal temperature conditions, raw material components such as 200g ursolic acid and 800g drug-loaded material taken in step 1 are dissolved in a certain amount of acetone solvent (by weight ratio of components, raw material group 65%, acetone solvent 35%);

[0049] Step 3, dilution: slowly drop the acetone solution obtained in step 2 into a certain amount of distilled water under stirring conditions (the volume ratio of acetone solution to distilled water is 1:4.5), and then obtain light blue ursolic acid microspheres acetone and water mixed solution;

[0050] Step 4, purification: put the diluted acetone solution o...

Embodiment 3

[0055] Step 1, dispensing: Weigh 360g ursolic acid and 640g drug-loaded material according to the weight ratio of the raw material components, wherein the drug-loaded material is an amphiphilic block copolymer polyhydroxy Acetic acid-polyethylene glycol (mPEG-PLGA), in which: mPEG molecular weight is 4000, PLGA molecular weight is 36000;

[0056] Step 2, drug dissolving: under normal temperature conditions, raw material components such as 360g ursolic acid and 640g drug-loaded material taken in step 1 are dissolved in a certain amount of acetone solvent (by weight ratio of components, raw material group points 50%, acetone solvent 50%);

[0057] Step 3, dilution: Slowly add the acetone solution obtained in step 2 to a certain amount of distilled water under stirring conditions (the volume ratio of acetone solution to distilled water is 1:5), and then obtain light blue ursolic acid microspheres acetone and water mixed solution;

[0058] Step 4, purification: put the diluted a...

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Abstract

The invention relates to the application of ursolic-acid nano medicine-carrying microspheres for treating tumors. The ursolic-acid nano medicine-carrying microspheres contain ursolic acid and a medicine-carrying material which are mixed, wherein the medicine-carrying material is a biparental segmented copolymer synthesized by one of polycaprolactone, polylactic acid or polyglycolic acid and polyethylene glycol, i.e. polycaprolactone-polyethylene glycol (mPEG-PCL), polylactic acid-polyethylene glycol (mPEG-PLA) or polyglycolic acid-polyethylene glycol (mPEG-PLGA); and the ursolic-acid nano medicine-carrying microspheres comprise 5 to 35wt% of ursolic acid and 65 to 95wt% of medicine-carrying material which are mixed.

Description

technical field [0001] The invention relates to an anti-tumor ursolic acid nano drug-loaded microsphere and a preparation method thereof. Background technique [0002] Ursolic acid, also known as ursolic acid and ursolic acid, is a pentacyclic triterpenoid compound that exists in natural plants. A variety of biological effects, ursolic acid also has obvious antioxidant function, so it is widely used as raw materials for medicine and cosmetics. In recent years, Ursolic Acid Inhibits Proliferation and Induces Apoptosis of Cancer Cells In Vitro and In Vivo published by Wang et al. J Biomed Biotechnol.2011;2011:419343.Ursolic acid inhibits proliferation and induces apoptosis of HT-29 colon cancer cells by inhibiting the EGFR / MAPK pathway.J Zhejiang Univ Sci B.2009;10(9):668–674. Relevant literatures at home and abroad show that ursolic acid has inhibitory effects on various tumors and can promote tumor cell apoptosis. However, due to its extremely poor water solubility, the a...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/16A61K31/56A61K47/34A61P35/00
Inventor 李晓林郑东辉张皓
Owner 李晓林
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