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Folate targeted ultrasound priming oridonin lipid microbubble and application thereof

A targeting technology of oridonin and folic acid, which is applied in the direction of liposome delivery, medical preparations containing non-active ingredients, and medical preparations containing active ingredients, etc., which can solve problems such as difficulty in penetrating cell membranes, and achieve inhibition tumor effect

Inactive Publication Date: 2015-04-08
NANJING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It not only solves the targeting problem of the drug delivery system, but also overcomes the problem that liposomes are difficult to penetrate the cell membrane under physiological conditions, and improves the anti-tumor effect of the drug

Method used

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  • Folate targeted ultrasound priming oridonin lipid microbubble and application thereof
  • Folate targeted ultrasound priming oridonin lipid microbubble and application thereof
  • Folate targeted ultrasound priming oridonin lipid microbubble and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027]The preparation of folic acid-targeted ultrasound-induced oridonin lipid microbubbles is carried out according to the following steps: take soybean lecithin 130mg, cholesterol 70mg, FA-PEG-DSPE (folate-coupled polymer complex) 500mg In the round-bottomed flask, add 30mL ethanol solvent to dissolve, evaporate the solvent under reduced pressure, the lipid forms a relatively uniform lipid film at the bottom of the round-bottomed flask, then add 40mg oridonin (C 20 h 28 o 6 ) and 40mg of epigallocatechin gallate in PBS buffer 30mL, continue to rotate for 0.5h, place it in the refrigerator (4-5°C) overnight to make it fully hydrated, add an appropriate amount of glass beads, and then fill it with 200mg of carbon dioxide gas. After shaking for 0.5 h, lipid microbubbles carrying oridonin were prepared.

[0028] After testing, the average particle diameter of the liposomes in the liquid preparation is 560nm, the particle diameters are all below 1000nm, and the particle size di...

Embodiment 2

[0030] The preparation of folic acid-targeted ultrasound-induced oridonin lipid microbubbles is carried out according to the following steps: Weigh 130 mg of soybean lecithin, 70 mg of cholesterol, and 500 mg of FA-PEG-Chol folic acid-coupled polymer complex and place it in a round bottom In the flask, add 30mL of acetone solvent to dissolve, evaporate the solvent under reduced pressure, and the lipid forms a relatively uniform lipid film at the bottom of the round bottom flask, then add 40mg of oridonin and 40mg of epigallocatechin gallate. 30mL of PBS buffer solution continued to rotate for 0.5h, placed in the refrigerator (4°C) overnight to fully hydrate, added an appropriate amount of glass beads, and then filled with 200mg of carbon dioxide gas and mechanically oscillated for 2h to prepare lipid microbes carrying oridonin A. Bubble.

[0031] After testing, the average particle diameter of the liposomes in the liquid preparation is 620nm, the particle diameters are all bel...

Embodiment 3

[0033] The preparation of folic acid-targeted ultrasound-induced oridonin lipid microbubbles was carried out in accordance with the following steps: Weigh 130 mg of soybean lecithin, 70 mg of cholesterol, and FA-PEG-CHEMS folic acid-coupled polymer complex and place it in a round-bottomed flask , add 30mL dichloromethane solvent to dissolve, evaporate the solvent under reduced pressure, the lipid forms a relatively uniform lipid film at the bottom of the round bottom flask, then add 40mg oridonin and 40mg epigallocatechin gallate Continue to rotate 30mL of PBS buffer solution for 0.5h, place it in the refrigerator (4°C) overnight to make it fully hydrated, add an appropriate amount of glass beads, and then fill it with 200mg of carbon dioxide gas and shake it mechanically for 1h to prepare a lipid carrying oridonin A microbubbles.

[0034] After testing, the average particle diameter of the liposomes in the liquid preparation is 480nm, the particle diameters are all below 1000...

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Abstract

The invention discloses a folate targeted ultrasound priming oridonin lipid microbubble as well as a preparation and an application thereof. The folate targeted ultrasound priming oridonin lipid microbubble is prepared by the following method: weighing a phospholipid component and a polymer composite coupling cholesterol with folate, adding a solvent to dissolve the components, decompression evaporating the solvent so that the lipid forms a relatively uniform lipid film on the bottom of a round-bottom flask, adding a proper amount of PBS buffer solution containing oridonin, continuing to rotate for 0.5-2 hours, stewing at 4-5 DEG C over the night for full hydration, adding a proper amount of glass beads, filling an inert gas and mechanically oscillating for 0.5-2 hours to obtain the folate targeted lipid microbubble containing the oridonin. The antineoplastic activity of the folate targeted ultrasound priming oridonin lipid microbubble is primarily researched under ultrasound guide, and In vivo studies confirm that the folate targeted ultrasound priming oridonin lipid microbubble significantly inhibits the growth of liver cancer, breast cancer and gastric cancer with high expression of folate receptor.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to folic acid-targeted ultrasound-promoted oridonin A lipid microvesicles for treating liver cancer, breast cancer and gastric cancer. Background technique [0002] According to the "2012 China Cancer Registration Annual Report" released by the National Cancer Registration Center, 6 people are diagnosed with cancer every minute. Primary liver cancer (mainly hepatocellular carcinoma, hereinafter referred to as liver cancer) is a malignant tumor with the sixth highest incidence rate and the third highest mortality rate in the world. There are about 748,300 new cases every year, and the number of liver cancer deaths worldwide is about 700,000 people. In Asia, the incidence of liver cancer is higher than other regions in the world due to the spread of hepatitis B virus and other reasons. China is an area with a high incidence of liver cancer, accounting for about 55% of global ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/352A61K47/34A61P35/00
Inventor 李伟王传金张哲徐悦
Owner NANJING UNIV OF SCI & TECH