Functional liposome for treating lung cancer as well a s preparation method and application of functional liposome

A technology targeting liposomes and lecithins, applied in the field of lung tumor drug research, can solve problems such as tumor recurrence, and achieve the effect of improving the effect of chemotherapy and preventing tumor recurrence.

Inactive Publication Date: 2017-12-05
SHIHEZI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, according to the theory of cancer stem cells (CSCs), this does not represent the complete elimination of cancer stem cells. If the cancer stem cells continue to proliferate after treatment, the tumor may relapse after remission

Method used

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  • Functional liposome for treating lung cancer as well a s preparation method and application of functional liposome
  • Functional liposome for treating lung cancer as well a s preparation method and application of functional liposome
  • Functional liposome for treating lung cancer as well a s preparation method and application of functional liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1, the preparation of liposome

[0050] 1. Preparation of blank liposomes

[0051] 1. Preparation of blank liposomes

[0052] Dissolve lecithin, cholesterol and DSPE-PEG2000 in methanol at a molar ratio of 63.86:9.83:1, remove methanol by rotary evaporation, and form a film in an eggplant-shaped flask by rotary evaporation at 35°C and 40rpm, add 10mL of 250mM ammonium sulfate, and first place in a water bath Sonicate for 5 minutes, then transfer to a serum bottle and perform further sonication in a JY92 ultrasonic cell pulverizer (ultrasonic working time is 10 s, intermittent time is 30 s, the whole time is 10 min, and the protection temperature is 35 ° C), and then use liposome extrusion The press was passed through 400nm and 200nm polycarbonate membranes respectively 3 times, and the liposome external phase was replaced with PBS solution (pH=7.4) by dialysis to obtain blank liposomes.

[0053] 2. Preparation of blank liposomes modified by distearoylphosph...

Embodiment 2

[0059] Embodiment 2, the performance measurement of liposome

[0060] 1. Determination of Encapsulation Efficiency

[0061] The unencapsulated ragragulin and EGGC were removed by dialysis, and the content was determined by high performance liquid chromatography. Take an appropriate amount of ragragulin liposomes, EGCG liposomes, FA-HPDL-EGCG liposomes and digest with acetonitrile before dialysis, and determine the contents of ragragulin and EGCG; , EGCG liposome, FA-HPDL-EGCG liposome add acetonitrile digestion, measure the content of the EGCG that entraps in the liposome, calculate drug encapsulation efficiency according to formula (1):

[0062] Encapsulation rate%=W 包 / W 总 ×100% (1)

[0063] where W 总 is the total drug dose; W 包 Indicates the amount of drug entrapped in liposomes.

[0064] In the prepared drug-loaded liposome, the encapsulation efficiency of ragragulin can reach 86%, and the encapsulation efficiency of EGCG can reach 75%.

[0065] 2. Particle size an...

Embodiment 3

[0074] Example 3. Research on the inhibitory effect of drug-loaded liposomes on lung adenocarcinoma A549 cells in vitro

[0075] 1. Training conditions

[0076] 1. Culture conditions of lung adenocarcinoma A549 cells

[0077] Lung adenocarcinoma A549 cells were cultured in DMEMF12 high-glucose medium containing 10% fetal bovine serum, 100 U / mL penicillin and 100 μg / mL streptomycin at 37 °C, 5% CO 2 Incubated in a saturated humidity incubator, the lung adenocarcinoma A549 cells grew adherently, and the cell morphology was spindle-shaped, ( figure 2 As shown in (A), the cells in the logarithmic growth phase were taken for the experiment.

[0078] 2. Culture conditions of lung adenocarcinoma A549 stem cells

[0079] A549 cells in the logarithmic growth phase were taken, washed with PBS, digested with 0.25% trypsin, blown into single cell suspension, resuspended in serum-free medium (containing DMEM / F12, bFGF, EGF, B27), 4~ After 5 days, the cells proliferate to form tumor st...

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Abstract

The invention discloses a functional liposome for treating lung cancer as well as a preparation method and an application of the functional liposome. The targeting liposome is prepared from lecithin, cholesterol, distearoyl phosphatidylethanolamine-polyethylene glycol and distearoyl phosphatidylethanolamine-polyethylene glycol-folic acid. According to the functional liposome provided by the invention, by modifying the DSPE-PEG2000-FA on the surface of liposome, an effect of targeting cancer cells is achieved; in the multifunctional lung cancer stem cell targeting compound liposome that an anti-tumor drug, namely hispidulin, and a tumor cell apoptosis inducer, namely EGCG, are entrapped in the liposome, the medicines (the hispidulin and the EGCG) can reach a focus part, and the two medicines, which are combined, can kill cancer cells and induce cancer stem cell apoptosis, so that a chemotherapy effect is greatly enhanced, and it is expected that the recurrence of the cancer can be effectively prevented. With the application of the functional liposome, it brings hope to the radical treatment of the lung cancer; therefore, the liposome has important theoretical significance and clinical significance.

Description

technical field [0001] The invention relates to a functional liposome and its preparation method and application, in particular to a functional liposome for treating lung tumors, its preparation method and application, and belongs to the field of lung tumor drug research. Background technique [0002] In recent years, the morbidity and mortality of tumors have increased significantly. Lung cancer is the malignant tumor with the highest morbidity and mortality in the world, of which non-small cell lung cancer (NSCLC) accounts for about 80%, and the number of lung cancer deaths is about 1.5 million every year. . The degree of malignancy of NSCLC is relatively high, and it is easy to relapse and transfer. More than 50% of the patients have reached a relatively advanced stage once they are diagnosed. Clinical treatment mostly adopts comprehensive treatment based on radiotherapy and chemotherapy, but the effect is not satisfactory. Radiation therapy is difficult to eradicate th...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/353A61K9/127A61K47/24A61P35/00
CPCA61K31/352A61K31/353A61K47/24A61K2300/00
Inventor 应雪李霞闫荷露何兰玉唐辉
Owner SHIHEZI UNIVERSITY
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