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Anti-tumor multi-medicine resistant targeted liposome

An anti-tumor drug, liposome technology, applied in the directions of anti-tumor drugs, liposome delivery, drug combination, etc., can solve the problems of single action target, clinical application impact, large toxic and side effects, etc., and achieves a simple preparation method, Enhance cytotoxicity and efficient killing effect

Inactive Publication Date: 2012-02-22
BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the current tumor MDR reversal agents generally have the problem of single target and high toxicity and side effects, which greatly affects their clinical application.
Existing individual studies have tried to combine antineoplastic drugs with tumor resistance reversal agents, but the final effect is not good
In addition, it has been reported that liposomes are used as carriers to simultaneously entrap antineoplastic drugs and other drugs to treat tumors, but further research has found that the combination of these drugs and antineoplastic drugs still cannot solve the problem of multidrug resistance.

Method used

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  • Anti-tumor multi-medicine resistant targeted liposome
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  • Anti-tumor multi-medicine resistant targeted liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Comparison of Plasma Leakage Rates of Different Tumor Resistance Reversal Agents-Adriamycin Combined with Encapsulated Liposomes

[0032] Weigh the prescribed amount of HSPC, CHOL, DSPE-PEG2000, quercetin or curcumin (HSPC: CHOL: DSPE-PEG2000: quercetin or curcumin = 120:40:15:6mol / mol) and place in a pear-shaped bottle , add absolute ethanol to dissolve. A uniform thin film was formed by rotary evaporation under reduced pressure at 40°C. Add 0.15mol / L ammonium sulfate solution, and hydrate in a water bath at 75°C under normal pressure for 30 minutes to fully swell and hydrate the phospholipids. The resulting suspension was subjected to probe ultrasonication (600W) for 9 minutes, and then sequentially extruded through 0.8 μm, 0.4 μm and 0.2 μm nucleated polycarbonate films for 5 times each to granulate. Gained liposomes are placed in a dialysis bag (molecular weight 8000-14000M), dialyzed with normal saline for 10h to form an ammonium sulfate gradient; then...

Embodiment 2

[0038] Example 2: Screening of the ratio of liposome excipients jointly loaded with quercetin (QUE) and doxorubicin (DOX)

[0039] Accurately weigh the prescribed amount of HSPC, CHOL and QUE according to Table 2, put them in a pear-shaped bottle, and add absolute ethanol to dissolve. A uniform thin film was formed by rotary evaporation under reduced pressure at 40°C. Add 0.15mol / L ammonium sulfate solution, and hydrate in a water bath at 75°C under normal pressure for 30 minutes to fully swell and hydrate the phospholipids. The obtained light yellow suspension was subjected to ultrasonic probe (600W) for 10 min. Gained liposomes were placed in a dialysis bag (molecular weight 8000-14000M), dialyzed with normal saline for 10 h to form an ammonium sulfate gradient; then mixed with the prescribed amount of DOX solution 1:1 (V / V), incubated in a water bath at 37°C for 25 min, Get this product.

[0040] Chromatographic conditions: RP-HPLC chromatographic conditions: chromatogra...

Embodiment 3

[0051] Example 3: Research on long-circulation liposomes jointly loaded with quercetin (QUE) and doxorubicin (DOX)

[0052] Further studies have shown that adding PEG-modified phospholipids or cholesterol to liposome-forming phospholipids or cholesterol can enable liposomes to achieve long-term circulation. In order to obtain long-circulating liposomes with better effect, the long-circulating liposomes jointly loaded with quercetin (QUE) and doxorubicin (DOX) were further studied according to Table 3 below. Precisely weigh the prescribed amount of HSPC, CHOL, QUE and DSPE-PEG2000, put them in a pear-shaped bottle, and add absolute ethanol to dissolve. A uniform thin film was formed by rotary evaporation under reduced pressure at 40°C. Add 0.15mol / L ammonium sulfate solution, and hydrate in a water bath at 75°C under normal pressure for 30 minutes to fully swell and hydrate the phospholipids. The obtained light yellow suspension was subjected to ultrasonic probe (600W) for 10...

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Abstract

The invention relates to an anti-tumor multi-medicine resistant targeted liposome and a preparation method thereof, in particular to an anti-tumor multi-medicine resistant long circulating targeted liposome. The invention is characterized in that: quercitin and an anti-tumor medicine are jointly coated in the liposome, and simultaneously target tumor tissues to reverse the multi-medicine resistance of tumors, cytotoxicity of anti-tumor medicines on medicine resistant tumors is enhanced, the change of pharmacokinetic properties of the anti-tumor medicines in vivo and the enhancement of toxic and side effects of the anti-tumor medicines in vivo, which are caused by the difference and interaction of the pharmacokinetic properties of different medicines in vivo, are avoided, and the treatmenteffect on medicine resistant tumors is improved.

Description

Technical field: [0001] The invention relates to an anti-tumor drug-resistant liposome and a preparation method thereof, in particular to an anti-tumor multidrug-resistant long-circulation targeting liposome. It is characterized in that quercetin and antineoplastic drugs are jointly encapsulated in liposomes, and simultaneously targeted to tumor tissues, reversing multidrug resistance of tumors, enhancing the cytotoxic effect of antineoplastic drugs on drug-resistant tumors, and avoiding the effects of different drugs. The changes in the pharmacokinetic properties of anti-tumor drugs and the enhancement of toxic and side effects caused by the differences and interactions in the pharmacokinetic properties in vivo can improve the therapeutic effect on drug-resistant tumors. Background technique: [0002] Tumor multidrug resistance (MDR) means that after long-term exposure of tumor cells to a chemotherapeutic drug, the tumor develops cross-resistance to a variety of anti-tumor ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/28A61K47/32A61K31/704A61K31/352A61P35/00
Inventor 戴俊东陈浩王玉蓉孙毅坤王英姿
Owner BEIJING UNIV OF CHINESE MEDICINE
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