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Nanoparticle liposome for releasing different medicines in programmed manner and preparation and use thereof

A procedural, nanoparticle technology, applied in liposome delivery, drug combination, medical preparations of non-active ingredients, etc., can solve problems such as undiscovered, cationic nanoparticle injection toxicity, etc., to improve utilization rate and reduce medical treatment Cost, effect of reducing patient suffering

Inactive Publication Date: 2011-09-21
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The Chinese patent "Nano Cell Delivery System" (Patent No.: 200580013065.9) involves the form of lipid vesicles encapsulating PLGA nanoparticles, and has protected the rights of the sequential effects of the two preparations, but its examples only involve The synergistic therapeutic effect of vascular inhibitor cabretastatin and chemotherapeutic drugs does not involve the application of reversing tumor multidrug resistance. In addition, in the present invention, dodecyldimethylammonium bromide (DMAB) is used as a binder to carry out The preparation of self-assembled preparations of nanoparticle liposomes, this preparation method can solve the injection toxicity problem of cationic nanoparticles, has a good application prospect, has not been reported so far, and it has not been found that dihydroartemisinin phospholipids Drugs and doxorubicin are co-encapsulated to prepare nanoparticle liposomes for the study of anti-drug resistance and anti-tumor effects

Method used

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  • Nanoparticle liposome for releasing different medicines in programmed manner and preparation and use thereof
  • Nanoparticle liposome for releasing different medicines in programmed manner and preparation and use thereof
  • Nanoparticle liposome for releasing different medicines in programmed manner and preparation and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0039] Embodiment 1: Preparation of DMAB modified doxorubicin nanoparticles

[0040] Get 100mg didodecyl dimethyl ammonium bromide preparation mass concentration and be 0.5% didodecyl dimethyl ammonium bromide aqueous solution 20mL, the mass ratio of lactide and glycolide in polylactic acid glycolic acid copolymer 50:50, 200 mg of poly(lactic-co-glycolic acid) copolymer with a molecular weight of 8000, 10 mg of doxorubicin were dissolved in 10 mL of ethyl acetate, emulsified and homogenized at 7000 r / min for 15 minutes, added distilled water to 100 mL, dispersed the emulsified system, dispersed After rotary evaporation, remove the organic solvent, centrifuge at 30000r / min for 30min, remove excess didodecyldimethylammonium bromide, discard the supernatant, wash with distilled water three times, and freeze-dry to obtain the doxorubicin-loaded nano Capsule 120mg.

Embodiment 2

[0041] Embodiment 2: Preparation of DMAB modified doxorubicin nanoparticles

[0042] Get 200mg of dodecyl dimethyl ammonium bromide preparation concentration and be 1% didodecyl dimethyl ammonium bromide aqueous solution 20mL, the mass ratio of lactide and glycolide in polylactic acid glycolic acid copolymer is 75 : 25, the molecular weight is 60000 poly(lactic-co-glycolic acid) copolymer 300mg, 10mg doxorubicin is dissolved in 10mL acetone, 10000r / min emulsifies and homogenizes for 15 minutes, adds distilled water and settles to 100mL, disperses the emulsified system, rotatively evaporates after dispersion, Remove the organic solvent, centrifuge at 30,000 r / min for 45 minutes, remove excess didodecyldimethylammonium bromide, discard the supernatant, wash with distilled water three times, and freeze-dry to obtain 210 mg of doxorubicin nanoparticles.

Embodiment 3

[0043] Embodiment 3: Preparation of DMAB modified doxorubicin nanoparticles

[0044] Get 800mg didodecyl dimethyl ammonium bromide preparation concentration and be 2% didodecyl dimethyl ammonium bromide aqueous solution 40mL, make the mass ratio of lactide and glycolide in the polylactic acid glycolic acid copolymer 25 : 75, the molecular weight is 100000 poly(lactic-co-glycolic acid) copolymer 2300mg, 10mg doxorubicin is dissolved in 20mL acetone, 15000r / min is emulsified and homogenized for 15 minutes, distilled water is added and the volume is adjusted to 250mL, the emulsified system is dispersed, and rotary evaporation after dispersion, Remove the organic solvent, centrifuge at 60,000 r / min to remove excess didodecyldimethylammonium bromide, discard the supernatant, wash with distilled water three times, and freeze-dry to obtain 1.5 g of doxorubicin nanoparticles.

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Abstract

The invention discloses a nanoparticle liposome for releasing different medicines in programmed manner and preparation and use thereof. The nanoparticle liposome is mainly prepared from the following components in part by mass: 19.34 to 50.79 parts of polylactic-co-glycolic acid, 5.78to 25.73 parts of dihydroartemisinin and phospholipid composite, 0.01 to 25.27 parts of phospholipid, 0.01 to 15.38 parts of didodecyldimethylammonium bromide, 0.01 to 20.0 parts of cholesterol, and 0.01 to 10.16 parts of adriamycin, wherein the molecular weight of the polylactic-co-glycolic acid is 5,000 to 300,000, and the phospholipid is natural phospholipid or synthetic phospholipid. The nanoparticle liposome for loading medicines of different natures can be used for treating breast cancer and leukocythemia, which have resistance to adriamycin, inverse the medicine resistance of tumors, improve the utilization rate of medicines and reduce pain in patients and the medical cost of patients.

Description

(1) Technical field [0001] The invention relates to a nanoparticle liposome and its preparation and application, in particular to a nanoparticle liposome for programmed release of various medicines and its preparation and application. (2) Background technology [0002] Tumor multidrug resistance (multidrug resistance, MDR) refers to the resistance of a drug to the tumor for a long time, which will cause cross-resistance to other anti-tumor drugs. The resulting multidrug resistance involves multi-purpose anti-tumor drugs commonly used in clinical practice, and is the key to the success of tumor treatment. Therefore, it has always been a hot spot in tumor treatment research, but there is no effective solution yet. [0003] Artemisinin is a peroxybridged sesquiterpene lactone compound extracted and isolated from the leaves of Artemisia annua by Chinese pharmaceutical workers in 1971. Dihydroartemisinin (DHA) is artemisinin Artemisinin and its derivatives are the final active m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K31/357A61K47/24A61K9/127A61P35/00A61P35/02A61P15/14
Inventor 金一李博李贞王成润
Owner ZHEJIANG UNIV
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