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Polyethylene glycol-poly(lactic-co-glycolic acid)-polylysine nano-delivery system, preparation method and application thereof

一种聚乳酸羟基乙酸、聚赖氨酸阳的技术，应用在乳状液输送、其他插入外来遗传材料的方法、胶囊输送等方向，能够解决化疗药物缺乏选择性、肿瘤细胞抗药性快速出现、剂量依赖性毒副作用等问题

Active Publication Date: 2012-07-25
SUNSHARES (SHANGHAI) TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A major problem is the general lack of selectivity of chemotherapy drugs, leading to serious dose-dependent side effects, which greatly limits the clinical therapeutic effect of chemotherapy drugs
Another concern is the rapid emergence of drug resistance in tumor cells

Method used

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  • Polyethylene glycol-poly(lactic-co-glycolic acid)-polylysine nano-delivery system, preparation method and application thereof
  • Polyethylene glycol-poly(lactic-co-glycolic acid)-polylysine nano-delivery system, preparation method and application thereof
  • Polyethylene glycol-poly(lactic-co-glycolic acid)-polylysine nano-delivery system, preparation method and application thereof

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Embodiment 1

[0044] The present invention is further described below with embodiment, but content of the present invention is not limited. Embodiment 1, preparation of polyethylene glycol monomethyl ether-polylactic acid glycolic acid-polylysine (mPEG-PLGA-PLL) (1) polyethylene glycol monomethyl ether-polylactic acid glycolic acid (mPEG-PLGA) Preparation: heat-resistant glass tube is heated and dried in vacuum, lactide / glycolide raw material with a certain molar mass ratio (ratio of 8:2, 7:3, 6:4, 5:5) is added, and the proportion of total raw material is added Add PEG with a mass percentage of 1% to 20% and a molecular weight range of 350 to 5000, then add a catalyst, pass nitrogen, heat to dissolve and vacuumize, cool and solidify, vacuumize for 2 hours, seal the tube, and react at 120-150°C for 8-50h. (2) Preparation of polyethylene glycol monomethyl ether-polylactic acid glycolic acid-tert-butoxycarbonyl (mPEG-PLGA-Boc(Z)): dissolve a certain amount of mPEG-PLGA in a dry organic solven...

Embodiment 2

[0046] Example 2, preparation of mPEG-PLGA-PLL nanoparticles loaded with mitoxantrone hydrochloride drug

[0047] Prepared by emulsification evaporation method, take the material mPEG-PLGA-PLL and dissolve it in dichloromethane or a mixed solvent of dichloromethane and acetone, add the aqueous solution of mitoxantrone hydrochloride, after ultrasonic emulsification, then add it into the aqueous solution containing F68, again ultrasound. Then stir at room temperature for 0.5-5h to remove the organic phase to obtain nanoparticle suspension. The particle size of the nanoparticles prepared above is controlled at 10-1000nm.

[0048] It is prepared by thin film emulsification method. The material mPEG-PLGA-PLL and mitoxantrone hydrochloride are dissolved in acetone solvent, and rotated to evaporate to form a film. Then add a certain amount of aqueous solution and stir at room temperature for 0.5-6h to obtain a nanoparticle suspension. . The particle size of the nanoparticles prepa...

Embodiment 3

[0050] Prepared by interfacial precipitation method, the material mPEG-PLGA-PLL and mitoxantrone hydrochloride were dissolved in acetone solvent, and at a certain stirring speed, the above solution was injected into a certain concentration and volume of polyvinyl alcohol (PVA) solution, pressurized The acetone is removed by volatilization, and the nanoparticle suspension is obtained. The particle size of the nanoparticles prepared above is controlled at 10-1000nm. Embodiment 3, the preparation of the mPEG-PLGA-PLL nanoparticle of carrying gene

[0051] Preparation by emulsification evaporation method: take the material mPEG-PLGA-PLL and dissolve it in dichloromethane or a mixed solvent of dichloromethane and acetone, add it into an aqueous solution containing F68 and sonicate. Then stir at room temperature for 0.5-5h to remove the organic phase to obtain mPEG-PLGA-PLL nanoparticle solution. An appropriate amount of mPEG-PLGA-PLL nanoparticle solution was added dropwise to an...

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Abstract

The invention belongs to the nanotechnical field, and discloses preparation of a methoxy polyethylene glycol-poly(lactic-co-glycolic acid)-polylysine(mPEG-PLGA-PLL) cationic polymer nano-drug delivery system and application thereof. The nano-drug delivery system can have multi-functional characteristics such as tumor targeting, reversing drug resistance and medical diagnosis functions through modification, and can be used for supporting organic medicaments, water-soluble medicaments, non-water-soluble medicaments, or developers for diagnosis. The preparation method is simple and convenient, is suitable for mass production, and is particularly suitable for the preparation of targeting drug delivery systems.

Description

technical field [0001] The invention belongs to the technical field of tumor targeted delivery and sustained release drug delivery system. Specifically, it is a nano drug delivery system with polyethylene glycol monomethyl ether-polylactic acid glycolic acid-polylysine (mPEG-PLGA-PLL) cationic polymer as the skeleton, a preparation method and its application in medicine. Background of the invention [0002] The clinical application of chemotherapy drugs to treat malignant tumors has achieved certain success in many cases, but there are also some serious problems. A major problem is that chemotherapeutic drugs generally lack selectivity, leading to serious dose-dependent side effects, which greatly limits the clinical therapeutic effect of chemotherapeutic drugs. Another problem is the rapid emergence of drug resistance in tumor cells. Therefore, the development of therapeutic methods that can specifically target tumor cells and cause minimal damage to normal cells has very...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K48/00A61K49/00A61K49/12A61K49/18A61K49/22A61K9/14A61P35/00
CPCC08G69/10A61K47/48907C08G63/664C08G2261/126C12N15/87A61K47/48238C08G63/6852C08G69/44A61K9/5153A61K48/0041C08G63/912A61K47/62A61K47/6935A61P35/00
Inventor 段友容孙颖刘培峰于晖亓雪莲王琪陈晓炎李晓昱
Owner SUNSHARES (SHANGHAI) TECH CO LTD
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