Binary drug loading nanoparticle with pH response and tumor targeting effect as well as preparation method and application thereof

A tumor-targeting and nanoparticle technology, which is applied in the direction of anti-tumor drugs, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of reducing the generality of the method and increasing the difficulty of synthesis, and achieve good therapeutic effects. Method Simple, Adaptable Effects

Inactive Publication Date: 2017-10-10
SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The targeted molecular modification of the surface of nanoparticles is the key technology. The methods of directly modifying the surface of nanoparticles and pre-preparing polymer-targeted molecule copolymers have the following d

Method used

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  • Binary drug loading nanoparticle with pH response and tumor targeting effect as well as preparation method and application thereof
  • Binary drug loading nanoparticle with pH response and tumor targeting effect as well as preparation method and application thereof
  • Binary drug loading nanoparticle with pH response and tumor targeting effect as well as preparation method and application thereof

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Embodiment 1

[0067] A method for preparing folic acid and polydopamine-modified pH-responsive tumor-targeting dual drug-loaded nanoparticles and its application in breast cancer targeted therapy, comprising the following steps:

[0068] (1) Preparation of drug-loaded nanoparticles: weigh 100 mg of cholic acid-polylactic acid-glycolic acid copolymer (CA-PLGA) and 10 mg of docetaxel in proportion, dissolve them in 8 mL of acetone, and stir at room temperature. Add dropwise to 100 mL of 0.03% (w / v) polyethylene glycol vitamin E succinate aqueous solution, continue to stir at room temperature for 12 hours to volatilize acetone, centrifuge at 18,000 rpm for 15 minutes, discard the supernatant, and use deionized water for precipitation Washed 3 times to obtain docetaxel (Docetaxel, DTX)-loaded nanoparticles CA-PLGA / NPs, freeze-dried and set aside;

[0069] (2) Modification of polydopamine: Proportionally, weigh 50 mg of the nanoparticles prepared in (1) and resuspend in 50 mL of 10 mM, pH=8.5 Tr...

Embodiment 2

[0084] A method for preparing folic acid and polydopamine-modified pH-responsive tumor-targeting dual drug-loaded nanoparticles and its application in breast cancer targeted therapy, comprising the following steps:

[0085] (1) Preparation of drug-loaded nanoparticles: weigh 100 mg of cholic acid-polylactic acid-glycolic acid copolymer (CA-PLGA), 2 mg of coumarin-6, dissolve in 8 mL of acetone, and stir at room temperature Add dropwise to 100mL of 0.03% (w / v) polyethylene glycol vitamin E succinate aqueous solution, continue to stir at room temperature for 12 hours to volatilize acetone, centrifuge at 18000rpm for 15 minutes, discard the supernatant, and use the precipitate Washing with deionized water 3 times to obtain nanoparticles CA-PLGA / NPs loaded with coumarin-6 (Coumarin-6, C6), freeze-dried and set aside;

[0086] (2) Modification of polydopamine: Proportionally, weigh 50 mg of the nanoparticles prepared in (1) and resuspend in 50 mL of 10 mM, pH=8.5 Tris buffer, weigh...

Embodiment 3

[0092] A method for preparing folic acid and polydopamine-modified pH-responsive tumor-targeting dual drug-loaded nanoparticles, comprising the following steps:

[0093] (1) Preparation of drug-loaded nanoparticles: Weigh 100 mg of polylactic-co-glycolic acid (PLGA) and 10 mg of paclitaxel in proportion, dissolve them in 10 mL of tetrahydrofuran, and add them dropwise to 100 mL of 0.03 % (w / v) polyethylene glycol vitamin E succinate aqueous solution, continue stirring at room temperature for 12 hours to volatilize tetrahydrofuran, centrifuge at 18000 rpm for 15 minutes, discard the supernatant, and wash the precipitate with deionized water 3 times to obtain paclitaxel (Paclitaxel, PTX) nanoparticles PLGA / NPs, freeze-dried for subsequent use;

[0094] (2) Modification of polydopamine: according to the ratio, weigh 50 mg of the nanoparticles prepared in (1) and resuspend in 50 mL of 10 mM Tris buffer solution with pH=8.5, weigh 10 mg of dopamine hydrochloride, and stir at room t...

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Abstract

The invention discloses a folic acid and polydopamine modified tumor-targeted binary drug loading nanoparticle with pH response as well as a preparation method and an application thereof. The preparation method comprises the following steps: (1) preparing hydrophobic drug loading nanoparticles; (2) modification of polydopamine; (3) modification of targeted ligand folic acid; and (4) a binary drug loading process of the pH response. The method disclosed by the invention is simple and wide in adaptability, and the prepared nanoparticle has good biocompatibility, biodegradability and target properties of multiple tumors; and due to the binary drug loading and pH response characteristics, the nanoparticle has an excellent treatment effect.

Description

technical field [0001] The invention relates to a pH-responsive and tumor-targeting double drug-loaded nanoparticle, a preparation method and an application. Background technique [0002] In recent years, cancer has become a major clinical fatal disease, and general tumor therapy mainly includes surgery, chemotherapy and radiotherapy. Although these therapies are still clinically effective methods, some of their shortcomings are worth noting: invasive treatment methods and various side effects often bring great pain to patients; traditional drug delivery methods make small molecules Drugs are randomly distributed in the body and cannot be effectively enriched in the tumor site, and a large amount of medication will bring drug resistance; these treatments cannot distinguish between normal cells and tumor cells, so that the randomly distributed drugs in the body can kill tumor cells while killing other normal cells. damage to cells. [0003] Drug delivery based on targeted n...

Claims

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Application Information

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IPC IPC(8): A61K47/59A61K47/54A61K47/60A61K47/69A61K9/14A61K47/34A61K9/51A61K38/05A61P35/00A61K31/337A61K33/24A61K31/428
CPCA61K9/146A61K9/5146A61K31/337A61K31/428A61K33/24A61K38/05A61K2300/00
Inventor 梅林曾小伟黄来强聂俊鹏程伟
Owner SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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