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Nano preparation for treating multidrug resistance tumours, composition and application of nano preparation and composition

A nano-preparation and multi-drug resistance technology, applied in the field of anti-tumor drugs, can solve the problems of paclitaxel's clinical application value reduction, tumor drug resistance and other problems, achieve good plasma stability, improve biocompatibility, and high quality of life Effect

Pending Publication Date: 2021-10-08
LINYI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in clinical application, it is very easy to cause tumor drug resistance (MDR), which in turn leads to a great reduction in the clinical application value of paclitaxel.

Method used

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  • Nano preparation for treating multidrug resistance tumours, composition and application of nano preparation and composition
  • Nano preparation for treating multidrug resistance tumours, composition and application of nano preparation and composition
  • Nano preparation for treating multidrug resistance tumours, composition and application of nano preparation and composition

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preparation example Construction

[0043] The second aspect of the present invention provides the preparation method of the nano-preparation for the treatment of multidrug-resistant tumors in the first aspect, the preparation method comprising: dispersing the drug in the lipid material to obtain a drug-loaded lipid core solution, and adding the drug-loaded lipid Targeting materials are added to the core solution for incubation to obtain the biomimetic sugar-lipid or biomimetic lipoprotein-structure nano preparation.

[0044] Preferably, the specific steps of the preparation method are as follows: add paclitaxel, resveratrol and lipid materials into an organic solvent to dissolve, evaporate the organic solvent to form a drug-containing film, add a buffer solution to the drug-containing film for ultrasonic hydration Obtain a drug-loaded lipid core solution; add targeting materials and incubate with stirring for 12-48 hours to obtain biomimetic sugar-lipid or biomimetic lipoprotein-structure nano preparations.

[...

Embodiment 1

[0058] Example 1 Co-loaded Paclitaxel and Resveratrol Nano-Preparation Preparation

[0059] (1) The amount of dioleoylphosphatidylethanolamine (DOPE) taken by weighing is 60mg, cholesterol hemisuccinate 15mg, cholesterol is 12mg, and total drug dose is 10mg, wherein, paclitaxel: resveratrol is 5:1 (w / w). Put the above raw materials into a 150mL eggplant-shaped bottle, add 10mL of absolute ethanol to dissolve, and spin dry at 37°C to form a film; then add 15mL of PBS, hydrate at 37°C for 20min; 150w probe and ultrasonic for 5min in an ice bath.

[0060] (2) Dissolve the epidermal growth factor with PBS (pH 7.4) to a solution with a concentration of 1 mg / mL, slowly add the above-mentioned epidermal growth factor solution to the above solution (1) under stirring conditions and continue to stir and incubate at a stirring rate of 30r / min (magnetic stirring), and incubated at 37°C for 24h to obtain the nano-preparation.

Embodiment 2

[0061] Example 2 Co-loaded Paclitaxel and Resveratrol Nano-Preparation Preparation

[0062] (1) The amount of dioleoylphosphatidylethanolamine (DOPE) taken by weighing is 62mg, cholesterol hemisuccinate 16mg, cholesterol is 13mg, and total drug dose is 12mg, wherein, paclitaxel: resveratrol is 4:1 (w / w). Put the above-mentioned raw materials into a 150mL eggplant-shaped bottle, add 15mL of absolute ethanol to dissolve, and spin evaporate to dryness under reduced pressure at 37°C to form a film; then add 15mL of PBS, hydrate at 37°C for 15min; 150w probe and sonicate in an ice bath for 8min.

[0063] (2) Dissolve the epidermal growth factor into a solution with a concentration of 1.2mg / mL with PBS (pH 7.4), slowly add the above-mentioned epidermal growth factor solution into the above-mentioned (1) solution under stirring conditions and continue to stir and incubate at a stirring rate of 30r / min (magnetic stirring), incubate at 37°C for 24h to obtain the nano-preparation.

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Abstract

The invention relates to a nano preparation for treating multidrug resistance tumours, a composition and application of the nano preparation and the composition. Tumour drug resistance is a main reason of current clinical chemotherapy failure; and in order to realize a drug resistance tumour reversal effect, the invention provides a nano preparation for drug resistance tumours and a preparation method of the nano preparation, wherein the nano preparation is a pharmaceutical composition of paclitaxel and resveratrol; and the nano preparation with a bionic structure is constructed through a pH-sensitive lipid material and a targeting material. Through verification, the nano preparation has a good entrapment effect and physicochemical properties, and shows good pH responsiveness in in-vitro release. Animal experiments prove that the nano preparation can effectively inhibit the tumour development process, is higher in safety when applied to animal bodies, is expected to be applied to clinical treatment and overcomes the defects of chemical medicine treatment.

Description

technical field [0001] The invention belongs to the technical field of anti-tumor drugs, and in particular relates to a nano-preparation for treating multidrug-resistant tumors and a preparation method, a composition containing the nano-preparation, and the use of the nano-preparation and the composition in preparing anti-tumor products application. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Cancer has become one of the main diseases that seriously threaten human health. The mortality rate caused by tumors in my country is relatively high, and the incidence rate is on the rise. Tumor multidrug resistance (MDR) is the main obstacle of clinical tumor chemotherapy, and...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K47/42A61K47/36A61K47/26A61K31/337A61K31/05A61P35/00A23L33/105A23L33/115A23L33/125A23L33/17A23L33/18
CPCA61K9/1271A61K9/1277A61K47/24A61K47/28A61K47/42A61K47/36A61K47/26A61K31/337A61K31/05A61P35/00A23L33/105A23L33/115A23L33/125A23L33/17A23L33/18A23V2200/00A61K2300/00A23V2200/308A23V2250/21A23V2250/54A23V2250/60
Inventor 陈聪慧
Owner LINYI UNIVERSITY
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