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Active tumor targeting controlled-release drug nano-micelle and preparation method and application thereof

A tumor-targeting, nanomicelle technology, applied in the field of biological and medical nanomaterials, can solve the problems of poor tissue selectivity, limit the clinical application of photodynamic therapy, aggregation-induced quenching, etc., to overcome poor water solubility and increase retention time in vivo , increase the effect of accumulation

Pending Publication Date: 2022-02-25
XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The purpose of the present invention is to provide an active tumor-targeting controllable release drug nanomicelle and its preparation method and application, so as to solve the problems of poor tissue selectivity and aggregation-induced quenching of traditional photosensitizers used in existing anti-tumor related drugs. Insufficient, which largely limits the clinical application of photodynamic therapy
[0008] In order to achieve the above-mentioned active tumor-targeted and controlled-release drug nanomicelles and their preparation methods, the application of traditional photosensitizers used in existing anti-tumor drugs has poor tissue selectivity, aggregation-induced quenching and other deficiencies, which are largely limited. To solve the problem of the clinical application of photodynamic therapy, the present invention provides the following technical solutions:

Method used

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  • Active tumor targeting controlled-release drug nano-micelle and preparation method and application thereof
  • Active tumor targeting controlled-release drug nano-micelle and preparation method and application thereof
  • Active tumor targeting controlled-release drug nano-micelle and preparation method and application thereof

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Embodiment 1

[0033] Embodiment 1. The present invention provides a nanomicelle with active tumor targeting and controlled release of drugs. The nanomicelle uses PEG-TK-PLGA as the basic skeleton and has cRGD modification on the surface.

[0034] Poly(lactic-co-glycolic acid) (PLGA) is the most commonly used biodegradable polymeric drug delivery vehicle today. In order to construct stimuli-responsive nanocarriers, the controlled-release drug nanosystems constructed with PLGA-based polymers have received a lot of attention. The thioketal bond (TK) can be specifically broken in response to the stimulation of reactive oxygen species, so as to achieve the localization of the tumor site and release chemotherapy drugs, effectively improving the utilization of anti-tumor drugs. In addition, polyethylene glycol (PEG) is a polymer material widely used for covalent modification of biopolymers such as proteins and peptides. PEG has the advantages of non-toxicity, non-immunogenicity, non-antigenicity,...

Embodiment 2

[0037] Example 2. Synthesis of nanomicelles that can actively target tumors in response to ROS stimulation

[0038] Concrete preparation method comprises the following steps:

[0039] (1) Synthesis of cRGD-PEG-TK-PLGA: The cRGD polypeptide is coupled with NHS-PEG-TK-PLGA through amidation reaction, and its synthetic route is as follows figure 1 As shown in A, 5 ml of NHS-PEG-TK-PLGA in dimethylformamide (DMF) was mixed into a DMF solution containing cRGD polypeptide (20 mg, 0.033 mmol). After reacting at room temperature for 24 hours, it was purified by ultrapure water dialysis (MWCO 3500) for 48 hours, and then freeze-dried to obtain cRGD-PEG-TK-PLGA. Coupling rate: 74.6%.

[0040] (2) Synthesis of ROS-responsive nanomicelles that can actively target tumors: PEG-TK-PLGA (9 mg) and cRGD-PEG-TK-PLGA (1 mg) were dissolved in THF / CHCl3 (v / v=1 :1, 1.5mL) solvent, and then slowly added ultrapure water (8.5mL). Then, it was dialyzed against ultrapure water for 1 d to prepare ROS...

Embodiment 3

[0042] Example 3, Synthesis of nanomicelles loaded with AIE photosensitizer (TB) and (or) chemotherapeutic drug paclitaxel (PTX) capable of active tumor targeting

[0043] (1) Synthesis of TB@RTK nanomicelles: PEG-TK-PLGA (9 mg), cRGD-PEG-TK-PLGA (1 mg) and AIE photosensitizer (TB) (1 mg) were dissolved in THF / CHCl3 (volume ratio v / v=1:1, 1.5mL) solvent, dissolved in the dark, and then slowly added ultrapure water (8.5mL). Then, it was dialyzed against ultrapure water for 1 d to prepare nanomicelles (TB@RTK) loaded with AIE photosensitizer (TB) with active tumor targeting. The detection result of high performance liquid chromatography showed that its drug loading was 7.43%.

[0044] (2) Synthesis of PTX@RTK nanomicelles: PEG-TK-PLGA (9mg), cRGD-PEG-TK-PLGA (1mg) and PTX (1mg) were dissolved in THF / CHCl3 (v / v=1:1 , 1.5 mL) solvent, and then slowly added ultrapure water (8.5 mL). Then, it was dialyzed with ultrapure water for 1 d to prepare nanomicelles (PTX@RTK) loaded with ...

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Abstract

The invention discloses an active tumor targeting controlled-release drug nano-micelle and a preparation method and application thereof. According to the cRGD-PEG-TK-PLGA polymer, PEG-TK-PLGA is adopted as a basic framework, cRGD modification is performed on the basic framework, the obtained amphiphilic polymer can be subjected to a self-assembly process in a water-based medium to form an active tumor targeting controlled-release drug nano-micelle entrapped with a hydrophobic drug, PLGA is a degradable functional polymer organic compound, and has good biocompatibility, no toxicity and good film forming performance; an ROS sensitive group thioketal bond (TK) is introduced into the carrier, so that the nano system is endowed with an ROS-triggered drug release behavior, and rapid, sufficient and accurate drug release in tumor cells is ensured; PEGylation modification can prolong the in-vivo retention time of the nano drug delivery system, improve the half-life period of plasma and increase the accumulation of tumor sites.

Description

technical field [0001] The invention relates to the technical field of biological and medical nanomaterials, in particular to an active tumor targeting controllable drug release nanomicelle and its preparation method and application. Background technique [0002] In recent years, the morbidity and mortality of malignant tumors have shown an obvious upward trend, and have become a serious threat to people's health, with the characteristics of high mortality and poor prognosis. Currently, chemotherapy is still one of the most common means of tumor treatment in clinic. However, due to its poor tissue selectivity and excessive side effects, chemotherapy still cannot achieve a satisfactory therapeutic effect. In order to solve these problems, researchers have applied nanotechnology to the treatment of tumors in recent years, and constructed various nano-drug delivery systems. Through high permeability and retention effect or active targeting, the drug can be accumulated at the t...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K47/64A61K47/60A61K47/59A61K47/69A61K31/337A61P35/00
CPCA61K41/0057A61K47/64A61K47/60A61K47/593A61K47/6907A61K31/337A61P35/00A61K2300/00
Inventor 高杨易小庆徐剑军胡少勃李素贞余聪苏喆邹天浩王为民周星孙平张陈程翔宋自芳郑启昌
Owner XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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