Self-assembled nano-drug as well as preparation method and application thereof

A nanomedicine and self-assembly technology, applied in nanomedicine, nanotechnology, nanotechnology and other directions, can solve problems such as increasing safety risks, affecting biological functions, organ damage, etc. antitumor effect

Active Publication Date: 2021-02-23
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

More importantly, the carrier material may have additional toxicity, which may cause damage to normal organs and affect the function of the organism. Its metabolism and clearance in the organism need to be further studied, which greatly increases the potential safety risk.
Therefore, it is still a huge challenge to realize the transformation of nano drug delivery system to clinical application.

Method used

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  • Self-assembled nano-drug as well as preparation method and application thereof
  • Self-assembled nano-drug as well as preparation method and application thereof
  • Self-assembled nano-drug as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Example 1 Preparation process of dasatinib self-assembled nanomedicine.

[0073] Dissolve 1 mg of dasatinib in 0.1 mL of dimethyl sulfoxide (DMSO) to prepare a 10 mg / mL organic solution; under ultrasonic vibration, slowly inject 0.1 mL of dasatinib into 0.9 mL of DMSO solution. In ultrapure water, the solution is mixed uniformly and self-assembles rapidly to form nano-drugs. The residual DMSO was removed by dialysis, and the obtained drug nanoparticles were further collected by centrifugation or lyophilization; washed with PBS, and finally uniformly dispersed in 1 mL of PBS to obtain dasatinib self-assembled nanomedicine.

[0074] figure 2 This is the scanning electron microscope image of the self-assembled nanomedicine of dasatinib prepared in Example 1 dispersed in PBS, which intuitively shows regular spherical morphology, uniform particle size and high dispersibility.

[0075] image 3 This is a photo of the dasatinib self-assembled nano-drug dispersion prepared ...

Embodiment 2

[0078] Example 2 The formation and preparation process of cabazitaxel and dasatinib spontaneously forming spherical ordered structures.

[0079] Dissolve 2 mg of cabazitaxel in 0.1 mL DMSO to prepare a first solution of 20 mg / mL; dissolve 2 mg of dasatinib in 0.1 mL of DMSO to prepare a second solution of 20 mg / mL; mix the first solution with the first solution. The two solutions were mixed evenly by volume 1:1. Under ultrasonic vibration, 0.2 mL of DMSO solution mixed with the two drugs was slowly poured into 1.8 mL of ultrapure water, so that the solution was evenly mixed and self-assembled rapidly to form nano-drugs; centrifugation Collected (50000g, 30min) to obtain the precipitate of drug nanoparticles, washed with PBS, and finally uniformly dispersed in 2 mL of PBS to obtain cabazitaxel-dasatinib co-assembled nanomedicine.

[0080] Image 6 This is the scanning electron microscope image of the cabazitaxel-dasatinib co-assembled nanomedicine synthesized in Example 2, whi...

Embodiment 3

[0083] Example 3 Preparation process of govatinib self-assembled nanomedicine.

[0084]Dissolve 1 mg of govatinib in 0.1 mL of DMSO to prepare a 10 mg / mL organic solution; under ultrasonic vibration, slowly inject 0.1 mL of govatinib in DMSO into 0.9 mL of ultrapure water to mix the solutions Uniform and rapid self-assembly occurs to form nanomedicines. The residual DMSO was removed by dialysis, and the obtained drug nanoparticles were further collected by centrifugation or freeze-drying; washed with PBS, and finally uniformly dispersed in 1 mL of PBS to obtain govatinib self-assembled nano-drug dispersion.

[0085] Figure 9 This is a photo of the self-assembled nano-drug dispersion of govatinib in Example 2. A clear and transparent solution can be observed, and the solution is left standing for 6 hours without precipitation.

[0086] Figure 10 It is the particle size distribution diagram of the govatinib self-assembled nanomedicine prepared in Example 2. It can be seen t...

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Abstract

The invention discloses a self-assembled nano-drug of a single drug of molecular targeted drugs, a co-assembled nano-drug of molecular targeted drugs and other hydrophobic drugs, a preparation methodand an application thereof. Meanwhile, all drugs used have been approved by the US FDA for market use and have good application prospects. The nanoparticle is formed by single-drug self-assembly of molecular targeted drugs, multi-drug co-assembly of molecular targeted drugs and hydrophobic drugs, does not need an additional carrier, has a passive targeting effect, and is easy to stay at a tumor site through an EPR effect, so that the toxic and side effects of the drugs on normal tissues are greatly reduced.

Description

technical field [0001] The invention belongs to the technical field of drug nanometerization, and in particular relates to a novel nanometer formulation with high dispersibility, stability, no need for additional carriers, and each component of which is an FDA-approved drug, as well as a preparation method and application thereof. Background technique [0002] In order to solve the shortcomings of small molecule anticancer drugs, especially hydrophobic drugs, such as short circulation cycle in vivo, low tumor targeting, and easy exposure to normal tissues, researchers have designed a variety of drug delivery systems to combine small molecule anticancer drugs. The drug is loaded inside the nanocarrier particles, thereby prolonging the residence time of the drug in the body, imparting active or passive targeting ability and realizing the controlled release of the drug. [0003] However, the construction of carrier-dependent nano-drug delivery systems often involves complex syn...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K45/00A61K9/19A61K47/06A61P35/00B82Y5/00B82Y40/00
CPCA61K9/5123A61K45/00B82Y5/00B82Y40/00A61P35/00A61K9/5192A61K9/19
Inventor 王杭祥陈晓娜
Owner ZHEJIANG UNIV
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