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A kind of self-assembled nano medicine and its preparation method and application

A nano-drug and self-assembly technology, applied in the direction of nano-drugs, drug combinations, nanotechnology, etc., can solve problems such as increasing safety risks, organ damage, affecting biological functions, etc., and achieve the effect of improving solubility and broad application prospects

Active Publication Date: 2022-04-22
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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  • A kind of self-assembled nano medicine and its preparation method and application
  • A kind of self-assembled nano medicine and its preparation method and application
  • A kind of self-assembled nano medicine and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Example 1 The 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; slowly inject 0.1 mL of the DMSO solution of Dasatinib into 0.9 mL of In ultrapure water, the solution is mixed evenly and self-assembles rapidly to form nano-medicines. Dialysis was used to remove residual DMSO, and the obtained drug nanoparticles were further collected by centrifugation or freeze-drying; washed with PBS, and finally uniformly dispersed in 1 mL of LPBS to obtain dasatinib self-assembled nano-medicine.

[0074] figure 2 It is a scanning electron microscope image of the self-assembled nano-medicine of dasatinib dispersed in PBS prepared in Example 1, visually showing regular spherical morphology, uniform particle size and high dispersibility.

[0075] image 3 It is a photo of the Dasatinib self-assembled nano-drug dispersion prepared in Example 1 (see the left f...

Embodiment 2

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

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

[0080] Figure 6 It is the scanning electron microscope picture of the cabazitaxel-dasatinib co-assembled nano-medicine synthesized in Example 2, which visually shows regular spherical morpholog...

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 solution Uniform and rapid self-assembly to form nanomedicines. Dialysis was used to remove residual DMSO, and the obtained drug nanoparticles were further collected by centrifugation or freeze-drying; washed with PBS, and finally uniformly dispersed in 1 mL of LPBS to obtain govatinib self-assembled nano-drug dispersion.

[0085] Figure 9 It is a photo of the govatinib self-assembled nano-medicine dispersion 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 nano-medicine prepared in Example 2. It can be seen that the...

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Abstract

The invention discloses a single-drug self-assembly of a molecular-targeted drug, a co-assembled nanometer drug of a molecular-targeted drug and other hydrophobic drugs, a preparation method and an application thereof. At the same time, the drugs used have been approved by the US FDA for marketing, and have good application prospects. Molecular targeted drug single-drug self-assembly, molecular targeted drug and hydrophobic drug multi-drug co-assembly to form nanoparticles, without additional carrier, has passive targeting effect, and is easy to stay in the tumor site through the EPR effect, thereby greatly reducing drug interaction. Toxic side effects of normal tissues.

Description

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

Claims

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Application Information

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Patent Type & Authority Patents(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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