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Novel nanometer drug and preparation method thereof

A nano-drug and nano-particle technology, used in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of low drug-carrying capacity and drug-carrying efficiency of carriers, affecting biological functions, and difficult to accurately control, and achieve a therapeutic approach. Synergy, guaranteed safety and low cost

Inactive Publication Date: 2018-09-21
SHANGHAI INST OF CERAMIC CHEM & TECH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the preparation of various drug delivery carriers usually requires complex synthetic schemes, including supramolecular self-assembly and chemical modification. These processes are always difficult to precisely control and have poor reproducibility, resulting in extremely low drug-loading capacity and drug-loading efficiency. , limiting its effectiveness in in vitro and in vivo experiments
At the same time, one or more inorganic materials, metal materials, and polymer materials are used in the preparation of the carrier. Although these materials are novel, on the other hand, the interaction between them and the therapeutic drug needs to be further studied, whether it will affect the efficacy of the drug. Efficacy needs to be tested one by one
More importantly, the carrier material may be cytotoxic, which will damage normal organs, affect the function of the organism, and even cause death
Therefore, it is still a huge challenge to realize the transformation of drug delivery system to clinical application.

Method used

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  • Novel nanometer drug and preparation method thereof
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  • Novel nanometer drug and preparation method thereof

Examples

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preparation example Construction

[0053] figure 1 A flow chart showing a process for preparing self-assembled nanomedicines according to an embodiment of the present invention. Such as figure 1 As shown, first, a drug solution is prepared. Specifically, the hydrophobic drug is dissolved in dimethyl sulfoxide to obtain a first solution. Dissolve indocyanine green in water or NaHCO 3 aqueous solution to obtain a second solution.

[0054] In the first solution, the concentration of the hydrophobic drug may be 0.5-2 g / L.

[0055] In the second solution, the concentration of indocyanine green may be 0.2-1 g / L. In the second solution, if NaHCO is used 3 aqueous solution as solvent, NaHCO 3 In aqueous solution, NaHCO 3 The concentration can be 0.02 ~ 5mM.

[0056] Then, the drugs are homogeneously mixed and self-assembled to form nanomedicines. Specifically, the first solution and the second solution are mixed. The mixing process of the two is the process of self-assembly to form nano-medicines.

[0057] ...

Embodiment 1

[0067] Dissolve 1 mg of paclitaxel in 0.1 mL of DMSO to make a 10 mg / mL organic solution; make 1 mg / mL of ICG in NaHCO 3 (0.05mM) aqueous solution; under ultrasonic vibration, 0.1mL paclitaxel DMSO solution was added dropwise to 0.6mL ICG solution at a rate of 20μL every 15s, so that the solution was mixed evenly and self-assembled rapidly to form nano-drugs; centrifugal collection (17000rpm, 30min) to obtain the precipitation of drug nanoparticles; wash with PBS, and finally evenly disperse in 1mL of LPBS.

[0068] figure 2 It is the TEM image of the paclitaxel-ICG self-assembled nano-medicine synthesized in Example 1, which visually shows regular spherical morphology, uniform particle size and high dispersion.

[0069] Figure 10 The particle size distribution diagram of the paclitaxel-ICG self-assembled drug synthesized in Example 1 is shown. It can be seen that the hydration kinetic diameter of the paclitaxel-ICG self-assembled nano-drug is about 100nm, with a single pe...

Embodiment 2

[0072] Dissolve 1 mg camptothecin in 0.1 mL DMSO to prepare a 10 mg / mL organic solution; prepare 1 mg / mL ICG in NaHCO 3 (0.05mM) aqueous solution; under ultrasonic vibration, the DMSO solution of 0.1mL camptothecin was added dropwise to the ICG solution of 0.6mL at a rate of 20 μL every 15s, so that the solution was mixed evenly and self-assembled rapidly to form nano-medicines; Collect by centrifugation (17000rpm, 30min) to obtain the precipitate of drug nanoparticles; wash with PBS, and finally evenly disperse in 1mL of PBS.

[0073] image 3 It is a TEM image of the camptothecin-ICG self-assembled nanomedicine synthesized in Example 2, which visually shows regular spherical morphology, uniform particle size and high dispersion.

[0074] Figure 11 The particle size distribution diagram of the camptothecin-ICG self-assembled drug synthesized in Example 2 is shown. It can be seen that the hydration kinetic diameter of the camptothecin-ICG self-assembled nano drug is about 4...

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Abstract

The invention discloses a novel nanometer drug and a preparation method thereof. The nanometer drug belongs to nanometer particles formed by self-assembling hydrophobic drug and indocyanine green.

Description

technical field [0001] The invention belongs to the technical field of drug nanotechnology, and relates to a novel nano drug with high dispersibility, stability, controllable particle size, no additional carrier, and each component is a drug approved by the U.S. Food and Drug Administration (FDA). its preparation method. Background technique [0002] In order to solve the defects of small-molecule tumor therapeutic drugs, especially hydrophobic drugs, with short circulation period in vivo, low tumor targeting, and easy damage to normal cells, researchers have designed a variety of drug delivery systems to encapsulate small-molecule therapeutic drugs Into the interior of biocompatible nanocarrier particles to achieve long cycle, active or passive targeted and controlled drug release. For example, in 2001, researchers discovered that MCM-41 mesoporous SiO 2 It has efficient drug storage and sustained release properties (Chem. Mat. 2001, 13, (2), 308-311) and good biocompatib...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/22A61K31/337A61K31/4745A61K31/44A61P35/00
CPCA61K9/145A61K31/337A61K31/44A61K31/4745A61P35/00
Inventor 蒋渠子于罗丹陈雨
Owner SHANGHAI INST OF CERAMIC CHEM & TECH CHINESE ACAD OF SCI
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