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Target drug loaded micelle suitable for loading of hydrophobic chemical drugs

A drug-loaded micelle, hydrophobic technology, used in drug combinations, anti-tumor drugs, pharmaceutical formulations, etc., can solve problems such as high cost, complex reaction process, and off-target targeting groups

Active Publication Date: 2019-05-07
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the reaction process of the above method is complicated, especially the latter needs to modify the antibody first, so that it can be modified with a sulfhydryl group that can be linked to maleimide, and the cost is relatively high. Disulfide bonds, and even amide bonds, which have been consistently considered to be more stable, circulate in the blood in vivo [Schumacher D et al., Status: Site-specific antibody-drug conjugates. Journal of Clinical Immunology, 2016, 36, S100-S7. ] Unstable, prone to off-target phenomenon due to the separation of targeting groups and nanoparticles

Method used

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  • Target drug loaded micelle suitable for loading of hydrophobic chemical drugs
  • Target drug loaded micelle suitable for loading of hydrophobic chemical drugs
  • Target drug loaded micelle suitable for loading of hydrophobic chemical drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0123] Embodiment 1 Preparation method of non-targeting nanocrystal micelles (that is, non-targeting drug-loaded micelles)

[0124] The drug loading is the percentage of the mass of paclitaxel to the mass of the polymer carrier material.

[0125] The molecular weight of PCL in the PCL-PEG-CHO used in this example is 5000Da; the molecular weight of PEG is 2000Da. The molecular weight of PCL in the PCL-PEG used in this example is 2000Da; the molecular weight of PEG is 2000Da.

[0126] Specifically, the preparation method of non-targeted drug-loaded micelles comprises the following steps:

[0127]Mix the PCL-PEG-CHO and the PCL-PEG according to the mass ratio of 2:1, then add paclitaxel with 5% of the total mass of PCL-PEG-CHO and PCL-PEG, and co-dissolve in 1ml chloroform and shake until completely dissolved and mix evenly; then add 10ml of deionized water and sonicate in a water bath with 100% power until a white uniform emulsion is formed. Remove the chloroform by rotary ev...

Embodiment 2

[0131] Embodiment 2, the preparation method of targeted nanocrystalline micelles (that is, targeted drug-loaded micelles)

[0132] Targeted drug-loaded micelles using NaCNBH 3 Preparation by reduction method. That is, in phosphate buffered saline solution, the aldehyde groups on the surface of the non-targeted drug-loaded micelles obtained in Example 1 and the primary amino groups on the surface of Herceptin (molar ratio -CHO / -NH2=15:1) pass through The schiff reaction forms a C=N bond, followed by NaCNBH 3 A stable C-N bond is formed under the action, and the reaction is carried out at 2-10°C and 350rpm for 24h, and the obtained targeted drug-loaded micelles are stored at 4°C for future use.

[0133] For details of the reaction diagram, see figure 2 .

Embodiment 3

[0134] Embodiment 3, performance determination of nanocrystalline micelles (comprising blank micelles, non-targeted drug-loaded micelles, targeted drug-loaded micelles)

[0135] 1. Determination of particle size

[0136] The particle size and polydispersity of the blank micelles obtained in Example 1, the non-targeted drug-loaded micelles obtained in Example 1, and the targeted drug-loaded micelles obtained in Example 2 were respectively measured at room temperature using a laser scattering particle size analyzer. coefficient.

[0137] The particle diameter of the blank micelle that embodiment 1 obtains, polydispersity index (PDI) see Figure 3A . For the particle size and polydispersity index (PDI) of the non-targeted drug-loaded micelles obtained in Example 1, see Figure 3B . For the particle size and polydispersity index (PDI) of the targeted drug-loaded micelles obtained in Example 2, see Figure 3C .

[0138] From Figure 3A , Figure 3B and Figure 3C , it ca...

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Abstract

The invention belongs to the technical field of drug transfer, and particularly relates to a target drug loaded micelle suitable for loading of hydrophobic chemical drugs. Amphipathic biodegradable materials (such as PCL-PEG ) and chemical drugs, which are safe to human bodies, are used to form stable nanometer crystallization micelles, so that the biological availability of drugs is improved, thecritical concentration of the micelles is reduced, and the in vitro long-acting cycle is realized; and tumor cells can be efficiently targeted, the chemical drugs enter the cells through receptor mediated endocytosis, and through self degradation, the drugs are released. The united target treatment of antibodies and the chemical drugs is performed on antibody antigen high-expression malignant tumours.

Description

technical field [0001] The invention belongs to the technical field of drug delivery, and in particular relates to a targeted drug-loaded micelle suitable for loading hydrophobic chemical drugs. Background technique [0002] Chemotherapy has been widely used in a variety of diseases today, especially for cancer, which seriously threatens human health, and is an indispensable and effective means. However, most chemical drugs have many problems such as poor water solubility and stability, lack of targeting, and poor distribution selectivity during clinical use, resulting in reduced bioavailability and even serious side effects. Therefore, searching for efficient and low-toxic drug delivery systems has become a research hotspot in related fields. At present, the tumor site delivery of hydrophobic chemical drugs can be roughly divided into the following types: (1) delivery by drug carriers, such as liposomes, polymer micelles, albumin nanoparticles, etc.; (2) microemulsion and ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K47/69A61K47/68A61K31/337A61P35/00
Inventor 杜子秀彭佳惠王红霞徐宇虹
Owner SHANGHAI JIAO TONG UNIV
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