A hyaluronic acid-docetaxel conjugate modified by dendrimers and its preparation method

A technology of docetaxel and hyaluronic acid, which is applied in the field of hyaluronic acid-docetaxel conjugates, can solve the problems of short residence time, high toxicity and side effects, and poor water solubility, so as to improve the therapeutic effect, prolong the circulation time, The effect of improving stability

Active Publication Date: 2022-03-08
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although DTX shows an encouraging anti-tumor efficacy, it has the same limitations as other small molecule chemotherapy drugs, such as poor water solubility, lack of targeting, short residence time in the body, and high toxicity.

Method used

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  • A hyaluronic acid-docetaxel conjugate modified by dendrimers and its preparation method
  • A hyaluronic acid-docetaxel conjugate modified by dendrimers and its preparation method
  • A hyaluronic acid-docetaxel conjugate modified by dendrimers and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] A dendrimer-modified hyaluronic acid-docetaxel conjugate, the conjugate is hyaluronic acid loaded with docetaxel and a dendrimer, and the structure is as follows:

[0042]

[0043] Wherein, n is selected from 0, 1, 2, 3, 4, 5....

Embodiment 2

[0045] This embodiment is on the basis of embodiment 1:

[0046] The particle size of the conjugate is 118-126nm.

[0047] The molecular weight of the hyaluronic acid is 48000Da.

Embodiment 3

[0049]Synthesis of dendrimer-modified hyaluronic acid-docetaxel conjugates:

[0050]

[0051] Introduce aminoethanethiol on the hyaluronic acid as the carrier to obtain HA-SH for later use; couple the maleimide-modified GFLG with docetaxel to obtain the conjugate Mal-GFLG-DTX, and then pass the thiol -Ene click reaction to connect Mal-GFLG-DTX to HA-SH to obtain a conjugate intermediate; then connect the saccharified dendron-8Glu to the sulfhydryl group on hyaluronic acid through sulfhydryl exchange reaction to obtain the finished product .

[0052] The synthesis method of HA-SH and Dendron-8Glu refers to "Glycodendron / pyropheophorbide-a(Ppa)-functionalized hyaluronic acid as a nanosystem for tumor photodynamic therapy" (Carbohydrate Polymers, 2020, 247, 116749).

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Abstract

The present invention provides a dendrimer-modified hyaluronic acid-docetaxel conjugate, which is hyaluronic acid loaded with docetaxel and dendrimers, designed and synthesized with CD44 targeting The nanoparticle delivery carrier based on hyaluronic acid effectively improves the therapeutic effect of docetaxel on triple-negative breast cancer.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a dendrimer-modified hyaluronic acid-docetaxel conjugate. Background technique [0002] Triple-negative breast cancer (TNBC) is a highly aggressive, highly metastatic systemic disease. Chemotherapy, as a long-term standard treatment for primary and metastatic tumors, is expected to achieve better therapeutic outcomes in TNBC treatment. Nanoparticles with active targeting function have become a research hotspot. By using the tumor microenvironment or the specificity of tumor cells, the specific delivery of drugs to tumor sites can be achieved, so as to achieve localized and efficient therapeutic effects and improve drug biosafety. sex. [0003] The transmembrane protein CD44 on the cell surface is closely related to the occurrence and development of tumors, and is highly expressed in many TNBC cells, which is closely related to the high invasion and high metastasis of TNBC. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/08A61K31/337A61K47/61A61K47/64A61K47/69A61P35/00
CPCC08B37/0072A61K47/61A61K47/641A61K47/6939A61K31/337A61P35/00
Inventor 罗奎张孝琴
Owner SICHUAN UNIV
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