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Cascade targeted medicine delivery system as well as preparation method and application thereof

A delivery system and targeted technology, which can be used in drug delivery, drug combination, pharmaceutical formulations, etc., can solve problems such as drug transport to the lesion site, tumor cell drug resistance, tissue and organ toxicity and side effects, and achieve drug bone marrow enrichment. , Bone marrow enrichment of high-efficiency drugs, overcoming the effect of precise delivery

Active Publication Date: 2018-05-08
苏州影睿光学科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Different from the treatment of other conventional tissue and organ solid tumors, due to the characteristics of bone tissue with high hardness, poor permeability, low blood flow, and the existence of blood-bone marrow barrier (BMB), traditional drug delivery methods are difficult to be effective The drug is transported to the lesion, so it is easy to cause drug resistance of tumor cells and cause serious toxic side effects to other normal tissues and organs

Method used

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  • Cascade targeted medicine delivery system as well as preparation method and application thereof
  • Cascade targeted medicine delivery system as well as preparation method and application thereof
  • Cascade targeted medicine delivery system as well as preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0058] The present invention prepares the cascade targeted drug delivery system of alendronate (Ald) and RGD double modification by the following method

[0059] (1) A pH-sensitive hydrazone bond (COOH-PEG2000-Hyd-PCL) was introduced between PEG 2000 modified with a hydrophilic terminal carboxyl group and hydrophobic polycaprolactone (PCL): (a) Synthesis of acylhydrazide-PEG derivatives : mPEG-SH is dissolved in chloroform, fully reacts with excess acyl hydrazide cross-linking agent MPBH in the presence of triethylamine, and removes unreacted substances by dialysis. After thin-layer chromatography analysis, lyophilize and then disperse in chloroform and store at low temperature; (b) 4-acetylphenylmaleimide activates phospholipids: in the presence of triethylamine, 4-acetylphenylmaleimide Amines and DSPE-SH fully react at room temperature. The activated phospholipids are separated by a silica gel column, and the product fractions are analyzed by thin-layer chromatography, coll...

Embodiment 2

[0064] The present invention prepares aspartic acid hexapeptide (Asp) by the following method 6 Cascade targeted drug delivery system double-modified with cell-penetrating peptide Tat

[0065] (1) A pH-sensitive hydrazone bond (COOH-PEG5000-Hyd-PCL) is introduced between PEG5000 modified with a hydrophilic terminal carboxyl group and hydrophobic polycaprolactone (PCL): (a) Synthesis of acyl hydrazide-PEG derivatives: mPEG-SH was dissolved in chloroform, fully reacted with excess acyl hydrazide cross-linking agent MPBH in the presence of triethylamine, and unreacted substances were removed by dialysis. After thin-layer chromatography analysis, lyophilize and then disperse in chloroform and store at low temperature; (b) 4-acetylphenylmaleimide activates phospholipids: in the presence of triethylamine, 4-acetylphenylmaleimide Amines and DSPE-SH fully react at room temperature. The activated phospholipids are separated by a silica gel column, and the product fractions are analyz...

Embodiment 3

[0069] The present invention prepares a cascade targeted drug delivery system double-modified by lactoferrin and alpha-fetoprotein by the following method

[0070] (1) A pH-sensitive hydrazone bond (COOH-PEG3000-Hyd-PCL) was introduced between PEG3000 modified with a hydrophilic terminal carboxyl group and hydrophobic polycaprolactone (PCL): (a) Synthesis of acyl hydrazide-PEG derivatives: mPEG-SH was dissolved in chloroform, fully reacted with excess acyl hydrazide cross-linking agent MPBH in the presence of triethylamine, and unreacted substances were removed by dialysis. After thin-layer chromatography analysis, lyophilize and then disperse in chloroform and store at low temperature; (b) 4-acetylphenylmaleimide activates phospholipids: in the presence of triethylamine, 4-acetylphenylmaleimide Amines and DSPE-SH fully react at room temperature. The activated phospholipids are separated by a silica gel column, and the product fractions are analyzed by thin-layer chromatograp...

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Abstract

The invention provides a cascade targeted medicine delivery system as well as a preparation method and application thereof. The cascade targeted medicine delivery system comprises first-stage bone target ligand, second tumor targeting ligand and a carrier system, wherein the carrier system is a nano carrier which is made of an amphiphilic polymer with a structure of a hydrophobic core and a hydrophilic shell; the first-stage bone target ligand and the second tumor targeting ligand are connected with the hydrophilic shell of the carrier system. By adopting the cascade targeted medicine deliverysystem prepared by using the preparation method provided by the invention, recognition of specific tumor cells in bone is achieved, the difficulty that a conventional bone tumor medicine cannot be precisely delivered is overcome, and a technical base is made for precise diagnosis and treatment on bone tumor and other bone related diseases.

Description

technical field [0001] The invention belongs to the field of nano-biological materials, and relates to a cascade targeted drug delivery system and its preparation method and application. Background technique [0002] Bone tumors, including primary bone tumors and metastatic bone tumors, have extremely high mortality and disability, and seriously endanger human health. Tumor cells are deposited in the bone, and their proliferation in the bone will cause changes in the bone marrow microenvironment, such as the release of a large number of osteoclast activating factors, causing an imbalance between osteolysis and osteogenesis, resulting in severe bone pathological damage; at the same time, disordered bone marrow The microenvironment further promotes the metastasis and erosion of tumor cells, forming a "vicious circle". Different from the treatment of other conventional tissue and organ solid tumors, due to the characteristics of bone tissue with high hardness, poor permeabilit...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/62A61K47/68A61K47/54A61K47/60A61K31/65A61K31/663A61K49/00A61P35/00A61P19/08
CPCA61K31/65A61K31/663A61K49/0054A61K49/0056A61K49/0067A61K49/0082A61K49/0084A61K49/0093
Inventor 王强斌李春炎张叶俊陈光村
Owner 苏州影睿光学科技有限公司
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