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A kind of peg-peptide linear-dendritic drug delivery system and its preparation method and application

A drug delivery system and linear technology, applied in the field of PEG-Peptide linear-dendritic drug delivery system and its preparation, can solve the problems of complex preparation process, complex drug system, and increased preparation process, etc.

Active Publication Date: 2022-03-04
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation process of the drug-loading system is complicated, and the coupling of the targeted molecule folic acid increases the preparation process; the combination of doxorubicin and photosensitizer also further complicates the drug system

Method used

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  • A kind of peg-peptide linear-dendritic drug delivery system and its preparation method and application
  • A kind of peg-peptide linear-dendritic drug delivery system and its preparation method and application
  • A kind of peg-peptide linear-dendritic drug delivery system and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] Embodiment 1, the preparation of linear-dendritic copolymer of the present invention

[0112] according to figure 1 The route diagram shown, the linear-dendritic copolymer (compound 5) of the present invention was synthesized. Concrete synthetic steps are as follows:

[0113] (1) Synthesis of compound 1

[0114] Under nitrogen protection, Fmoc-Lys(Fmoc)-OH (4.00g, 6.78mmol), H-Glu(OtBu)-OtBu·HCl (3.01g, 10.17mmol), HOBt (1.37g, 10.17mmol) and HBTU (3.86g, 10.17mmol) was dissolved in 20mL of ultra-dry N,N-dimethylamide, and then DIPEA (3.50g, 27.12mmol) was slowly added dropwise thereto under ice bath. After the reaction was stirred in an ice bath for 1 h, the reaction was continued at room temperature for 24 h. After the reaction, the reaction solution was diluted into 300mL ethyl acetate, and successively washed with saturated NaHCO 3 solution, washed with 1M HCl solution and saturated NaCl solution, collected the organic layer and washed it with anhydrous MgSO 4...

Embodiment 2

[0123] Embodiment 2, the preparation of drug delivery system of the present invention

[0124] according to figure 1 The synthetic route shown is to synthesize the linear dendritic nano-drug PPDP (i.e. compound 6) of the present invention, specifically:

[0125] Under nitrogen protection, compound 5 (300.0 mg, 33.2 μmol), Pyropheophorbide a (142.0 mg, 265.6 μmol), HOAt (40.7 mg, 298.8 μmol) and HATU (113.6 mg, 298.8 μmol) were dissolved in 10 mL of ultra-dry N , N-dimethylamide, and then DIPEA (154.4 mg, 1.20 mmol) was slowly added dropwise thereto under ice-cooling. After the reaction was stirred in an ice bath for 1 h, the reaction was continued at room temperature for 48 h under dark conditions. After the reaction, the reaction solution was dialyzed in ultrapure water for 2 days with a dialysis bag with a molecular weight cut-off of 8000, and passed through a size exclusion chromatography column (Superose 12HR / 16 / 30column on an FPLC system (GE Healthcare) column) for fu...

Embodiment 3

[0126] Embodiment 3, the preparation of self-assembly system of the present invention

[0127] The compound 6 prepared in the above-mentioned Example 2 was added into pure water to prepare a 200 μg / mL solution, and self-assembled to obtain the self-assembly system of the present invention (such as figure 2 shown).

[0128] The beneficial effects of the present invention are demonstrated through experimental examples below.

[0129] The experimental method that the present invention adopts is as follows:

[0130] 1. Mass Spectrometry and NMR Spectroscopy

[0131] Weigh about 1mg of the sample, fully dissolve it in the corresponding solvent, and test it on a liquid chromatography-mass spectrometer or matrix-assisted laser desorption ionization time-of-flight mass spectrometer; weigh about 5mg of the sample, and add 0.5mL of heavy water or deuterium The sample was fully dissolved by substituting dimethyl sulfoxide as a solvent, and tested on a high-resolution superconducting ...

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Abstract

The present invention provides a linear-dendritic copolymer, the structure of the linear-dendritic copolymer is shown in formula I. The present invention also provides a drug delivery system, which is obtained after the coupling reaction between the linear-dendritic copolymer and the photosensitizer. Studies have shown that the drug delivery system PPDP of the present invention can self-assemble in a selective solvent to form nanoparticles with uniform size, good monodispersity, high stability and weak negative charge, which not only has excellent photophysical properties, but also Effectively generate ROS to kill tumor cells; it significantly reduces the skin phototoxicity of photosensitizers; it not only exhibits better biological safety, excellent fluorescence imaging function, long-term blood circulation function and long-term and high-concentration The tumor-targeting and enrichment effect of the invention also has significant anti-tumor activity, and shows good application prospects in the preparation of anti-tumor drugs.

Description

technical field [0001] The invention belongs to the field of polymer materials, and in particular relates to a PEG-Peptide linear-dendritic drug delivery system and its preparation method and application. Background technique [0002] At present, chemotherapy is one of the main means of clinical treatment of malignant tumors. However, traditional chemotherapeutic drugs generally have high toxicity and side effects, not only lack of tumor selectivity, but also easily lead to multidrug resistance of tumors after long-term use. These inevitable defects are an important reason for the failure of chemotherapy. Therefore, how to improve the disadvantages of traditional chemotherapy drugs such as poor curative effect and high side effects, and seek a low-toxicity, high-efficiency and economical treatment for malignant tumors is a hot research direction in the field of oncology. [0003] As an emerging tumor treatment method, photodynamic therapy (PDT) has brought a new opportunity...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G65/333A61K41/00A61K47/60A61K47/69A61P35/00
CPCC08G65/33396C08G65/33327A61K41/0071A61K47/60A61K47/6935A61P35/00
Inventor 罗奎顾忠伟郑秀丽潘达艺龚启勇
Owner WEST CHINA HOSPITAL SICHUAN UNIV