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Preparation method and applications of triblock polymer micelle

A polymer glue and tri-block technology, applied in the field of polymers, can solve the problems of high cytotoxicity and increased tumor cell uptake

Active Publication Date: 2017-12-01
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Among them, polyethyleneimine and polyamide have abundant amino groups on the surface, which can prepare positively charged nanoparticles, interact with negatively charged cell membranes, and increase the uptake of tumor cells to carriers, but such polymers usually have high cytotoxicity. To some extent, its application is limited

Method used

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  • Preparation method and applications of triblock polymer micelle
  • Preparation method and applications of triblock polymer micelle
  • Preparation method and applications of triblock polymer micelle

Examples

Experimental program
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Embodiment 1

[0093] The preparation of triblock polymer comprises the following steps:

[0094] (1) Synthesis of CSO-ss-

[0095] Dissolve 1.578g of dithiodipropionic acid, 1.437g of EDC and 0.861g of NHS in 20ml of DMF, activate at 40°C for 30min for use; weigh 0.6g of CSO and disperse it in 20mL of distilled water, add a small amount of NaOH to adjust its pH to 7- 8. Slowly drop it into the dithiodipropionic acid solution under stirring conditions, stir and react at 40°C for 12h, dialyze with distilled water for 1d (MWCO=1000), filter the dialysate, and freeze-dry the filtrate to obtain CSO-ss- , the yield was 95%.

[0096] (2) Synthesis of CSO-ss-PEI

[0097] Dissolve 1 g of CSO-ss- prepared in step (1) in 100 mL of distilled water, and stir to form an aqueous solution; dissolve 2.935 g of EDC and 1.435 g of NHS in 5 ml of distilled water to form an aqueous solution of activator, and add it to the aqueous solution of CSO-ss- for activation After 30 minutes, dissolve 2g of PEI in 5ml ...

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Abstract

The invention provides a preparation method of a triblock polymer micelle. The preparation method comprises the following steps: (1) enabling chitosan oligosaccharide and dithiodipropionic acid to react under the effect of an activating agent, thus obtaining a first intermediate; (2) enabling the first intermediate and polyethyleneimine to react under the effect of the activating agent, thus obtaining a second intermediate; (3) enabling the second intermediate and urocanic acid to react under the effect of the activating agent, thus obtaining a triblock polymer; and (4) dissolving the triblock polymer obtained in the step (3) in water, thus obtaining the triblock polymer micelle. The triblock polymer micelle has the excellent tissue permeability and enhanced penetration and retention effects, so that a natural passive targeting effect is achieved, and a new candidate system is provided for the development of nanocarriers.

Description

technical field [0001] The invention relates to the technical field of polymers, in particular to a preparation method and application of a triblock polymer micelle. Background technique [0002] At present, the treatment of tumors has become a global problem that needs to be solved urgently. Chemotherapy is usually used in clinical treatment, which has different degrees of adverse effects on the patient's physical condition, prone to vomiting, hair loss and other adverse reactions, and prone to resistance. Drug properties, currently on the market albumin nanoparticles are expensive, the tumor targeting is not ideal, and the loaded drugs or genes cannot be released quickly and effectively, and chemotherapy methods are prone to multi-drug resistance, and the tumor cannot be removed cleanly. Adverse phenomena such as rapid tumor invasion and metastasis. As a new type of drug carrier, polymer micelles have shown great application potential in many fields such as medicine, and ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/36A61K31/704A61K48/00A61P35/00
CPCA61K9/1075A61K31/704A61K47/36A61K48/0041
Inventor 张学农杨舒迪
Owner SUZHOU UNIV
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