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Polylysine nano prodrug micelle with charge turning and targeting functions and preparation and application thereof

A polylysine and charge inversion technology is applied in the application field of preparing tumor-targeted drugs to achieve the effects of increasing the ability to enter cells, avoiding protein adsorption, and avoiding metabolic burden

Inactive Publication Date: 2016-05-11
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, such positively charged polymers are easily recognized by the reticuloendothelial system and cleared out of the blood circulation, and can also be adsorbed to proteins in the blood, which poses certain risks

Method used

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  • Polylysine nano prodrug micelle with charge turning and targeting functions and preparation and application thereof
  • Polylysine nano prodrug micelle with charge turning and targeting functions and preparation and application thereof
  • Polylysine nano prodrug micelle with charge turning and targeting functions and preparation and application thereof

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Experimental program
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Effect test

Embodiment 1

[0039] (1) Preparation of Nε-benzyloxycarbonyl-L-lysine anhydride by phosgene method: ultrasonically disperse 2.62 g (0.02 mol) of Nε-benzyloxycarbonyl-L-lysine in 90 mL of anhydrous THF. N 2Protected, vigorously stirred at 50°C. Dissolve 5.94g of recrystallized triphosgene in 15mL of anhydrous THF, and add it dropwise to the reaction system until the solution becomes clear, then continue stirring for 90min, and finally distill off about 2 / 3 of the triphosgene under reduced pressure. The solvent was then added into a large amount of n-hexane, and the solid was obtained by suction filtration, and then recrystallized twice, and the product was vacuum-dried at room temperature overnight to prepare Z-Lys-NCA.

[0040] (2) DOX-triggered NCA ring-opening polymerization to prepare DOX-PLL (Z): 20 mg of DOX was dissolved in 3 mL of anhydrous DMF, and 320 mg of Z-Lys-NCA prepared above was dissolved in 1 mL of anhydrous DMF. Slowly added dropwise to DOX / DMF solution, under N 2 Under...

Embodiment 2

[0056] (1) Preparation of Nε-benzyloxycarbonyl-L-lysine anhydride by phosgene method: ultrasonically disperse 2.62 g (0.02 mol) of Nε-benzyloxycarbonyl-L-lysine in 90 mL of anhydrous THF. N 2 Protected, vigorously stirred at 50°C. Dissolve 5.94g of recrystallized triphosgene in 15mL of anhydrous THF, and add it dropwise to the reaction system until the solution becomes clear, then continue stirring for 90min, and finally distill off about 2 / 3 of the triphosgene under reduced pressure. The solvent was then added into a large amount of n-hexane, and the solid was obtained by suction filtration, and then recrystallized twice, and the product was vacuum-dried at room temperature overnight to prepare Z-Lys-NCA.

[0057] (2) DOX-triggered NCA ring-opening polymerization to prepare DOX-PLL (Z): 20 mg of DOX was dissolved in 2.5 mL of anhydrous DMF, and 210 mg of Z-Lys-NCA prepared above was dissolved in 0.7 mL of anhydrous DMF. It was slowly added dropwise to the DOX / DMF solution u...

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Abstract

The invention discloses a polylysine nano prodrug micelle with charge turning and targeting functions and preparation and application thereof. The polylysine nano prodrug micelle takes a hydrophobic drug as an inner core, the structure of the hydrophobic drug contains amino, a polylysine chain serves as a shell layer and is composed of 10-25 lysines, the amino of the hydrophobic drug is connected with carboxyl located at the tail end of the polylysine chain through an amido bond, amino located at the tail end of the polylysine chain modifies an upper targeting ligand through an amido bond as well, and beta-carboxyl amidation is performed on amino located at a side chain of the polylysine chain. According to the polylysine nano prodrug micelle with the charge turning and targeting functions and preparation and application thereof, the structure and preparation process of the prodrug micelle are simplified, the prodrug micelle has both the active and passive targeting properties and the pH responding property, the treatment efficiency can be improved, and the toxic and side effects are reduced.

Description

technical field [0001] The invention relates to a polylysine nano-prodrug micelle with charge reversal and targeting functions, a preparation method thereof and an application in preparing tumor-targeting drugs. Background technique [0002] In recent years, due to various reasons such as the environment, cancer has become more and more common in daily life, and it shows a trend of younger age, which seems to have become the biggest threat to human health. However, due to the low selectivity of commonly used anticancer drugs, in order to achieve clinical efficacy, patients are generally given relatively high drug doses, but this may also cause serious damage to healthy cells. Therefore, the current more effective approach to cancer is to develop efficient drug delivery systems to reduce drug damage to healthy cells. [0003] At present, the common anticancer drugs are mainly DNA poisons. As the name suggests, these drugs must enter the nucleus to exert their due effect. Ho...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K45/06A61K9/10A61P35/00A61K31/704A61K31/7048
CPCA61K9/1075A61K31/704A61K31/7048A61K45/06
Inventor 张静陈佳达冯杰
Owner ZHEJIANG UNIV OF TECH
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