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Charge conversion type nanometer drug carrier and preparation method thereof

A nano-drug carrier and charge conversion technology, applied in the field of medicine, can solve problems such as difficult to overcome the blood-brain barrier, and achieve the effect of overcoming the blood-brain barrier

Active Publication Date: 2017-05-17
HAISI MEIYU SHENZHEN TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, none of the existing drug carriers satisfies the above three points at the same time, so it is difficult for the current drug carriers to overcome the blood-brain barrier (BBB)

Method used

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  • Charge conversion type nanometer drug carrier and preparation method thereof

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preparation example Construction

[0032] The second embodiment of the present invention provides a method for preparing the above-mentioned charge conversion nano drug carrier, including:

[0033] Carrier body preparation steps: acylate chitosan to generate hydrophobic chitosan, then graft polyethylene glycol with alkynyl at the end, and then connect with targeting peptide with azide at the end by Click reaction to obtain positively charged Targeting peptide modified polyethylene glycol-hydrophobic modified chitosan;

[0034] Carrier lock preparation steps: poly(Nε-benzyloxycarbonyllysine) debenzyloxy group to expose -NH 2 , and then react with 2,3-dimethylmaleic anhydride to obtain polylysine with side chain modification of 2,3-dimethylmaleic acid;

[0035]Nano drug particle carrier preparation steps: use the dialysis method, reverse evaporation method or emulsification solvent evaporation method to prepare the polyethylene glycol-hydrophobic modified chitosan modified by the targeting peptide into a nano co...

Embodiment 1

[0059] 1. Preparation of charge conversion drug carrier:

[0060] a. Synthesis of D-PLL-DMMA

[0061] Weigh 11.2g of Nε-benzyloxycarboxy-L-lysine solid and dissolve it in 180mL of anhydrous tetrahydrofuran; weigh 5.2g of bis(trichloromethyl)carbonate solid and dissolve it in 40mL of anhydrous tetrahydrofuran, pour into in the funnel. In the oil bath reaction, the reaction temperature was kept at about 50°C. Drop the dissolved bis(trichloromethyl)carbonate solution drop by drop into Nε-benzyloxycarboxy-L-lysine, drop it for 1-2 hours, and react for 0.5 hours after the drop is completed. The reaction product was concentrated by rotary evaporation to 20-30 mL. The product was precipitated with 200 mL of anhydrous n-butane, recrystallized at -4°C for 6 h and filtered with suction, and the filtrate was removed. The solid obtained by suction filtration was dried in a vacuum oven for 12 hours, and stored at -20°C;

[0062] In an ice-water bath, slowly drop 20 mg / mL diethylamine ...

Embodiment 2

[0073] 1. Preparation of charge conversion drug carrier:

[0074] a. Synthesis of D-PLL-DMMA

[0075] Weigh 11.2g of Nε-benzyloxycarboxy-L-lysine solid and dissolve it in 180mL of anhydrous tetrahydrofuran; weigh 5.2g of bis(trichloromethyl)carbonate solid and dissolve it in 40mL of anhydrous tetrahydrofuran, pour into in the funnel. In the oil bath reaction, the reaction temperature was kept at about 50°C. Drop the dissolved bis(trichloromethyl)carbonate solution drop by drop into Nε-benzyloxycarboxy-L-lysine, drop it for 1-2 hours, and react for 0.5 hours after the drop is completed. The reaction product was concentrated by rotary evaporation to 20-30 mL. The product was precipitated with 200 mL of anhydrous n-butane, recrystallized at -4°C for 6 h and filtered with suction, and the filtrate was removed. The solid obtained by suction filtration was dried in a vacuum oven for 12 hours, and stored at -20°C;

[0076] In an ice-water bath, slowly drop 20 mg / mL diethylamine ...

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Abstract

The invention is suitable for the medicinal technical field and provides a charge conversion type nanometer drug carrier and a preparation method thereof. The charge conversion type nanometer drug carrier comprises an inner core and an outer core, wherein the inner core is served as a carrier main body; the outer core is served as a carrier lock for performing charge conversion on the carrier main body; the inner core and the outer core are combined under the effects of positive and negative charges; the carrier main body is made from the target peptide modified polyethylene glycol-hydrophobic modified chitosan with positive charges; the carrier lock is made from polylysine with the side chain modified with 2,3-dimethyl maleic acid. The charge conversion type nanometer drug carrier provided by the invention has a dual-charge conversion function; the negative charges are loaded on the surface of the charge conversion type nanometer drug carrier; under a weak acid condition, the carrier lock is opened, the carrier charges are reversed, the negative charges are reversed into positive charges, the target peptide is exposed on the micellar surface, a targeting function is achieved and the blood brain barrier is overcome.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a charge conversion nano drug carrier and a preparation method thereof. Background technique [0002] Nano-drug carrier is a delivery system coated with nano-sized therapeutic drugs, which can enter capillaries through blood circulation, prolong the circulation time in the blood stream, and enter the lesion through the gap between endothelial cells, and be absorbed by cells. The way of pinocytosis is absorbed to achieve targeted drug use, which helps to reduce the dosage of the drug and reduce its side effects. Nano-drug carriers have small particle size and high specific surface area, which can embed hydrophobic drugs, improve their solubility, and reduce the side effects of co-solvents in conventional drugs; they can be conveniently transported in the body, and can realize multiple drugs and A combination of multiple diagnostic and therapeutic approaches. These a...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/36A61K47/34A61K47/42
CPCA61K9/5146A61K9/5161A61K9/5169
Inventor 陈仕国严瑶瑶刘斌
Owner HAISI MEIYU SHENZHEN TECH CO LTD
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