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Charge transfer type nano pharmaceutical composition and preparation method thereof

A technology of charge conversion and nano-medicine, 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: 2017-05-24
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 transfer type nano pharmaceutical composition 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 an azide-terminated targeting peptide through Click reaction to obtain a 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 core, and then use the positive and neg...

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 technical field of medicines and provides a charge transfer type nano pharmaceutical composition and a preparation method thereof. The charge transfer type nano pharmaceutical composition is prepared from a drug-loading inner core and an outer core; the outer core is a carrier lock for carrying out charge transfer on the drug-loading inner core; the drug-loading inner core is combined with the outer core by a positive and negative charge action; a carrier of the drug-loading inner core is positively-charged and targeting peptide-modified polyethylene glycol-hydrophobic modified chitosan; the drug is a hydrophobic drug and loaded in the carrier; the carrier lock is polylysine of which a side chain is modified with 2,3-dimethyl maleic acid. According to the charge transfer type nano pharmaceutical composition provided by the invention, the combination of multiple drugs and multiple diagnosis and treatment methods is realized, so that a new path is opened for tumor diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a charge conversion nano drug composition 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. The...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/36A61K47/34A61K47/42A61K47/10
CPCA61K9/5146A61K9/5161A61K9/5169
Inventor 陈仕国严瑶瑶刘斌
Owner HAISI MEIYU SHENZHEN TECH CO LTD
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