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Polyleucine-polyaspartic acid block copolymer stereo-composite medicine carrying micelle and preparation method thereof

A technology of block copolymer and polyaspartic acid, which is applied in the field of biomedical materials, can solve the problems of short drug half-life and low encapsulation rate, and achieve the effect of not easy to escape, stable micelles, and enhanced therapeutic effect

Active Publication Date: 2020-01-07
AFFILIATED HOSPITAL OF NANTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The technical problem to be solved by the present invention is that the existing polyamino acid drug carriers still have defects such as low encapsulation efficiency and short half-life of the drug, and block copolymerized amino acids are used to realize the drug-loaded stereostructure to increase the drug-loading capacity and slow release Effect

Method used

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  • Polyleucine-polyaspartic acid block copolymer stereo-composite medicine carrying micelle and preparation method thereof
  • Polyleucine-polyaspartic acid block copolymer stereo-composite medicine carrying micelle and preparation method thereof
  • Polyleucine-polyaspartic acid block copolymer stereo-composite medicine carrying micelle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Step 1: Mix 20g of N-carboxy-L-leucine-anhydride in the ring with 1g of Co(PMe3)4 to form a reaction system. After cooling with liquid nitrogen, vacuumize, polymerize at 60°C for 24 hours in a nitrogen atmosphere, and then add 80gN -carboxyl-L-aspartic acid-cyclic acid anhydride to continue the polymerization reaction for 24 hours, the reaction product is filtered after precipitation treatment, and poly-L-amino acid block copolymer is obtained after drying;

[0029] Step 2: Mix 20g of N-carboxy-D-leucine-anhydride in the ring with 1g of Co(PMe3)4 to form a reaction system. After cooling with liquid nitrogen, vacuumize, polymerize at 60°C for 24 hours in a nitrogen atmosphere, and then add 80gN -carboxyl-L-aspartic acid-anhydride in the ring continued to polymerize for 24 hours, and the reaction product was filtered after precipitation treatment, and poly-D-amino acid block copolymer was obtained after drying;

[0030] Step 3: Cool 1g of poly-L-amino acid block copolymer...

Embodiment 2

[0034] Step 1: Mix 10g of N-carboxy-L-leucine-anhydride in the ring with 1g of Co(PMe3)4 to form a reaction system. After cooling with liquid nitrogen, vacuumize, polymerize at 20°C for 1 hour in a nitrogen atmosphere, and then add 190gN -carboxyl-L-aspartic acid-cyclic acid anhydride continued to polymerize for 48 hours, the reaction product was filtered after precipitation treatment, and poly-L-amino acid block copolymer was obtained after drying;

[0035] Step 2: Mix 10g of N-carboxy-D-leucine-anhydride in the ring with 1g of Co(PMe3)4 to form a reaction system. After cooling with liquid nitrogen, vacuumize, polymerize at 20°C for 1 hour in a nitrogen atmosphere, and then add 190gN -carboxyl-L-aspartic acid-cyclic acid anhydride continued to polymerize for 48 hours, and the reaction product was filtered after precipitation treatment, and poly-D-amino acid block copolymer was obtained after drying;

[0036]Step 3: Cool 1g of poly-L-amino acid block copolymer and 1g of poly-D...

Embodiment 3

[0039] Step 1: Mix 15g of N-carboxy-L-leucine-anhydride in the ring with 1g of Co(PMe3)4 to form a reaction system. After cooling with liquid nitrogen, vacuumize, polymerize at 100°C for 48 hours in a nitrogen atmosphere, and then add 30gN -carboxyl-L-aspartic acid-cyclic acid anhydride to continue the polymerization reaction for 1 hour, the reaction product is filtered after precipitation treatment, and poly-L-amino acid block copolymer is obtained after drying;

[0040] Step 2: Mix 15g of N-carboxy-D-leucine-anhydride in the ring with 1g of Co(PMe3)4 to form a reaction system. After cooling with liquid nitrogen, vacuumize, polymerize at 100°C for 48 hours in a nitrogen atmosphere, and then add 30gN -carboxyl-L-aspartic acid-cyclic acid anhydride to continue the polymerization reaction for 1h, the reaction product is filtered after precipitation treatment, and the poly-D-amino acid block copolymer is obtained after drying;

[0041] Step 3: Cool 1g of poly-L-amino acid block c...

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Abstract

The invention discloses a polyleucine-polyaspartic acid block copolymer stereo-composite medicine carrying micelle and a preparation method thereof. The preparation method comprises the following steps: performing block copolymerization on a poly-L-leucine monomer and a poly-L-aspartic acid monomer; performing block copolymerization on a poly-D-leucine monomer and a poly-D-aspartic acid monomer; performing an acyl halogenation reaction on the obtained poly-L-amino acid block copolymer and the obtained poly-D-amino acid block copolymer with SOCl2 respectively, further adding DMF (dimethyl formamide), triethylamine and a first medicine, and performing a reaction so as to obtain a poly-L-amino acid-first medicine copolymer and a poly-D-amino acid-first medicine copolymer; and finally mixing the poly-L-amino acid-first medicine copolymer and the poly-D-amino acid-first medicine copolymer in a PBS (phosphate buffer) of an equal mass, adding a second medicine, performing high-speed homogenization, and performing extrusion by using a filtering membrane of which the aperture is 100nm, so as to obtain the medicine carrying micelle. The medicine carrying micelle disclosed by the invention has a high enveloping rate, has a slow release velocity and has a low macrophage taking velocity, and thus the purpose of long-circulation target tumor dosing can be achieved.

Description

technical field [0001] The invention belongs to the field of biomedical materials, in particular to a polyleucine-polyaspartic acid block copolymer stereocomplex drug-loaded micelles and a preparation method thereof. Background technique [0002] The polymer drug delivery system refers to the use of polymer carriers for encapsulation, adsorption or chemical connection of drugs, and the selective distribution and physical and chemical properties of the drug carrier itself are used to deliver the drug to the lesion site, and the drug can be delivered to the lesion through diffusion and other methods. Released slowly, so as to achieve the purpose of treating diseases safely and effectively. However, biocompatibility, biodegradability and safety restrict the use of some pharmaceutical polymer materials, and the development of safe polymer materials with new functions has always been a hot spot in pharmaceutical research. Amino acid is the basic unit of biological functional mac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/64A61K31/7068A61K31/337A61P35/00
CPCA61K47/6907A61K47/64A61K31/7068A61K31/337A61P35/00A61K2300/00
Inventor 陆舒尹晓敏赵宏胜陆洋
Owner AFFILIATED HOSPITAL OF NANTONG UNIV
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