Preparation methods of poly (aspartic acid-co-lactic acid) graft polymer and nanoparticles of poly (aspartic acid-co-lactic acid) graft polymer

A technology of grafting polymer and aspartic acid, applied in nanotechnology, drug combination, pharmaceutical formulation and other directions, can solve problems such as poor hydrophilicity

Inactive Publication Date: 2011-04-20
BEIJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] The present invention overcomes the disadvantage of poor hydrophilicity of polylactic acid, utilizes the hydrophilicity and biocompatibility of polyaspartic acid, and provides a poly(aspartic acid-co-lactic acid) graft polyme

Method used

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  • Preparation methods of poly (aspartic acid-co-lactic acid) graft polymer and nanoparticles of poly (aspartic acid-co-lactic acid) graft polymer
  • Preparation methods of poly (aspartic acid-co-lactic acid) graft polymer and nanoparticles of poly (aspartic acid-co-lactic acid) graft polymer
  • Preparation methods of poly (aspartic acid-co-lactic acid) graft polymer and nanoparticles of poly (aspartic acid-co-lactic acid) graft polymer

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preparation example Construction

[0030] According to the preparation method provided by the present invention, the reaction is carried out under nitrogen, and the conditions of the reaction include: the molar ratio of the aspartic acid to the lactide is 1:1-10, relative to 10 g of light brown solid, the amount of the first organic solvent is 5-20mL, the reaction temperature is 160-180°C, and the contact time is 16-26 hours.

[0031] Since aspartic acid can self-polymerize to form polyaspartic acid at high temperature, lactide can directly react with -OH on polyaspartic acid. Therefore, in the present invention, direct reaction of lactide and aspartic acid is selected to obtain the poly(aspartic acid-co-lactic acid) graft polymer represented by formula (1). Both lactide and aspartic acid used in the present invention are commercially available.

[0032] Preferably, the preparation method provided by the present invention also includes removing N,N-dimethylformamide from the product obtained after the reaction...

Embodiment 1

[0043] Synthesis of Poly(Aspartic Acid-co-Lactic Acid) Grafted Polymer

[0044] Add L-aspartic acid (3.33g, 0.025mol) (Alfar Aesar company, 98%, analytically pure), L-lactide (7.2g, 0.05mol) (Alfar Aesar company, 97%, analytically pure) Into a 50mL single-necked round bottom flask, evacuate for 1 hour to remove oxygen, pass through nitrogen, and under the protection of nitrogen, stir the reaction in an oil bath at 180°C. The solution turned into a yellow transparent liquid. After reacting for 2.5 hours, the temperature was lowered to 160° C. for 21 hours. The reaction solution is viscous light brown liquid. Remove from the oil bath and cool to give a light brown solid which is dissolved in 15 mL of DMF and unreacted lactide is filtered. The filtrate was precipitated in 250 mL of deionized water and washed three times with 100 mL of deionized water. Dry in a vacuum oven at 25° C. for 36 hours to obtain 8.4 g of poly(aspartic acid-co-lactic acid) graft polymer.

[0045] Aft...

Embodiment 2

[0054] Synthesis of Poly(Aspartic Acid-co-Lactic Acid) Grafted Polymer

[0055] Add L-aspartic acid (6.66g, 0.05mol) (Alfar Aesar company, 98%, analytically pure), L-lactide (7.2g, 0.05mol) (Alfar Aesar company, 97%, analytically pure) Into a 50mL single-necked round bottom flask, evacuate for 1 hour to remove oxygen, feed nitrogen, and stir the reaction in an oil bath at 180°C under the protection of nitrogen. The solution turned into a yellow transparent liquid. After reacting for 3 hours, the temperature was lowered to 160° C. for 23 hours. The reaction solution is viscous light brown liquid. Remove from the oil bath and cool to give a light brown solid which is dissolved in 20 mL of DMF and unreacted lactide is filtered. The filtrate was precipitated in 250 mL of deionized water, and washed three times with 200 mL of deionized water. Dry in a vacuum oven at 20°C for 24 hours to obtain 11.1 g of poly(aspartic acid-co-lactic acid) graft polymer.

[0056] After detection...

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Abstract

The invention discloses preparation methods of a poly (aspartic acid-co-lactic acid) graft polymer and nanoparticles of the poly (aspartic acid-co-lactic acid) graft polymer, which belong to the field of medicaments. A preparation method for the graft polymer comprises the following steps of: mixing aspartic acid and lactide in a molar ratio of 1:1-10, introducing nitrogen and reacting in an oil bath at the temperature of between 160 and 180 DEG C for 16 to 26 hours with stirring to obtain viscous light brown liquid; and taking out of the oil bath and cooling to obtain light brown solid and dissolving in N,N-dimethylformamide; and filtering unreacted lactide, washing a product obtained after filtering and vacuum-drying at the temperature of between 20 and 30 DEG C for 24 to 48 hours to obtain the poly (aspartic acid-co-lactic acid) graft polymer. The invention also provides a method for coating doxorubicin hydrochloride by using the nanoparticles of the polymer. The invention has the advantages that: the process is convenient to operate, the production cost is reduced, the prepared medicament carrying nanoparticles are mono-dispersed regular spheres, the particle size is controlled to be between 100 and 260nm, and an agglomeration phenomenon is not caused.

Description

technical field [0001] The invention relates to a preparation method of a poly(aspartic acid-co-lactic acid) graft polymer and a preparation method of doxorubicin hydrochloride encapsulated in nanoparticles Background technique [0002] Polyaspartic acid (PASP) belongs to a class of polyamino acids, which is a polymeric amino acid with a carboxylic acid side chain. It is a polymer formed by shrinking the amino and carboxyl groups of aspartic acid monomers. There are α, β two configurations. The polyaspartic acid fragments in natural polyamino acids all exist in the α form, while most of the synthetic polyaspartic acid is a mixture of α and β configurations. The polyaspartic acid obtained by thermal condensation polymerization is easily broken by the action of microorganisms and fungi because of the peptide bond on the main chain of the structure, and the final degradation products are water and carbon dioxide which are harmless to the environment. Therefore, polyaspartic a...

Claims

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Application Information

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IPC IPC(8): C08G63/685C08G63/08C08G73/10A61K31/704A61K47/34A61P35/00B82Y40/00
Inventor 胡利明韩思媛吴雁王欢赵宇亮
Owner BEIJING UNIV OF TECH
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