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Poly(glutamic acid-co-lactic acid)-phosphatidyl ethanolamine graft polymer, and preparation method and application thereof

A technology of phosphatidylethanolamine and graft polymer, which is applied in the field of poly-phosphatidylethanolamine graft polymer and its preparation, can solve problems such as poor hydrophilicity, achieve good effect, prolong drug effect, improve bioavailability and The effect of biological activity

Inactive Publication Date: 2014-07-23
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The object of the present invention is to overcome the shortcoming of the poor hydrophilicity of polylactic acid and phosphatidylethanolamine, utilize the hydrophilicity and biocompatibility of polyglutamic acid, provide a kind of novel amphiphilic poly(glutamic acid-co-lactic acid )-phosphatidylethanolamine graft polymer

Method used

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  • Poly(glutamic acid-co-lactic acid)-phosphatidyl ethanolamine graft polymer, and preparation method and application thereof
  • Poly(glutamic acid-co-lactic acid)-phosphatidyl ethanolamine graft polymer, and preparation method and application thereof
  • Poly(glutamic acid-co-lactic acid)-phosphatidyl ethanolamine graft polymer, and preparation method and application thereof

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preparation example Construction

[0042] The present invention also provides a kind of preparation method of poly(glutamic acid-co-lactic acid)-phosphatidylethanolamine graft polymer, wherein, the method comprises the following steps:

[0043] (1) Under the protection of an inert gas, glutamic acid is contacted with lactide to obtain the first product containing a poly(glutamic acid-co-lactic acid) graft polymer having a structure shown in formula (3),

[0044] Formula (3);

[0045] (2) In the presence of a six-membered heterocyclic compound containing a nitrogen heteroatom, in a first organic solvent, the first product is contacted with 4-nitrobenzene chloroformate, or the unreacted product is separated from the first product The reactant, will separate the first product of unreacted reactant and 4-nitrobenzoic chloroformate contact, obtain the poly(glutamic acid-co-lactic acid)- The second product of 4-nitrobenzoate graft polymer; The first organic solvent is a six-membered heterocyclic compound capable o...

Embodiment 1

[0090] This example is used to illustrate the synthesis of poly(glutamic acid-co-lactic acid)-dipalmitoylphosphatidylethanolamine graft polymer

[0091] (1) L-glutamic acid (1.47 grams, 0.01mol) (Alfar Aesar company, 98% by weight, analytically pure), L-lactide (7.2 grams, 0.05mol) (Alfar Aesar company, 97% by weight, Analytical grade) was added to a 50 ml single-necked round-bottomed flask, vacuumed for 1 hour to remove oxygen, fed with nitrogen, and stirred and reacted in an oil bath at 170°C under the protection of nitrogen, the solution turned into a yellow transparent liquid. After reacting for 6 hours, the temperature was lowered to 150° C. for 24 hours, and the reaction liquid was viscous light brown liquid. Take it out from the oil bath and cool it down to produce a yellow-brown solid, which is dissolved in 15 ml of N,N-dimethylformamide (Beijing Chemical Plant, analytical grade), and filtered to remove unreacted lactide. The filtrate was precipitated in 250 ml of dei...

Embodiment 2

[0120] (1) L-glutamic acid (1.47 grams, 0.01mol) (Alfar Aesar company, 98% by weight, analytically pure), L-lactide (7.2 grams, 0.05mol) (Alfar Aesar company, 97% by weight, Analytical grade) was added to a 50 ml single-necked round-bottomed flask, vacuumed for 1 hour to remove oxygen, fed with nitrogen, and stirred and reacted in an oil bath at 170°C under the protection of nitrogen, the solution turned into a yellow transparent liquid. After reacting for 3 hours, the temperature was lowered to 140° C. for 18 hours, and the reaction liquid was viscous light brown liquid. Take it out from the oil bath and cool it down to produce a yellow-brown solid, which is dissolved in 20 ml of N,N-dimethylformamide (Beijing Chemical Plant, analytical grade), and filtered to remove unreacted lactide. The filtrate was precipitated in 250 ml of deionized water and washed three times with 100 ml of deionized water. After drying in a vacuum oven at 20°C for 48 hours, 8.2 grams of a brown solid...

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Abstract

The present invention relates to poly(glutamic acid-co-lactic acid)-phosphatidyl ethanolamine graft polymer having a structure shown as a formula (1), wherein n is 20-60, x is 15-100, y is 15-100, the grafting rate is 90-170%, and A is a group having a structure shown as a formula (2). The invention also provides a preparation method of the poly(glutamic acid-co-lactic acid)-phosphatidyl ethanolamine graft polymer and an application of the poly(glutamic acid-co-lactic acid)-phosphatidyl ethanolamine graft polymer in preparing pharmaceutical compositions. A nanomicelle of the amphiphilic poly(glutamic acid-co-lactic acid)-phosphatidyl ethanolamine graft polymer can be used as a water-soluble drug carrier, and also can be used as a fat-soluble drug carrier. The applicable type is wide, the drug effect can be effectively prolonged, and the bioavailability and biological activity can be improved.

Description

technical field [0001] The invention relates to a poly(glutamic acid-co-lactic acid)-phosphatidylethanolamine graft polymer, a preparation method thereof, and an application in the preparation of a pharmaceutical composition. Background technique [0002] Polyglutamic acid (PGA) is a high-molecular amino acid polymer formed by the combination of L-glutamic acid (L-Glu) and the like through γ-amide bonds, which can be degraded by lysosomal enzymes in vivo into The endogenous substance glutamic acid is not easy to produce accumulation and toxic side effects. Its molecular chain has a highly active side chain carboxyl group (-COOH), which is easy to combine with some drugs to form stable complexes. It is an ideal biodegradable polymer material for medicine in vivo. Polyglutamic acid (PGA) was first isolated and extracted from Japanese natto, and can be obtained through chemical synthesis and microbial polymerization. The traditional peptide synthesis method is to connect amin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G69/48C08G69/44A61K47/34
Inventor 吴雁刘小广苏世帅刘君星李明军
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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