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LHRH-bonded amphiphilic biodegradable polymer, preparation method and application

A biodegradable, LHRH-6-NH2 technology, applied in the field of biomedicine, can solve the problems of poor stability of LHRH, high cost, and difficulty in linking drug molecules with LHRH, and achieve reduction of toxic and side effects, low cost, high bioavailability and The effect of stability

Active Publication Date: 2012-09-12
CHANGZHOU INST OF ENERGY STORAGE MATERIALS &DEVICES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] The purpose of the present invention is to solve the defects of the prior art that LHRH is difficult to connect drug molecules, LHRH is poor in stability and high cost in blood circulation, and provides an amphiphilic biodegradable polymer bonded to LHRH, a preparation method and use

Method used

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  • LHRH-bonded amphiphilic biodegradable polymer, preparation method and application
  • LHRH-bonded amphiphilic biodegradable polymer, preparation method and application
  • LHRH-bonded amphiphilic biodegradable polymer, preparation method and application

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preparation example Construction

[0050] The preparation method of the amphiphilic biodegradable polymer bound with LHRH is to prepare the polymer shown in formula a, when the LHRH polypeptide derivative is LHRH-10-COOH, the steps are as follows:

[0051] Dissolve LHRH-10-COOH in N,N-dimethylformamide or water to dissolve it, add 1-ethyl-(3-dimethylaminopropyl) carbonyl dicarboxylate with 1.5-3 times the molar number of carboxyl groups Imine hydrochloride (EDC·HCl) and 4-dimethylaminopyridine (DMAP) with 0.01 times the number of moles of carboxyl groups, stirred in ice bath for 10-30 minutes, and added with 1-3 times the number of moles of carboxyl groups containing terminal amino groups or terminal hydroxyl groups Two-block copolymer, kept in an ice bath and naturally raised to room temperature, stopped the reaction after 12-24 hours to obtain a reaction solution, placed the reaction solution in a dialysis bag with a molecular weight cut-off of 3500 g / mol and dialyzed with distilled water for 24-48 hours, The...

Embodiment 1

[0085] Example 1: Polypeptide targeting LHRH-6-NHCO-PEG 5K -PLA 2K Preparation of block copolymers

[0086] 0.5mmol carboxyl-terminated diblock copolymer COOH-PEG 5K -PLA 2K (The subscript number in the molecular formula represents the number-average molecular weight of the block, the same below), 0.61mg DMAP and 0.75mmol EDC·HCl are placed in a dry ampoule, add 10ml distilled water and stir for 30 minutes under ice-cooling, add 0.25mmolLHRH -6-NH 2 , kept in an ice bath and naturally raised to room temperature, stirred for 12 hours, placed in a dialysis bag with a molecular weight cut-off of 3500 g / mol, dialyzed with distilled water, changed the water every 6 hours, and lyophilized after 24 hours to obtain a white polypeptide targeting block copolymer LHRH-6-NHCO-PEG 5K -PLA 2K freeze-dried powder. figure 1 It is the ultraviolet-visible absorption spectrum of the block copolymer of bonded LHRH derivatives, and the curve 2 in the figure is the LHRH-6-NHCO-PEG of embodim...

Embodiment 2

[0087] Example 2: Polypeptide targeting LHRH-6-PEG 10K -PGA 20K Preparation of block copolymers

[0088] 1mmol carboxyl-terminated block polymer COOH-PEG 10K -PGA 20K , 1.22mg DMAP and 3mmol EDC·HCl were placed in a dry ampoule, and 10ml N,N-dimethylformamide was added under ice cooling to dissolve and stir for 30 minutes, and 1mmol LHRH-6-NH 2 , kept in an ice bath and naturally raised to room temperature, stirred for 24 hours, placed in a dialysis bag with a molecular weight cut-off of 3500g / mol, dialyzed with distilled water, changed the water every 12 hours, and freeze-dried after 48 hours to obtain a white polypeptide targeting block copolymer LHRH-6-PEG 10K -PGA 20K freeze-dried powder.

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Abstract

The invention discloses a LHRH-bonded amphiphilic biodegradable polymer, a preparation method and application, and belongs to the technical field of biomedicine and overcoming the defects that in the prior art, LHRH has difficulty in being connected with a medicinal molecule and the LHRH has poor stability in blood circulation and high in cost. The bonded LHRH amphiphilic biodegradable polymer isformed by bonding LHRH polypeptide derivatives and a diblock copolymer, or bonding the LHRH polypeptide derivatives and a triblock copolymer; and two LHRH polypeptides are included, namely a 10th-site carboxylated LHRH-10-COOH and a 6th-site glycine- dextrorotatory lysine-replaced LHRH-6-NH2. The invention also provides the preparation method of the bonded LHRH amphiphilic biodegradable polymer. The LHRH-bonded amphiphilic biodegradable polymer can prepare a medicine-loading nanoparticle with an LHRH targeting function, is applicable for a variety of medicines and has a function of targeting a cancer cell which highly expresses an LHRH receptor.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to an amphiphilic biodegradable polymer bonded with LHRH, a preparation method and an application. Background technique [0002] LHRH is the abbreviation of luteinizing hormone releasing hormone (luteinizing-hormone-releasing hormone), which means the following polypeptide composed of 10 amino acids, which has the following structure: [0003] [0004] American scientist A.V.Schally isolated LHRH (also known as Gn-RH at the time) from pig hypothalamus in 1971, clarified its amino acid sequence and successfully synthesized it, thus winning the 1977 Nobel Prize in Medicine. The function of LHRH, just as its name expresses, is to promote the secretion of progesterone and regulate the functions of human sexual organs and reproductive system. Many derivatives of LHRH have been studied, one of which is similar to its function and is its agonist, and the other is its ant...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K17/08A61K47/42A61K47/48A61K9/14
Inventor 景遐斌王瑞岳军肖海华胡秀丽谢志刚黄宇彬
Owner CHANGZHOU INST OF ENERGY STORAGE MATERIALS &DEVICES
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