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Responsive polymeric micelle drug carrying system and preparation method thereof

A polymer glue, responsive technology, used in pharmaceutical formulations, active ingredients of heavy metal compounds, anti-tumor drugs, etc. Effect

Active Publication Date: 2014-06-25
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, clinically used antineoplastic drugs have many defects in their application, such as: poor stability of water-soluble agents, high toxicity and side effects of drugs, and killing normal cells of the human body while treating diseases

Method used

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  • Responsive polymeric micelle drug carrying system and preparation method thereof
  • Responsive polymeric micelle drug carrying system and preparation method thereof
  • Responsive polymeric micelle drug carrying system and preparation method thereof

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preparation example Construction

[0044] The present invention also provides a preparation method for the functionalized polyethylene glycol monomethyl ether-b-poly(L-lysine) represented by the above formula (I), comprising: A) the polyethylene glycol with terminal amination Monomethyl ether is mixed with N(ε)-benzyloxycarbonyl-L-lysine-N-cyclic acid anhydride in an organic solvent to react to obtain N-benzyloxycarbonyl-protected polyethylene glycol monomethyl ether-b -poly(L-lysine); B) deprotecting the N-benzyloxycarbonyl-protected polyethylene glycol monomethyl ether-b-poly(L-lysine) in a strongly acidic solution to obtain Polyethylene glycol monomethyl ether-b-poly(L-lysine); C) Mix the polyethylene glycol monomethyl ether-b-poly(L-lysine) with acid anhydride for reaction, dialyze, Freeze-dry to obtain functionalized polyethylene glycol monomethyl ether-b-poly(L-lysine); the acid anhydride is succinic anhydride, 2,3,4,5-tetrahydrophthalic anhydride, dimethylmaleic One or more of acid anhydride, tetramethy...

Embodiment 1～5

[0081] Weigh 10g of polyethylene glycol monomethyl ether with a number average molecular weight of 1000 (0.01mol), 2000 (0.005mol), 5000 (0.002mol), 10000 (0.001mol) and 20000 (0.0005mol), respectively, and put them into 5 In a dry reaction flask with a branched mouth, add 100ml of toluene to azeotropically remove water, then dissolve the obtained solids in 100ml of anhydrous dichloromethane, cool to 0°C, add 5.06g (0.05mol) , 2.53g (0.025mol), 1.01g (0.010mol), 0.51g (0.005mol) and 0.25g (0.0025mol) triethylamine, and then dropwise added 22.91g, 11.46g, 4.58g, 2.29g and 1.15g Methanesulfonyl chloride. After the addition of methanesulfonyl chloride, react at 0°C for 2h, return to 25°C, and continue to react for 24h under stirring. After the reaction is completed, filter to remove the formed precipitate. The filtrate is settled with ether, filtered, washed, and vacuum-dried at 25°C for 24h , to obtain polyethylene glycol monomethyl ether methanesulfonate. Carry out nuclear ma...

Embodiment 6

[0086] Mix 1mol N-benzyloxycarbonyl-L-lysine and 0.6mol bis(trichloromethyl)carbonate at 25°C, add tetrahydrofuran, heat to 50°C for 2 hours, after the reaction, put the reaction mixture in Settled in excess petroleum ether, separated, washed, recrystallized and dried to obtain N(ε)-benzyloxycarbonyl-L-lysine-N-cyclic acid anhydride.

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Abstract

The invention provides a responsive polymeric micelle drug carrying system and a preparation method thereof. The responsive polymeric micelle drug carrying system is formed by compounding an anti-tumor drug with functional polyethylene glycol monomethyl ether-b-poly(L-lysine) which is as shown in formula (I). Compared with the prior art, firstly, the drug carrying system disclosed by the invention takes an anti-protein nonspecific adsorption material as a shell of a polymer micelle so that the water solubility of the polymer micelle is enhanced and the circulation time of the polymer micelle in the system is prolonged; secondly, in the provided functional polyethylene glycol monomethyl ether-b-poly(L-lysine), all the blocks are different in length and side chain substituent groups are different in types, so that functional polyethylene glycol monomethyl ether-b-poly(L-lysine) with different pH value response points can be obtained, thus the response points of the polymeric micelle drug carrying system formed by functional polyethylene glycol monomethyl ether-b-poly(L-lysine) can be regulated.

Description

technical field [0001] The invention belongs to the technical field of polymer drug carriers, and in particular relates to a responsive polymer micelle drug-loading system and a preparation method thereof. Background technique [0002] Tumor has become one of the most serious diseases threatening human health. The commonly used clinical cancer treatment methods include chemotherapy, radiotherapy and surgical treatment, among which chemotherapy is the most commonly used and important treatment approach. However, the clinically used anti-tumor drugs have many defects in their application, such as: poor stability of water-soluble agents, high toxicity and side effects of drugs, and killing normal cells of the human body while treating diseases. The drug delivery system and controlled release can just solve these problems. Drug controlled release refers to the process of preparing drugs and appropriate carriers in a certain proportion and form, and controlling the drug's actio...

Claims

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Application Information

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IPC IPC(8): C08G69/48C08G69/40C08G69/42C08G65/48A61K47/34A61K9/107A61K9/19A61P35/00A61K31/704A61K31/7048A61K31/282A61K33/24
Inventor 丁建勋陈进进庄秀丽陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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