A kind of hydroxychloroquine amphiphilic polymer drug prodrug, preparation method and application thereof

An amphiphilic polymer, hydroxychloroquine technology, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of difficult control of drug load, poor water solubility of the system, long reaction time, etc., to improve the pharmacokinetics Kinetic behavior, reduced binding capacity, improved water solubility

Active Publication Date: 2021-02-09
ZHEJIANG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] At present, the solution to this type of problem is mainly to connect hydroxychloroquine to polyglutamic acid or polysaccharides through chemical reactions, but due to the long reaction time of this type of reaction, and the drug loading is not easy to control, and when the content of hydroxychloroquine is too high , will also lead to poor water solubility of the whole system

Method used

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  • A kind of hydroxychloroquine amphiphilic polymer drug prodrug, preparation method and application thereof
  • A kind of hydroxychloroquine amphiphilic polymer drug prodrug, preparation method and application thereof
  • A kind of hydroxychloroquine amphiphilic polymer drug prodrug, preparation method and application thereof

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Embodiment

[0052] Synthesis of Hydroxychloroquine Amphiphilic Polymer Prodrug:

[0053] In this example, a hydroxychloroquine amphiphilic polymer prodrug with disulfide bonds was synthesized, with a molecular weight of about 10,000 and a uniform molecular weight distribution, wherein the molecular weight of polyethylene glycol monomethyl ether was 5,000.

[0054] 1. Synthesis of polyethylene glycol monomethyl ether chain transfer agent (PEG-PETTC):

[0055] Take 4g polyethylene glycol monomethyl ether (molecular weight 5000, 0.8mmol) and reflux toluene to remove water, spin dry, add 100mL dichloromethane to dissolve, add 5 equivalents of 4-cyano-4-(2-phenylethanesulfide Alkylthiocarbonyl) sulfanyl valeric acid (PETTC) and 0.5 equivalent of 4-dimethylaminopyridine (DMAP), drop 5 equivalents of dicyclohexylcarbodiimide (DCC) dichloromethane under ice bath conditions (DCM) solution, the ice bath was removed after the dropwise addition, and stirred at room temperature for 48 hours. The rea...

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Abstract

The invention discloses a hydroxychloroquine amphiphilic polymer drug prodrug, which is composed of a hydrophilic polyethylene glycol monomethyl ether and a hydrophobic hydroxychloroquine polymer, and the hydroxychloroquine polymer is bonded to the hydroxychloroquine polymer through a breakable chemical bond. On polyethylene glycol monomethyl ether, the described hydroxychloroquine amphiphilic polymer prodrug can self-assemble in water into nanoparticles with a particle size of 20-300nm, which improves the pharmacokinetic behavior of free hydroxychloroquine, At the same time, the hydroxychloroquine amphiphilic polymer prodrug nanoparticles can be loaded with a variety of hydrophobic drugs, including camptothecin and its derivatives, paclitaxel, doxorubicin, bortezomib , and various negatively charged drug molecules, which have a wide range of applications.

Description

technical field [0001] The invention belongs to the field of drug prodrugs and its preparation, and in particular relates to a hydroxychloroquine amphiphilic polymer drug prodrug and its preparation method and application. Background technique [0002] Hydroxychloroquine (as shown in formula A) is a 4-aminoquinoline antimalarial drug, which can be used to treat systemic lupus erythematosus, rheumatoid arthritis and other immune diseases. Hydroxychloroquine is clinically used as oral hydroxychloroquine sulfate, and its pharmacology and mechanism of action are similar to chloroquine, but its toxicity is lower than that of chloroquine. The structural difference between hydroxychloroquine and chloroquine is that the N-ethyl group at the end of the side chain of chloroquine is hydroxylated, so it is named hydroxychloroquine. [0003] [0004] In recent years, more and more studies have found that hydroxychloroquine and chloroquine have various biological and pharmacological a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/60A61K31/4706A61P37/02A61P29/00A61P19/02A61P37/00
CPCA61K31/4706A61K47/6935A61P19/02A61P29/00A61P37/00A61P37/02
Inventor 刘祥瑞王惠芳白皓宇王砾莹唐建斌周珠贤申有青
Owner ZHEJIANG UNIV
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