Chloroquine-polymerized nanogel delivery system and preparation method thereof

A nanogel and delivery system technology, applied in the field of chemotherapy drug delivery system and its preparation, can solve the problems of inability to deliver multiple substances at the same time, inability to achieve multifunctional modification, large particle size, etc., and achieve controllable loading capacity. , Inhibition of cancer cell proliferation, the effect of controllable amount of modification

Inactive Publication Date: 2017-11-24
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The first prior art achieves the delivery of chemotherapeutic drugs by forming prodrugs, but its particle size is large and cannot deliver multiple substances at the same time; Modification of function

Method used

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  • Chloroquine-polymerized nanogel delivery system and preparation method thereof
  • Chloroquine-polymerized nanogel delivery system and preparation method thereof
  • Chloroquine-polymerized nanogel delivery system and preparation method thereof

Examples

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Effect test

Embodiment 1

[0051] Embodiment 1 A kind of preparation method of hydroxychloroquine-lauric acid-hydroxyethyl starch

[0052] (1) Synthesis of hydroxychloroquine: Dissolve 1 g of hydroxychloroquine sulfate in 2 ml of pure water, add 2 ml of 30% ammonia water dropwise under constant stirring until a white insoluble product is produced, add dichloromethane to extract the aqueous phase 4-6 Once, the organic phase was collected and anhydrous sodium sulfate was added overnight, and the solvent was distilled off under reduced pressure to obtain the final desalted product hydroxychloroquine.

[0053] (2) Synthesis of lauric acid-hydroxyethyl starch: Dissolve 100 mg of hydroxyethyl starch in 2 ml of dimethyl sulfoxide, add 124 mg of dicyclohexylcarbodiimide and 127 mg of 4-dimethylaminopyridine and 30 mg of lauric acid, reacted for 12-18 hours under the protection of an inert gas, and removed the insoluble matter by suction filtration, then added the reaction solution to 10 times the amount of anhy...

Embodiment 2

[0056] Embodiment 2 A kind of preparation method of hydroxychloroquine-lauric acid-hyaluronic acid

[0057] (1) Synthesis of hydroxychloroquine: Dissolve 1 g of hydroxychloroquine sulfate in 2 ml of pure water, add 2 ml of 30% ammonia water dropwise under constant stirring until a white insoluble product is produced, add dichloromethane to extract the aqueous phase 4-6 Once, the organic phase was collected and anhydrous sodium sulfate was added overnight, and the solvent was distilled off under reduced pressure to obtain the final desalted product hydroxychloroquine.

[0058] (2) Synthesis of lauric acid-hyaluronic acid: Dissolve 100 mg of hyaluronic acid in 2 ml of dimethyl sulfoxide, add 103 mg of dicyclohexylcarbodiimide, 103 mg of 4-dimethylaminopyridine and 25.7 mg lauric acid, react for 12-18 hours under the protection of an inert gas, remove the insoluble matter by suction filtration, add the reaction solution to 10 times the amount of anhydrous ether, filter with sucti...

Embodiment 3

[0060] Embodiment 3 A kind of preparation method of hydroxychloroquine-lauric acid-dextran

[0061] (1) Synthesis of hydroxychloroquine: Dissolve 1 g of hydroxychloroquine sulfate in 2 ml of pure water, add 2 ml of 30% ammonia water dropwise under constant stirring until a white insoluble product is produced, add dichloromethane to extract the aqueous phase 4-6 Once, the organic phase was collected and anhydrous sodium sulfate was added overnight, and the solvent was distilled off under reduced pressure to obtain the final desalted product hydroxychloroquine.

[0062](2) Synthesis of lauric acid-dextran: Dissolve 100 mg dextran in 2 ml dimethyl sulfoxide, add 240 mg dicyclohexylcarbodiimide, 240 mg 4-dimethylaminopyridine and 60 mg Lauric acid, react for 12-18 hours under the protection of an inert gas, remove the insoluble matter by suction filtration, add the reaction solution to 10 times the amount of anhydrous ether, filter with suction, dissolve the solid with ultrapure w...

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Abstract

The invention discloses a chloroquine-polymerized nanogel delivery system and a preparation method thereof. The delivery system contains chloroquine-polymerized nanogel particles, and antitumor medicines which are wrapped with the particles, wherein the chloroquine-polymerized nanogel is prepared through hydroxychloroquine and polysaccharide framework which is modified through a hydrophobic side chain. According to the medicine delivery system, malignant tumor and tumor metastasis are treated synchronously; the signal cascade of cancer cells metastasizing to surrounding and distant sides is stopped while cancer cell proliferation is inhibited, and malignant cancer can be effectively treated.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations and the field of biomedicine technology, in particular to a chemotherapeutic drug delivery system using hydroxyethyl starch polymerized with hydroxychloroquine as a carrier and a preparation method thereof. Background technique [0002] Tumor is a malignant disease that seriously threatens human health and life. The vast majority of malignant tumors are only discovered in the late stage of the disease, when the cancer cells have already infiltrated and metastasized severely in the lungs, liver, lymph nodes and other tissues, and are often accompanied by perineural infiltration with a worse prognosis. Although the nano drug delivery system has achieved many achievements in the treatment of most tumors, the therapeutic effect on metastatic malignant tumors is not significant, which is related to its inability to enrich in secondary metastases of cancer. Therefore, new methods must be soug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/61A61K47/36A61K31/4706A61K31/337A61K31/704A61K31/4745A61K31/12A61P35/00
CPCA61K9/06A61K31/12A61K31/337A61K31/4706A61K31/4745A61K31/704A61K47/36A61K2300/00
Inventor 大卫欧佩奇孙敏捷张斐然
Owner CHINA PHARM UNIV
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