Polymerized chloroquine fluorenylmethyl nanogel delivery system and preparation method thereof

A chloroquine fluorene methyl carbonyl nanometer and delivery system technology, which can be used in pharmaceutical formulations, powder delivery, drug combinations, etc., can solve the problems of insignificant treatment effect of advanced malignant tumors and no anti-tumor metastasis function, and achieve stable structure, High drug loading and the effect of inhibiting autophagy

Active Publication Date: 2020-06-09
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, since nanogels mostly use traditional gel materials and do not have anti-tumor metastasis function, the therapeutic effect on malig...

Method used

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  • Polymerized chloroquine fluorenylmethyl nanogel delivery system and preparation method thereof
  • Polymerized chloroquine fluorenylmethyl nanogel delivery system and preparation method thereof
  • Polymerized chloroquine fluorenylmethyl nanogel delivery system and preparation method thereof

Examples

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Embodiment 1

[0039] Preparation method of polymerized chloroquine-fluorenylmethylcarbonyl dextrin nanogel drug-loading system

[0040] Step 1, preparation of hydroxychloroquine: Dissolve 0.6 g of hydroxychloroquine sulfate in 2 mL of pure water, add excess 30% ammonia water under constant stirring until the white insoluble product does not continue to increase, add dichloromethane to extract 4 -6 times, the organic phase was collected and an appropriate amount of anhydrous sodium sulfate was added overnight, and the solvent was distilled off under reduced pressure to obtain the final desalted product.

[0041] Step 2, the synthesis of fluorenylmethylcarbonyl dextrin: Dissolve 210 mg dextrin in 2 mL dimethylformamide, add 206 mg dicyclohexylcarbodiimide, 24 mg 4-dimethylaminopyridine and 297 mg Fmoc-glycine, react for 12-24 h under an inert gas environment, remove the insoluble matter, add the reaction solution to 10 times the amount of anhydrous ether, centrifuge at a speed of 3000 rpm for...

Embodiment 2

[0047] Preparation method of polymerized chloroquine-fluorenylmethylcarbonyl dextran nanogel drug-loading system

[0048] Step 1, preparation of hydroxychloroquine: Dissolve 0.6 g of hydroxychloroquine sulfate in 2 mL of pure water, add excess 30% ammonia water under constant stirring until the white insoluble product does not continue to increase, add dichloromethane to extract 4 -6 times, the organic phase was collected and an appropriate amount of anhydrous sodium sulfate was added overnight, and the solvent was distilled off under reduced pressure to obtain the final desalted product.

[0049] Step 2, synthesis of fluorenylmethylcarbonyl dextran (HF): Dissolve 164 mg of dextran in 2 mL of dimethylformamide, add 206 mg of dicyclohexylcarbodiimide, 24 mg of 4-dimethylformamide Aminopyridine and 297 mg Fmoc-glycine were reacted for 12-24 h under an inert gas environment. After removing insoluble matter, the reaction liquid was added to 10 times the amount of anhydrous ether, ...

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Abstract

The invention discloses a polymerized chloroquine fluorenylmethyl nanogel delivery system. The delivery system comprises nanogel particles of polymerized chloroquine fluorenylmethyl and an anti-tumordrug wrapped in the particles. The nanogel particles are formed by crosslinking a polysaccharide main chain modified with hydroxychloroquine and fmoc-D-methionine, the molecular weight of the polysaccharide main chain is 5-100 kD, the molar substitution degree of the hydroxychloroquine on the polysaccharide main chain is 5%-50%, and the molar substitution degree of the fmoc-D-methionine on the polysaccharide main chain is 1%-30%. The polymerized chloroquine fluorenylmethyl nanogel delivery system can inhibit the autophagy level in cells and block a signal channel of tumor cell metastasis, meanwhile, entrap an antitumor drug paclitaxel through the pi-pi conjugation effect, and inhibit metastasis and proliferation of malignant tumors at the same time.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a polymerized chloroquine fluorenylmethylcarbonyl nanogel delivery system and a preparation method thereof. Background technique [0002] In China, the incidence of tumors has increased significantly in recent years, and most of them are patients with malignant tumors. The metastasis of malignant tumor cells has significantly increased the mortality of patients. Paclitaxel, a traditional chemotherapeutic drug, binds to intracellular tubulin and hinders microscopic protein dissociation, thereby blocking cell mitosis and promoting tumor cell apoptosis, which brings hope for tumor treatment. However, due to the extremely low water solubility of paclitaxel, the traditional paclitaxel injection needs to use a mixed solution of polyoxyethylene castor oil and absolute ethanol as a solubilizer, but polyoxyethylene castor oil will cause a series of allergic...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/337A61K31/438A61K47/54A61P35/00A61P35/04
CPCA61K9/0019A61K47/6939A61K31/337A61P35/00A61P35/04A61K31/438A61K47/542A61K2300/00
Inventor 孙敏捷董婧雯
Owner CHINA PHARM UNIV
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