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Glycyrrhetinic acid prodrug micelle for jointly carrying chemotherapy drug and preparation method thereof

A technology of glycyrrhetic acid and chemotherapeutic drugs is applied in the field of glycyrrhetic acid prodrug micelles and preparation thereof, which can solve the problems of large toxic and side effects, limited application of chemotherapeutic drugs, lack of selectivity in anti-tumor effects, etc. drug resistance, increased entrapment capacity, and enhanced synergistic antitumor efficacy

Active Publication Date: 2018-10-19
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most chemotherapy drugs have anti-tumor effects, lack of selectivity, high toxicity and side effects, and face the challenge of tumor drug resistance, which severely limits the clinical application of chemotherapy drugs.

Method used

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  • Glycyrrhetinic acid prodrug micelle for jointly carrying chemotherapy drug and preparation method thereof
  • Glycyrrhetinic acid prodrug micelle for jointly carrying chemotherapy drug and preparation method thereof
  • Glycyrrhetinic acid prodrug micelle for jointly carrying chemotherapy drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: the synthesis of PEG-GA polymer prodrug

[0036] 5 g polyethylene glycol monomethyl ether (molecular weight: 2K), 0.56 g lysine (Boc) 2 , 0.35 g DCC, and 0.01 g DMAP were dissolved in 25 mL of dichloromethane, and reacted with magnetic stirring at room temperature for 1 day, separated and purified by absolute ethanol and ether, and dried under reduced pressure to obtain PEG-lysine as a white solid Acid (Boc) 2 polymer.

[0037] 1 g PEG-Lysine (Boc) 2 The polymer was dissolved in 1.5 mL of dichloromethane and 1.5 mL of trifluoroacetic acid, stirred magnetically at room temperature for 0.5 h, separated and purified by ether, and dried under reduced pressure to obtain a pale yellow oily PEG-lysine polymer de-Boc grouped.

[0038] 1 g of PEG-lysine polymer, 3 g of GA, 0.6 g of DCC and 0.01 g of DMAP were co-dissolved in 10 mL of dichloromethane, stirred at room temperature for 1 day, separated and purified by absolute ethanol and diethyl ether, and reduced ...

Embodiment 2

[0039]Embodiment 2: the synthesis of PEG-GA polymer prodrug

[0040] 5 g polyethylene glycol monomethyl ether (molecular weight: 5K), 1.2 g lysine (Boc) 2 , 0.7 g DCC and 0.04 g DMAP were dissolved in 20 mL of methanol, and reacted with magnetic stirring at room temperature for 3 days, separated and purified by diethyl ether and absolute ethanol, and dried under reduced pressure to obtain a white solid PEG-lysine ( Boc) 2 polymer.

[0041] 1 g PEG-Lysine (Boc) 2 The polymer was dissolved in 5 mL of dichloromethane and 5 mL of trifluoroacetic acid, stirred with magnetic force at room temperature for 2 h, separated and purified by diethyl ether and absolute ethanol, and dried under reduced pressure to obtain a light yellow oily PEG-lysine de-Boc grouped Acid polymers.

[0042] 1 g PEG-lysine polymer, 1.5 g GA, 0.3 g DCC, and 0.02 g DMAP were co-dissolved in 5 mL chloroform and 20 μL triethylamine, and reacted with magnetic stirring at room temperature for 3 days. Separation...

Embodiment 3

[0043] Embodiment 3: the synthesis of PEG-GA polymer prodrug

[0044] 5 g polyethylene glycol monomethyl ether (molecular weight: 2K), 2.5 g lysine (Boc) 2 , 2 g of DCC and 1 g of DMAP were dissolved in 20 mL of dichloromethane and 5 mL of tetrahydrofuran, reacted with magnetic stirring at room temperature for 7 days, separated and purified by petroleum ether, diethyl ether and absolute ethanol, and dried under reduced pressure to obtain White solid PEG-lysine (Boc) 2 polymer.

[0045] 1 g PEG-Lysine (Boc) 2 The polymer was dissolved in 2.5 mL of dichloromethane and 2.5 mL of trifluoroacetic acid, stirred with magnetic force at room temperature for 6 h, separated and purified by petroleum ether and diethyl ether, and dried under reduced pressure to obtain PEG-lysine de-Boc grouped as light yellow oil acid polymer.

[0046] 1 g of PEG-lysine polymer, 2.8 g of GA, 1.3 g of DCC and 0.45 g of DMAP were co-dissolved in 4 mL of dichloromethane and 1 mL of tetrahydrofuran, and 65...

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Abstract

The invention relates to a glycyrrhetinic acid prodrug micelle for jointly carrying chemotherapy drug and a preparation method thereof. The micelle uses polyethylene glycol-glycyrrhetinic acidpolymerprodrug as a carrier; the chemotherapy drug is physically embedded and carried in the glycyrrhetinic acid prodrug micelle. The chemotherapeutic medicine and glycyrrhetinic acid are combined; a nanometer technology is used for building a chemotherapy drug carrying prodrug micelle co-delivery system; by regulating and controlling the bridging molecule number of lysine and glycyrrhetinic acid in polyethylene glycol-glycyrrhetinic acid prodrug, the jointly carrying proportion of the glycyrrhetinic acid and chemotherapeutic medicine can be regulated and controlled; the optimum combined chemotherapyproportioning ratio of the combined use drug is realized. Compared with the carrying of two kinds of drug jointly in a physical mode, the glycyrrhetinic acid prodrug micelle uses the jointly drug carrying mode of combining physical joint carrying and chemical bonding, the carrying quantity of the combined use drug can be obviously improved; the medicine delivery efficiency of the polymer prodrugmicelle can be improved.

Description

technical field [0001] The invention belongs to the field of polymer materials and new formulations of pharmaceutical preparations, in particular to a glycyrrhetinic acid prodrug micelle co-carrying chemotherapeutic drugs and a preparation method thereof. Background technique [0002] Malignant tumors are one of the most important diseases that seriously threaten human health. Chemotherapy is currently the main means of treating tumors. Cytotoxic chemotherapy drugs, such as paclitaxel, dasatinib, cisplatin, camptothecin, hydroxycamptothecin, topotecan, doxorubicin, 5-fluorouracil, vincristine, etc., constitute the classics of modern tumor chemotherapy. model. However, most chemotherapeutic drugs have a lack of selectivity in anti-tumor effects, high toxicity and side effects, and the challenge of tumor drug resistance, which severely limits the clinical application of chemotherapeutic drugs. At present, the treatment of tumors has changed from a single drug to a combinatio...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K45/06A61K31/56A61K47/60A61P35/00C08G65/333C08G65/331
CPCA61K9/1075A61K31/56A61K45/06A61K47/60A61P35/00C08G65/3314C08G65/33306A61K2300/00
Inventor 刘艳华杨彤杨建宏兰杨曹爱晨
Owner NINGXIA MEDICAL UNIV
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