Method for preparing nano-drug common delivery system based on pectin and multi-arm polyethylene glycol

A multi-arm polyethylene glycol and nano-drug technology, which is applied in drug delivery, capsule delivery, drug combination, etc., can solve the problems of unclear effective treatment measures for colon cancer, low bioavailability, and short half-life in vivo. Good clinical application prospects, prolonging the time of taking medicine, and low toxicity and side effects

Inactive Publication Date: 2016-08-31
BEIJING FORESTRY UNIVERSITY
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Problems solved by technology

[0002] Colon cancer (colorectal cancer, referred to as CRC) is one of the common malignant tumors of the digestive tract, the third most common cancer, and the fourth fatality rate in the world. However, the effective treatment measures for colon cancer are still unclear. Various drugs such as dihydroartemisinin (DHA) and betulinic acid (BA) have inhibitory effects on colon cancer, and their bioavailability is not high when taken orally. Short, requires continuous intravenous administration, high toxicity and side effects, such as making DHA and BA into a colon-targeted drug delivery system that achieves a higher drug concentration in the local tumor, will bring important clinical application value to the cure of colon cancer

Method used

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  • Method for preparing nano-drug common delivery system based on pectin and multi-arm polyethylene glycol

Examples

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Embodiment 1

[0021] Embodiment 1, a kind of preparation method based on pectin and multi-armed polyethylene glycol co-delivery system of nano-medicine:

[0022] 1. Dissolve 0.5g PET with 10ml dimethylsulfoxide (DMSO) or pyridine (Py), then add 0.52g activator 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride Salt (EDC), 0.06g catalyst 4-dimethylaminopyridine (DMAP), stir, then add 1g dihydroartemisinin to react for 48h, add 3V diethyl ether to precipitate, stir evenly, discard the supernatant after centrifugation, repeat this 5 times , and vacuum-dry the final precipitate to obtain PET-DHA powder A;

[0023] 2. Dissolve 0.5g of eight-armed polyethylene glycol in 5ml of tetrahydrofuran, add 0.55g of EDC, 0.05g of DMAP and 1g of betulinic acid (BA), react for 12h, then add 3V ether / ethanol to precipitate, centrifuge to remove the supernatant, The lower precipitate was dissolved in chloroform, washed several times with methanol, centrifuged, and the precipitate was vacuum-dried to ...

Embodiment 2

[0026] Embodiment 2, a kind of preparation method based on pectin and multi-arm polyethylene glycol co-delivery system of nano-medicine:

[0027] In this example, through the same synthesis method and steps as in Example 1, the molar ratio of PET to DHA is 1:5, the molar ratio of 8ARM-PEG-COOH to BA is 1:1, and the particle size measured is 20 ~100nm.

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Abstract

The invention discloses a method for preparing a nano-drug common delivery system based on a pectin and multi-arm polyethylene glycol and particularly relates to a novel pectin nano-drug. A pectin (PET) and eight-arm polyethylene glycol (8 ARM-PEG-COOH) serve as carriers and load dihydroartemisinin (DHA) and betulinic acid (BA) together; firstly, eight-arm polyethylene glycol reacts with betulinic acid (BA) to form polyethylene glycol-dihydroartemisinin (8 ARM-PEG-BA), the pectin reacts with a certain amount of dihydroartemisinin to form pectin-dihydroartemisinin (PET-DHA), then 8 ARM-PEG-BA reacts with PET-DHA to form BA-PEG-PET-DHA, then BA-PEG-PET-DHA and 10-hydroxycamptothecine (HCPT) are self-assembled to form nano particles BA-PEG-PET-DHA (HCPT).NPs, drug loading efficiency is high, and targeting performance is high. The method for preparing the nano-drug common delivery system based on the pectin and multi-arm polyethylene glycol has the sustained release function, pectin and multi-arm polyethylene glycol are good in biocompatibility, and the formed nano-drug is low in toxicity. The method belongs to the fields of biopharmacy and nanotechnology. The preparation process is simple, operation is convenient, and the experiment period is short.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals and nanotechnology, and relates to a drug delivery system, in particular to a preparation method of a pectin- and multi-arm polyethylene glycol-based nano-medicine co-delivery system. Background technique [0002] Colon cancer (colorectal cancer, referred to as CRC) is one of the common malignant tumors of the digestive tract, the third most common cancer, and the fourth fatality rate in the world. However, the effective treatment measures for colon cancer are still unclear. Various drugs such as dihydroartemisinin (DHA) and betulinic acid (BA) have inhibitory effects on colon cancer, and their bioavailability is not high when taken orally. Short, requires continuous intravenous administration, high toxicity and side effects, such as making DHA and BA into a colon-targeted drug delivery system that achieves a higher drug concentration in the local tumor, will bring important clinical application ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/36A61K47/10A61K31/366A61K31/56A61K31/4745A61P35/00
CPCA61K9/0002A61K9/5146A61K9/5161A61K31/366A61K31/4745A61K31/56
Inventor 雷建都刘彦雪何静刘静王璐莹晋禄禄
Owner BEIJING FORESTRY UNIVERSITY
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