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Carmustine supported glioma targeted polymer micelle and preparation method thereof

A glioma targeting and polymer glue technology, which is applied in the direction of medical preparations with non-active ingredients, polymer compound non-active ingredients, medical preparations containing active ingredients, etc., to achieve clinical transformation and increase cycle time , Conducive to the effect of pooling and concentration

Active Publication Date: 2016-11-23
毕云科 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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It is unbearable for patients

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  • Carmustine supported glioma targeted polymer micelle and preparation method thereof
  • Carmustine supported glioma targeted polymer micelle and preparation method thereof
  • Carmustine supported glioma targeted polymer micelle and preparation method thereof

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preparation example Construction

[0034] In one embodiment of the present invention, the preparation method of the glioma targeting polymer micelles loaded with carmustine comprises the following steps:

[0035] 1) prepare polyethylene glycol-polylactic acid-glycolic acid copolymer;

[0036] 2) Prepare T7 peptide-modified polyethylene glycol-polylactic acid-glycolic acid copolymer;

[0037] 3) The polyethylene glycol-polylactic acid-glycolic acid copolymer prepared in step 1) and the T7 peptide-modified polyethylene glycol-polylactic acid-glycolic acid copolymer prepared in step 2) were mixed with carmustine according to 10:1 mass ratio mixed with solvent to dissolve, after removing the solvent, a film of polymer micelles was obtained;

[0038] 4) Dispersing the film of polymer micelles obtained in step 3) in a hydration medium to obtain carmustine-loaded glioma-targeting polymer micelles.

[0039] In one embodiment of the present invention, in the preparation method of glioma-targeting polymer micelles load...

Embodiment 1

[0056] Example 1: Synthesis of T7-PEG-PLGA amphiphilic material.

[0057] (1) Add 0.4g (0.1mmol) carboxy-terminated polylactic acid-glycolic acid copolymer (PLGA, molecular weight 4000) to 5ml anhydrous dimethylformamide (DMF) at room temperature, then add 30.2mg (0.2mmol) N-hydroxysuccinimide (NHS) and 57.5mg (0.3mmol) 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) were added to the above solution, and Stir the reaction at room temperature for 24 hours; then add 0.5 g (0.1 mmol) of aminated polyethylene glycol derivatives (Mal-PEG-NH 2 , molecular weight 5000), continued to react for 2 hours; after the reaction was completed, the reactant was transferred to a dialysis bag (molecular weight 5000), and lyophilized after dialysis in pure water for 24 hours to obtain pure product amphiphilic material maleimide Group-terminated polyethylene glycol-polylactic acid-glycolic acid copolymer (Mal-PEG-PLGA);

[0058] (2) Dissolve the above-mentioned amphiphilic mate...

Embodiment 2

[0062] Example 2: Preparation of carmustine-loaded glioma-targeting micelles (T7-PEG-PLGA / BCNU) and carmustine-loaded glioma non-targeting micelles (mPEG-PLGA / BCNU) .

[0063] Weigh 8mg mPEG-PLGA, 2mg pure T7-PEG-PLGA, 1mg BCNU original drug and put them in a 10ml round bottom flask, add 5ml dichloromethane to dissolve completely; distill under reduced pressure on a rotary evaporator for 15 minutes to completely Remove the organic solvent and form a uniform transparent film on the wall of the round bottom flask; add 1ml of triple distilled water to the bottle, equilibrate with ultrasound for 15 minutes to completely disperse the film on the wall of the bottle, and continue stirring for 30 minutes at room temperature; filter the resulting solution carefully The insoluble drug was removed, and finally the glioma-targeted micelles loaded with BCNU (hereinafter referred to as T7-PEG-PLGA / BCNU) were obtained.

[0064] The result is as follows:

[0065] The particle diameter of th...

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Abstract

The invention provides a carmustine supported glioma targeted polymer micelle. The micelle contains a polyethylene glycol-polylactic acid-glycolic acid copolymer, T7 peptide modified polyethylene glycol-polylactic acid-glycolic acid copolymer and carmustine, wherein the mass ratio of the polymer micelle to the drug carmustine is 10 to 1. The invention further provides the polymer and a preparation method of a targeted micelle, namely a thin-film hydration method. According to the method, the stable polymer micelle having specific targeted brain capillary endothelial and glioma cells can be formed. Compared with traditional treatment drugs, the targeted micelle has the strongest toxic effect of the glioma cells and can greatly reduce the side effects on the whole body. In addition, it is shown through HPLC testing that the targeted drug can be still close to a 100% original drug after being saved at the room temperature for one week. Therefore, the polymer micelle can be applied to conventional treatment means such as intravenous injection of carmustine, and a novel implementable way is provided for BCNU having application defects existing at present.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a glioma targeting micelle loaded with carmustine and a preparation method thereof. Background technique [0002] The structural formula of Carmustine (trade name BCNU) is as follows: [0003] [0004] Carmustine is an alkylating anti-tumor drug, which has the advantages of high fat solubility, small molecular weight, and low plasma protein binding rate. It can quickly pass through the blood-brain barrier and exert its anti-tumor effect through the alkylation of DNA and RNA. It is considered as the "gold standard" of intracranial glioma chemotherapy. However, the plasma half-life of BCNU is short, only 15-20 minutes, and the blood concentration is almost 0 24 hours after administration, and the local tumor cannot reach the effective concentration and time of action. Increased drug doses can lead to systemic side effects such as bone marrow suppression a...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/175A61K47/42A61K47/34A61P35/00
Inventor 毕云科赵世光蒋晨卢逸飞
Owner 毕云科
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