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Liver targeting taxol nanometer suspension and preparation method thereof

A nanosuspension, paclitaxel technology, applied in the field of medicine, can solve the problems of inability to administer intravenously, low solubility of paclitaxel, and large toxic and side effects of preparations, and achieves good application prospects, improved therapeutic effects, and increased drug dosage effects.

Inactive Publication Date: 2015-04-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Aiming at the problems of low paclitaxel solubility, poor bioavailability, high toxicity and side effects of existing preparations, and inability to be used for intravenous administration, the present invention designs a paclitaxel nanosuspension with stable liver-targeting material, which utilizes the surface of liver parenchymal cells The asialoglycoprotein receptor specifically recognizes galactose ligand and receptor-mediated phagocytosis, and delivers the drug to the liver for targeted drug delivery

Method used

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  • Liver targeting taxol nanometer suspension and preparation method thereof
  • Liver targeting taxol nanometer suspension and preparation method thereof
  • Liver targeting taxol nanometer suspension and preparation method thereof

Examples

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Embodiment 1

[0032] Synthesis of lactobionic acylated poloxamer F127 (GLC-F127): (1) Dissolve 5 g of poloxamer F127 in 50 mL of acetone, then add 60 mL of pre-cooled n-hexane to precipitate poloxamer F127, Filter and dry in vacuo to obtain purified poloxamer F127. Dissolve 0.63 g of purified poloxamer F127 and 0.24 g of NaH in 15 mL of anhydrous chloroform, and add 0.1 g of 2-bromoethylamine hydrobromide (BrCH 2 CH 2 NH 3 Br) was dissolved in an appropriate amount of chloroform, and then the BrCH 2 CH 2 NH 3 The chloroform solution of Br was slowly added dropwise to the above solution within 1 h under nitrogen protection, and magnetically stirred at room temperature for 24 h. After the reaction, dialyze with deionized water for 24 hours, and vacuum freeze-dry to obtain F127-NH 2 White crystalline powder (2) Dissolve 1.136g of lactobionic acid, 0.3g of NHS, 0.42g of EDC·HCl and 0.03g of DMAP in 10mL of anhydrous DMSO, add 0.1mL of triethylamine, protect it under nitrogen, and stir mag...

Embodiment 2

[0034] Preparation of liver-targeted paclitaxel nanosuspension: 4 mg of paclitaxel was accurately weighed, dissolved in 2 mL of methanol, and magnetically stirred until completely dissolved to obtain solution A. Accurately weigh 16 mg of poloxamer F127-GLC and dissolve it in 48 mL of water, and magnetically stir until completely dissolved to obtain solution B. Under the condition of ultrasonication in an ice bath, slowly inject solution A into solution B with a syringe, and ultrasonicate at 400W for 5min. Methanol was removed by rotary evaporation at 40°C, and the obtained crude nanosuspension was placed in a high-pressure homogenizer, and homogenized 15 times at 0°C and 800 bar pressure to obtain the liver-targeted paclitaxel nanosuspension. The particle size is 179.1 nm, and the polydispersity coefficient is 0.19.

Embodiment 3

[0036] Preparation of liver-targeted paclitaxel nanosuspension: Accurately weigh 16 mg of paclitaxel, dissolve in 2 mL of methanol, and magnetically stir until completely dissolved to obtain solution A. Accurately weigh 64mg of poloxamer F127-GLC and dissolve it in 48mL of water, and magnetically stir until completely dissolved to obtain solution B. Under the condition of ultrasonication in an ice bath, slowly inject solution A into solution B with a syringe, and ultrasonicate at 400W for 5min. Methanol was removed by rotary evaporation at 40°C, and the obtained crude nanosuspension was placed in a high-pressure homogenizer, and homogenized 15 times at 0°C and 800 bar pressure to obtain the liver-targeted paclitaxel nanosuspension. The particle size is 182.3 nm, and the polydispersity coefficient is 0.21.

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Abstract

The invention discloses a liver targeting taxol nanometer suspension and a preparation method of the liver targeting taxol nanometer suspension. Taxol serves as therapeutic, poloxamer F127 modified by lactobionic acid serves as a stabilizer, the liver targeting taxol nanometer suspension is prepared with an ultrasonic coprecipitation united high pressure homogenizing method, the particle size ranges from 160 nm to 200 nm, and the polydispersity index is 0.2 + / - 0.012. According to the nanometer suspension, the galactose residue on the poloxamer F127 is acylated by lactobionic acid, asialoglycoprotein receptors on liver surface parenchyma cells are recognized, and the effect of liver targeted drug delivery is achieved.

Description

technical field [0001] The invention relates to a liver-targeted paclitaxel nanosuspension and a preparation method thereof, belonging to the field of medicine. Background technique [0002] Paclitaxel (PTX) is a tetracyclic diterpene antineoplastic drug extracted and isolated from the bark of Taxus brevifolia in 1971 by American chemists Wall and Wani. Horwitz et al. reported its mechanism of action in 1979. Due to its unique mechanism of action and curative effect, since the 1990s, it has been approved by the US FDA to be used independently or in combination with other drugs for advanced ovarian cancer, metastatic breast cancer, non-small cell lung cancer and Kpaosi's related to AIDS. Tumor treatment, showing broad application and development prospects. The molecular formula of paclitaxel is C 47 h 51 NO 14 , the molecular weight is 853.92, and the structural formula is as follows: [0003] [0004] The solubility of paclitaxel in water is very low, about 4μg.mL ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/337A61K47/34A61K47/26A61P35/00A61P1/16
Inventor 王柏刘学印
Owner CHINA PHARM UNIV
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