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Docetaxel and berbamine double-load drug chitosan nanoparticles and preparation method thereof

A chitosan nanoparticle and docetaxel technology, which is applied in the directions of pharmaceutical formulations, antitumor drugs, and drug combinations, can solve the problems of poor absorption and low solubility of docetaxel, and achieves increased drug absorption, convenient use, and improved drug absorption. The effect of oral bioavailability

Inactive Publication Date: 2016-10-19
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The preparation of docetaxel into oral preparations needs to overcome many obstacles, such as the low solubility of docetaxel (<10 μg / mL), poor absorption, and docetaxel is the substrate of P-gp efflux protein and CYP3A metabolic enzyme, which has been Docetaxel absorbed into cells is also easily recognized by P-gp efflux proteins or metabolized by CYP3A in the liver to be excreted

Method used

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  • Docetaxel and berbamine double-load drug chitosan nanoparticles and preparation method thereof
  • Docetaxel and berbamine double-load drug chitosan nanoparticles and preparation method thereof
  • Docetaxel and berbamine double-load drug chitosan nanoparticles and preparation method thereof

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Embodiment 1

[0054] This embodiment relates to a preparation method of docetaxel-nicotinamide co-crystal, comprising the following steps:

[0055]Add 5 mg of docetaxel and nicotinamide (molar ratio 1:1) into 2.5 mL of methanol, and stir at 50° C. at 200 rpm for 2 h. The methanol solvent system is cooled to room temperature in a fume hood, the solvent in the system is slowly volatilized to precipitate crystals, and then dried in a vacuum desiccator.

[0056] In the present embodiment, the XRD characterization of the docetaxel-nicotinamide cocrystal is as follows figure 1 shown by figure 1 It can be seen that both docetaxel and nicotinamide have obvious crystal diffraction peaks; in the spectrum of the physical mixture, the characteristic diffraction peaks of docetaxel are relatively obvious, and the characteristic peaks of nicotinamide are weakened, but there is no disappearance of the characteristic peaks; In the spectrum of the compound, the characteristic diffraction peaks of docetaxel...

Embodiment 2

[0058] This embodiment relates to a preparation method of docetaxel-nicotinamide co-crystal, comprising the following steps:

[0059] Add 5 mg of docetaxel and nicotinamide (molar ratio 1:10) into 5 mL of methanol, and stir at 60° C. at 500 rpm for 2 h. The methanol solvent system is cooled to room temperature in a fume hood, the solvent in the system is slowly volatilized to precipitate crystals, and then dried in a vacuum desiccator.

[0060] In this embodiment, the solubility of the docetaxel-nicotinamide co-crystal in water is 31 μg / mL.

Embodiment 3

[0062] This embodiment relates to a preparation method of docetaxel-nicotinamide co-crystal, comprising the following steps:

[0063] Add 5 mg of docetaxel and nicotinamide (molar ratio 1:20) into 20 mL of ethanol, and stir at 1500 rpm at 40° C. for 24 h. The ethanol solvent system is cooled to room temperature in a fume hood, the solvent in the system is slowly volatilized to precipitate crystals, and then dried in a vacuum desiccator. The docetaxel-nicotinamide co-crystal formation rate in this example was 97.6%.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to docetaxel and berbamine double-load drug chitosan nanoparticles and a preparation method thereof. According to the nanoparticles, docetaxel and nicotinamide are prepared into eutectic crystals, and then chitosan nanoparticles are covered with the eutectic crystals and berbamine at the same time. According to the oral taking nanoparticles, the eutectic crystals are formed by nicotinamide and a main drug, and the water solubility of nicotinamide is improved. The sensibilization of berbamine is utilized for promoting apoptosis of cancer cells; chitosan is utilized for prolonging the retention time of the drug in the body and reducing the in-vivo clearance rate of the drug. Docetaxel, berbamine and chitosan are combined for use and prepared into the nanoparticles, the nanoparticles are absorbed by the gastrointestinal tract after being orally taken, and the function of remarkably improving the oral taking bioavailability of paclitaxel is achieved. The preparation method of the nanoparticles is simple, the production cost is low, and mass production is easy.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a docetaxel and berbamine double-loaded chitosan nanoparticle and a preparation method thereof. Background technique [0002] Docetaxel, a second-generation taxane compound, is one of the most effective broad-spectrum anticancer drugs. At present, the dosage forms of docetaxel on the market are Taxotere and Abraxane for injection. Due to the extremely low solubility of docetaxel in water, Taxotere contains Tween-80 as a co-solvent, and a large amount of ethanol is added to solubilize it before clinical use, which makes the existence of Taxotere serious. toxicity and sensitization. Compared with injections, oral preparations have many advantages, such as strong patient compliance, no need for specialized medical staff to administer injections, and lower C max Toxic and side effects caused by excessive dosage, etc., therefore, docetaxel oral prepar...

Claims

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Application Information

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IPC IPC(8): A61K31/4748A61K47/36A61K47/02A61K9/14A61P35/00A61K31/337
CPCA61K9/146A61K31/337A61K31/4748A61K2300/00
Inventor 沈琦李静吴健张君
Owner SHANGHAI JIAO TONG UNIV
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