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Prepn process of microcapsule with included anticancer medicine

A technology of anticancer drugs and microcapsules, which is applied in microcapsules, capsule delivery, pharmaceutical formulations, etc., can solve the problems of microcapsule or microsphere permeability and sustained release performance, cannot be guaranteed to be removed, and environmental pollution, etc., to achieve Excellent stability, good biocompatibility, wide range of effects

Inactive Publication Date: 2006-05-17
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the use of organic solvents and emulsifiers, not only may cause environmental pollution, but also cannot guarantee the complete removal of organic solvents and emulsifiers that are harmful to the human body in the preparation
In addition, the permeability and sustained release properties of microcapsules or microspheres prepared by emulsion method are usually difficult to control on the microscopic scale
Therefore, it is extremely challenging to find a drug carrier that is environmentally friendly, whose sustained-release performance can be precisely regulated, and has good comprehensive properties.

Method used

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  • Prepn process of microcapsule with included anticancer medicine
  • Prepn process of microcapsule with included anticancer medicine
  • Prepn process of microcapsule with included anticancer medicine

Examples

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example 1

[0040] Mix 50mL of calcium nitrate solution with a concentration of 0.025M / L and 100mg of polystyrene sodium sulfonate (PSS), and after 10 minutes, quickly add 50mL of a sodium carbonate solution with a concentration of 0.025M / L. After 15 minutes, the generated calcium carbonate containing PSS (expressed as CaCO 3 (PSS)) The precipitate was collected by centrifugation, washed 3 times with water, and stored. Prepared CaCO 3 The scanning electron micrographs of (PSS) particles are shown in figure 1 .

[0041] 1 mL (solid content 5-10%) of the above-mentioned CaCO with a diameter of 2-10 μm 3 (PSS) microparticles were placed in a 2 mL centrifuge tube. (1) Centrifuge to remove supernatant, wash with water 3 times. (2) Add 1 mL of polyallylamine hydrochloride (PAH) solution to 0.2-0.5 M / L NaCl solution, and shake the centrifuge tube. After 10 min, wash with water 3 times to remove excess PAH, thus the CaCO 3 (PSS) surface adsorbed a layer of PAH (expressed as CaCO 3 (PSS)-P...

example 2

[0044] (1) Dissolve 2 g (10 mmol) of p-toluenesulfonyl chloride (TsCl) in 50 mL of pyridine. Dissolve 5 g (2.5 mmol) of monomethoxypolyethylene glycol in 50 mL of dichloromethane, and add the above-mentioned TsCl solution in pyridine with stirring. React for 12 hours. The reaction product was extracted by adding 50mL of 3mol / L hydrochloric acid, and the organic layer was added with 2.5g NaHCO 3 , stirred and filtered to obtain crude polyethylene glycol p-toluenesulfonate (PEG-Ts). The crude PEG-Ts was dissolved in 5 mL THF with stirring, and precipitated with ether three times. The pure PEG-Ts was obtained after vacuum drying. (2) Take 2.38g (1.09mmol) of PEG-Ts, add 0.4335g (0.0062mmol) of PAH in borax solution (pH=9.18), stir, and react at room temperature for 24h. (3) Dialyzing the resulting product for a sufficient time to remove small molecule impurities. After lyophilization, the final product polyallylamine grafted with polyethylene glycol (PAH-g-PEG) was obtained....

example 3

[0047] Microcapsules were prepared as in Example 1, but the last layer replaced PAH with rhodamine-labeled PAH-g-PEG to obtain CaCO 3 (PSS) / (PAH / PSS) 4 / PAH-g-PEG microcapsules. After 10 seconds, observed under the laser confocal microscope, it was found that the rhodamine-labeled PAH-g-PEG was assembled on the microcapsules, which had a hollow and complete structure ( Figure 5 ).

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Abstract

The present invention discloses the preparation process of microcapsule with included anticancer medicine. The process adopts colloid particle containing polyelectrolyte as template, assembles polyelectrolytes with dislike charges via layer-by-layer self-assembling to the surface of colloid particle, and dissolves or decomposes the colloid particle to obtain hollow polymer microcapsule containing polyelectrolyte. The microcapsule has wall micro structure and thickness capable of being regulated precisely in nanometer size, and the contained polyelectrolyte can interact with the medicine so as to include the medicine into the microcapsule. The included medicine has controllable release speed. Introducing polyelectrolyte with grafted polyglycol to the surface of the microcapsule can raise the biocompatibility of the microcapsule. The process of the present invention is simple, feasible and repeatable, and suitable for inclusion and controllable release of various kinds of water soluble anticancer medicine.

Description

technical field [0001] The invention relates to a method for preparing layer-layer assembled microcapsules and using the microcapsules to embed anticancer drugs, in particular to a microcapsule with good water dispersibility, storage stability and sustained release performance and its preparation technology. technical background [0002] In clinical practice, a routine method for treating tumors is chemotherapy, that is, using chemical drugs to treat tumors. Daunorubicin and doxorubicin can be embedded in the DNA double helix and bind to DNA to change its template, inhibit DNA and RNA polymerase, prevent the synthesis of DNA and RNA, and are non-specific drugs for the cell cycle. Clinically used for acute and chronic leukemia, malignant lymphoma, gastric cancer, liver cancer, etc., it is a broad-spectrum anticancer drug. However, these two drugs are highly toxic, and in addition to killing cancer cells, they also have a strong killing effect on normal cells. Therefore, it ...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/704A61K35/00A61K47/32
Inventor 高长有赵庆贺张双沈家骢
Owner ZHEJIANG UNIV
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