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Targeted sustained release medicine carrying nanoparticle and preparation method thereof

A drug-loaded nano- and nano-microsphere technology, which is applied in the fields of pharmaceutical formulations, antineoplastic drugs, and drug combinations, can solve problems such as insufficient research, and achieve the effects of prolonging the action time, uniform size, and smooth shape

Active Publication Date: 2014-12-31
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because its research is mostly used in fluorescence imaging and imaging therapy, there are still insufficient researches on its drug loading and drug release.

Method used

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  • Targeted sustained release medicine carrying nanoparticle and preparation method thereof
  • Targeted sustained release medicine carrying nanoparticle and preparation method thereof
  • Targeted sustained release medicine carrying nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Adopt emulsification-solvent volatilization method to prepare the method for nano microsphere:

[0051] A FA-PEG-PLGA / PEG-PLGA-CAP+CAP / TMOS nanosphere, which contains chemically bonded and physically encapsulated capecitabine molecules, and the degradable carrier I is FA-PEG-PLGA connected with a targeting agent The degradable carrier II is a polymer compound of PEG-PLGA-CAP connected with the anti-tumor drug capecitabine, the carrier I and the carrier II are mixed at a ratio of 1:3, and the oil phase uses dichloromethane . The surfactant concentrations of the two emulsifications were 4% and 1%, respectively. The twice emulsified surfactant solution is 2 times and 30 times the volume of dichloromethane respectively, the amount of the CAP substance added in the preparation is 13 times the amount of the substance bonded to the drug, and the amount of the TMOS substance added is the carrier 100 times the amount of the total substance. Its specific preparation scheme is:...

Embodiment 2

[0064] The difference between this embodiment and embodiment 1 is:

[0065] The amount of the organic solvent in step 1) in Example 1 was 15 mL. The volume of the PVA aqueous solution in step 4) is 30mL, and the volume of the PVA aqueous solution in step 5) is 450mL.

[0066] The obtained nano-microspheres were tested and characterized by a laser particle size analyzer and a scanning electron microscope, and it was found that the particle size of the nano-microspheres in this example was smaller than that in Example 1, with an average of 190 nm; the surface roughness increased. This is because in this embodiment, the volume of the organic solvent increases and the viscosity of the oil phase decreases, so the carrier and the drug are more easily dispersed into fine droplet sizes. In addition, the increase of the oil phase also shortens the volatilization distance of the oil phase, accelerates the solidification speed of the nano-microspheres, and increases the surface roughnes...

Embodiment 3

[0068] The difference between this embodiment and embodiment 1 is:

[0069] The volume of the PVA aqueous solution in step 5) in Example 1 was adjusted to 500 mL, that is, the volume of the second emulsified surfactant solution was 50 times the volume of the organic solvent. The obtained nano-microspheres were tested and characterized by a laser particle size analyzer and a scanning electron microscope, and it was found that the particle size of the nano-microspheres in this example was smaller than that in Example 1, and the surface roughness was increased. This is because in this embodiment, the volume of the outer water phase increases, and the volatilization speed of the oil phase solvent accelerates, so the solidification time of the nano-microspheres is shortened, and the higher flow pressure will form a porous structure on the surface and inside of the microspheres, resulting in nano-microspheres. The number of voids on the surface of the ball increases, and the surface...

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Abstract

The invention discloses a targeted sustained release medicine carrying nanoparticle and a preparation method thereof. A mixture of a carrier I containing tumor targeted molecules and a carrier II containing antineoplastic drugs serves as a carrier of the nanoparticle, an organo-siloxane reagent easily hydrolyzed serves as a silane coupling reagent, and the nanoparticle which has a core-shell structure including that drugs are wrapped in the core through chemical bond connection and in a physical mode and the targeted molecules are exposed outside is obtained through micro emulsion technical preparation. The drugs are wrapped on the nanoparticle through a chemical method and the physical method, the mass fraction of the drugs in a nanoparticle is increased, preliminary-stage release is slowed down, and later-stage release is supplemented. The organo-siloxane reagent forms another layer of shell on a macromolecule two-block interface layer due to strong hydrolysis of the organo-siloxane reagent and the characteristic that the organo-siloxane reagent and a hydrophilic chain of amphipathy block polymers easily form hydrogen bonds, and therefore the effect of slow-release is strengthened.

Description

technical field [0001] The invention belongs to the technical field of chemical medicines, and relates to capecitabine-loaded macromolecule targeted slow-release nano-microspheres and a preparation method thereof. Background technique [0002] Malignant tumors are currently one of the most serious diseases that endanger human life. Malignant tumors require comprehensive treatment because of their intractability, and chemotherapy is one of the indispensable means. Capecitabine, whose trade name is Xeloda, is an antineoplastic drug with good efficacy and strong safety in the treatment of metastatic tumors. In September 1998, it was approved by the US FDA for the clinical treatment of advanced primary or metastatic breast cancer that was ineffective for paclitaxel and doxorubicin. In 2001, it was approved by the FDA for the treatment of metastatic colorectal cancer. Although in the clinical trials of Xeloda, no side effects caused by drug overdose were found. However, the tra...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K47/34A61K47/04A61K45/00A61K31/337A61K31/704A61K9/16A61P35/00
Inventor 魏坤彭小敏
Owner SOUTH CHINA UNIV OF TECH