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Vincristine-reversal agent composite nano-granule and preparation method and use thereof

A kind of technology of vincristine and vincristine sulfate, applied in the field of medicine

Inactive Publication Date: 2009-02-11
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There is no compound nanoparticle in which vincristine and reversal agent are co-encapsulated in the same nanoparticle, and it has been applied to anti-drug-resistant tumor activity.

Method used

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  • Vincristine-reversal agent composite nano-granule and preparation method and use thereof
  • Vincristine-reversal agent composite nano-granule and preparation method and use thereof
  • Vincristine-reversal agent composite nano-granule and preparation method and use thereof

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Embodiment Construction

[0016] The compound nanoparticle of vincristine reversal agent of the present invention is prepared by compounding vincristine and reversal agent in PLGA.

[0017] Among them, vincristine uses its sulfate salt—vincristine sulfate (VCR), and the reversal agent uses verapamil (VRP) or quercetin (quercetin, QC).

[0018] The ratio of PLGA, vincristine and reversal agent is as follows:

[0019] PLGA: 20-80 mg, vincristine: 50-1000 μg, reversal agent: 1 mg-20 mg; among them, PLGA is dissolved in an organic solvent so that its concentration is 20-80 mg / ml.

[0020] The preparation of vincristine-reversal agent composite nanoparticles of the present invention can adopt emulsification solvent volatilization method, spray drying method, self-emulsification / solvent dispersion method, precipitation method, interface deposition method, solvent-non-solvent method, etc. The commonly used surfactant is Polyvinyl alcohol (PVA).

[0021] Such as:

[0022] 1. The emulsified solvent evaporati...

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Abstract

The invention relates to a vincristine-reversion agent compound nano particle, a preparation thereof and applications, belonging to the medicine field. A first technical problem to be solved by the invention is: overcoming the phenomena of multidrug resistance MDR of various tumor cells to the vincristine, namely, the vincristine and the reversion agent are wrapped and carried in a PLGA in a compound way, for preparing the nano particles. With the purposes of obtaining the smaller-diameter nano particles and reducing the vestigital of the surface active agent, F68 and TPGS are adopted as the surface active agent; compared with PVA, the TPGS and the F68 can obviously increase the mortality of drug-resistant breast cancer cells (p is smaller than 0.05); and the tumor-inhibition rate of the TPGS is obviously higher than that of the F68.

Description

technical field [0001] The invention relates to vincristine reversal agent composite nanoparticles, a preparation method and application thereof, and belongs to the field of medicine. Background technique [0002] Tumor multidrug resistance (MDR) refers to that after a drug acts on a tumor to make it resistant, the tumor also has cross-resistance to a variety of anti-tumor drugs that have not been exposed to, have nothing to do with structure, and have different mechanisms. drug resistance. It involves a variety of antitumor drugs commonly used in clinical practice, and is one of the most serious obstacles to the successful chemotherapy of tumors. Over the past two decades, research has been dedicated to overcoming multidrug resistance by restoring the sensitivity of drug-resistant tumors to chemotherapy drugs. Although some reversal effects have been achieved in vitro experiments, the results in vivo, especially clinical trials, are not very good. ideal. The main reasons...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/475A61K31/275A61K31/352A61P35/00
Inventor 宋相容魏于全侯世祥
Owner SICHUAN UNIV
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