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Polymeric micelle entrapping difficultly soluble anti-tumor medicine curcumin and preparation method and application of polymeric micelle

An anti-tumor drug and polymer glue technology, which is applied in the field of polymer micelles containing insoluble anti-tumor drug curcumin and its preparation, can solve the problems of low bioavailability, easy degradation, and poor stability of curcumin. Achieve the effects of improving in vivo and in vitro stability, enhancing passive targeting ability, and increasing solubility

Active Publication Date: 2017-05-10
SHAANXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Curcumin is insoluble in water (2.99×10 -8 mol / L), ordinary oral administration is not absorbed, and there is a serious hepatic first-pass effect, that is, after gastrointestinal administration, it is metabolized by the liver before being absorbed into the blood circulation, so that the amount of the drug entering the blood circulation is extremely reduced and the metabolism and clearance rate of curcumin in the body is faster, so under general administration, the bioavailability (<1%) of curcumin is very low, poor stability (unstable under alkaline conditions, prone to degradation), And curcumin as an anti-tumor drug, the most important thing is to achieve the maximum enrichment of the drug in tumor tissue

Method used

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  • Polymeric micelle entrapping difficultly soluble anti-tumor medicine curcumin and preparation method and application of polymeric micelle
  • Polymeric micelle entrapping difficultly soluble anti-tumor medicine curcumin and preparation method and application of polymeric micelle
  • Polymeric micelle entrapping difficultly soluble anti-tumor medicine curcumin and preparation method and application of polymeric micelle

Examples

Experimental program
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Effect test

Embodiment 1

[0048] Weigh 60mg of P123, 240mg of F127, and 10mg of curcumin, so that the mass ratio of pluronic and curcumin is 30:1; add 4mL of tetrahydrofuran, and ultrasonicate in a water bath for 10 minutes to fully dissolve the carrier material and the drug. The solution was placed in a rotary evaporator at 37° C. for 1 h, and dried overnight in vacuum to obtain an orange-yellow film. Swell the film at 37°C for 15 minutes, add 8 mL of 37°C deionized water for hydration, stir for 30 minutes, filter and sterilize with a 0.22 μm microporous membrane to obtain the curcumin Pluronic F127 / P123 mixed micelle preparation.

Embodiment 2

[0050] Weigh 80mg of P123, 220mg of F127, 8mg of curcumin, add 4ml of methanol, and sonicate in a water bath for 10min to fully dissolve the carrier material and the drug. The solution was placed in a rotary evaporator at 37° C. for 1 h, and dried overnight in vacuum to obtain an orange-yellow film. Swell the film at 37°C for 15 minutes, add 6 mL of 37°C deionized water for hydration, stir for 30 minutes, and filter and sterilize with a 0.22 μm microporous membrane to obtain the curcumin Pluronic F127 / P123 mixed micelle preparation.

Embodiment 3

[0052] Weigh 100mg P123, 200mg F127, 6mg curcumin, add 4ml acetone, and ultrasonicate in a water bath for 10min to fully dissolve the carrier material and the drug. The solution was placed in a rotary evaporator at 37° C. for 1 h, and dried overnight in vacuum to obtain an orange-yellow film. Swell the film at 37°C for 15 minutes, add 4 mL of 37°C deionized water for hydration, stir for 30 minutes, filter and sterilize with a 0.22 μm microporous membrane to obtain the curcumin Pluronic F127 / P123 mixed micelle preparation.

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Abstract

The invention relates to a polymeric micelle entrapping difficultly soluble anti-tumor medicine curcumin and a preparation method and application of the polymeric micelle. The polymeric micelle is characterized in that by adopting a thin film dispersion method, Pluronic is used as a carrier, and the curcumin is entrapped into a hydrophobic kernel PPO (polypropylene oxide) of the Pluronic, so as to prepare the polymeric micelle entrapping the difficultly soluble anti-tumor medicine curcumin. The polymeric micelle has the advantages that the Pluronic comprises three blocks of PEO (polyethylene oxide)-PPO-PEO, a monomer can be discharged by kidney, the biocompatibility is good, a PPO chain can form the hydrophobic kernel to entrap the difficultly soluble anti-tumor medicine, the dissolvability is increased, and the in-vitro and in-vivo stability is improved; a PEO chain can form a hydrophilic shell, a space stabilizing function and a permeation and retention effect are realized, the phagocytosis of a reticuloendothelial system is avoided, the body circulation time is prolonged, the passive targeting capability is improved, and the bioavailability and the anti-tumor effect of the curcumin are improved.

Description

[0001] 【Technical field】 [0002] The invention belongs to the field of pharmaceutical preparations, in particular to a curcumin polymer micelle carrying an insoluble antitumor drug, a preparation method and application thereof. [0003] 【Background technique】 [0004] Curcumin (Curcumin) is a natural active ingredient extracted from the root of the genus Curcuma (Curcuma longa L) in the ginger family. , and the toxicity and side effects are small, and it has broad application prospects as a drug. At present, the most important research on curcumin lies in the development of anticancer agents. [0005] The structural formula of curcumin is C 21 h 20 o 6 , molecular weight: 368.37, the structural formula is as follows: [0006] [0007] Curcumin is insoluble in water (2.99×10 -8 mol / L), ordinary oral administration is not absorbed, and there is a serious hepatic first-pass effect, that is, after gastrointestinal administration, it is metabolized by the liver before being...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/12A61K47/10A61P35/00
CPCA61K9/1075A61K31/12A61K47/10
Inventor 王筱冰吴鹏英贾亚丽王攀刘全宏
Owner SHAANXI NORMAL UNIV
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