Composite micelle carrying anti-tumor medicine and preparation method thereof

An anti-tumor drug and composite micelle technology, which is applied in the field of composite micelles carrying anti-tumor drugs and their preparation, can solve the problems of poor micelle stability, easy drug leakage, low encapsulation rate and the like, and achieves the encapsulation rate High, increased intracellular accumulation, good stability

Inactive Publication Date: 2010-06-16
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the small proportion of the hydrophobic segment of pluronic, the encapsulation efficiency of many drugs, especially insoluble drugs, is low, and the

Method used

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  • Composite micelle carrying anti-tumor medicine and preparation method thereof
  • Composite micelle carrying anti-tumor medicine and preparation method thereof
  • Composite micelle carrying anti-tumor medicine and preparation method thereof

Examples

Experimental program
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Effect test

Example Embodiment

[0046] Example 1

[0047] Take 1mg of P105 (molecular weight 6500Da) and 10mg of PEG-PLGA with molecular weight of 6500Da (where the molar ratio of PEG to PLGA is 1), dissolve them in 2ml of chloroform, add 1mg of alkalized doxorubicin hydrochloride, and vortex. After all the materials are dissolved, add 10ml of water at a rate of five seconds per drop under ultrasonic conditions. Place the solution on a magnetic stirrer, stir for 2h at 700r / min, stir for 24h at 100r / min, and vacuum for 120min to remove trichloride Methane, the medicinal solution is concentrated to about 5ml to prepare a transparent composite micelle solution, in which the concentration of doxorubicin is 200μg / mL and the encapsulation rate is 52.3%.

Example Embodiment

[0048] Example 2

[0049] Take 10mg of P105 (molecular weight 6500Da) and 10mg of PEG-PCL (molecular weight of 5000Da) (where the molar ratio of PEG to PCL is 7.08), dissolve them in 2ml of chloroform, add 2mg of alkalized adriamycin hydrochloride, and vortex. After all the materials are dissolved, under ultrasonic conditions, add the solution to 20ml of water at a rate of five seconds per drop, place the solution on a magnetic stirrer, stir at 1000r / min for 60min, stir slowly at 300r / min for 8h, and vacuum for 120min to remove three Using methyl chloride, a transparent composite micelle solution was prepared, in which the concentration of doxorubicin was 100 μg / mL and the encapsulation rate was 56.5%.

Example Embodiment

[0050] Example 3

[0051] Take 50mg of P105 (molecular weight 6500Da) and 10mg of PEG-PCL with molecular weight of 16000Da (the molar ratio of PEG to PCL is 3.19), dissolve them in 4ml of chloroform, add 5mg of alkalized doxorubicin hydrochloride, and vortex. After all the materials are dissolved, under ultrasonic conditions, add the solution to 30ml of water at a rate of five seconds per drop, place the solution on a magnetic stirrer, stir at 1500r / min for 30min, stir slowly at 300r / min for 12h, and vacuum for 60min to remove three Methyl chloride was used to prepare a transparent composite micelle solution, in which the concentration of doxorubicin was 250 μg / mL and the encapsulation efficiency was 55.5%.

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Abstract

The invention discloses composite micelle carrying an anti-tumor medicine and a preparation method thereof. The composite micelle is prepared from the following raw materials: pluronic, an amphiphilic block copolymer, an anti-tumor medicine, an organic solvent and water, wherein the mass ratio of the pluronic to the amphiphilic block copolymer is 1-1000:10; the mass ratio of the total mass of the pluronic and the amphiphilic block copolymer to the anti-tumor medicine is 2-100:1. The invention combines the advantages of the pluronic and the amphiphilic block copolymer, and the prepared composite micelle has uniform particle diameter and can overcome a multidrug resistance action. Fluorescent HPLC proves that the composite micelle can obviously increase the intracellular accumulation of the medicine and can be applied to the field of the reversion of the multidrug resistance of tumors. The invention has simple preparation method and very good application prospect.

Description

technical field [0001] The invention relates to the preparation and application of a micellar drug delivery system, in particular to a composite micelle carrying an antitumor drug and a preparation method thereof. Background technique [0002] Chemotherapy plays a very important role in the clinical treatment of tumors. However, multidrug resistance (MDR) produced by tumor cells to chemotherapy drugs is an important reason for the failure of clinical treatment. MDR is an important cellular defense mechanism for tumor cells to avoid drug attacks. It is a phenomenon that tumor cells are resistant to one chemotherapeutic drug and also have cross-resistance to other drugs (with different chemical structures and mechanisms of action). The mechanism is very important. complex. In recent years, drug delivery system (DDS), as a new MDR reversal strategy, has shown good results and attracted the attention of pharmaceutical researchers. [0003] As a material for preparing micelles,...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/32A61K9/00A61K45/00A61K31/704A61K31/337A61K31/4745A61P35/00
Inventor 高建青韩旻刁媛媛
Owner ZHEJIANG UNIV
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