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Drug-loaded liposome overcoming tumor drug resistance, preparation method and application thereof

A technology of liposomes and long-circulation liposomes, which is applied in the fields of antineoplastic drugs, liposome delivery, and pharmaceutical formulations. Inhibiting the effect of chemotherapy drug-resistant tumors

Active Publication Date: 2013-06-12
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0030] The purpose of the present invention is to overcome the defects that various forms of chemotherapeutic drugs in the prior art have poor curative effect on drug-resistant tumors, and provide a drug-loaded liposome with better curative effect on drug-resistant tumors and its preparation method and application

Method used

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  • Drug-loaded liposome overcoming tumor drug resistance, preparation method and application thereof
  • Drug-loaded liposome overcoming tumor drug resistance, preparation method and application thereof
  • Drug-loaded liposome overcoming tumor drug resistance, preparation method and application thereof

Examples

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preparation example Construction

[0045] The invention provides a method for preparing drug-loaded liposomes, which is characterized in that the method comprises, using thin film-ultrasonic method, liposome source, distearoylphosphatidylethanolamine-methoxypolyethylene glycol 2000 The drug-loaded liposome is prepared with a drug active component, and the drug active component is paclitaxel and resveratrol.

[0046] Wherein, the molar ratio of the liposome source, distearoylphosphatidylethanolamine-methoxy polyethylene glycol 2000 and the active ingredient of the drug can be the ratio of the conventional liposome carrier to the active ingredient of the drug, Preferably, the molar ratio of the liposome source, distearoylphosphatidylethanolamine-methoxy polyethylene glycol 2000 and the active pharmaceutical component is 1:0.01-1:0.001-0.5, more preferably 1: 0.02-0.2:0.01-0.3, most preferably 1:0.05-0.1:0.02-0.1.

[0047] According to the method of the present invention, in the pharmaceutically active component,...

Embodiment 1

[0067] This example is used to prepare drug-loaded liposome: PTX+Res liposome-1.

[0068] (1) will 4×10 -2 mol soybean lecithin, 2×10 -3 mol distearoylphosphatidylethanolamine-methoxy polyethylene glycol 2000 mixed with 150ml of absolute ethanol, after dissolving, add 3×10 -4 mol paclitaxel and 1.2×10 -3 mol resveratrol to obtain the first mixed solution,

[0069] (2) evaporation removes the absolute ethanol in the first mixed solution to form a thin film,

[0070] (3) The film was mixed with 5ml of physiological saline, and the drug-loaded liposome was obtained by ultrasonication, that is, PTX+Res liposome-1.

[0071] The conditions of the ultrasound include: the frequency is 350W, the ultrasound is 18s, the interval is 8s, and the ultrasound is 15 times.

Embodiment 2

[0073] This example is used to prepare drug-loaded liposome: PTX+Res liposome-2.

[0074] (1) will 4×10 -2 mol soybean lecithin, 2×10 -3 mol distearoylphosphatidylethanolamine-methoxy polyethylene glycol 2000 mixed with 200ml of absolute ethanol, after dissolving, add 3×10 -4 mol paclitaxel and 3.6×10 -3 mol resveratrol to obtain the first mixed solution,

[0075] (2) evaporation removes the absolute ethanol in the first mixed solution to form a thin film,

[0076] (3) The film was mixed with 4ml of physiological saline, and the drug-loaded liposome was obtained by ultrasonication, that is, PTX+Res liposome-2.

[0077] The conditions of the ultrasound include: the frequency is 400W, the ultrasound is 15s, the interval is 5s, and the ultrasound is 10 times.

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Abstract

The invention provides a drug-loaded liposome which comprises long-circulating liposome and pharmaceutically active ingredients wrapped in the long-circulating liposome, wherein the pharmaceutically active ingredients comprise paclitaxel and resveratrol. The invention further provides a preparation method of the drug-loaded liposome. The method comprises, by using a thin film-ultrasonic method, preparing liposome sources, distearoyl phosphatidyl ethanolamine-methoxy polyethylene glycol 2000 and the pharmaceutically active ingredients into the drug-loaded liposome, wherein the pharmaceutically active ingredients comprise the paclitaxel and the resveratrol. The invention further provides the drug-loaded liposome prepared by the invention. In addition, the invention provides an application of the liposome in preparing antitumor drug and in treating the tumor. The drug-loaded liposome contains the paclitaxel and the resveratrol, has activity of inhibiting development of drug-sensitive tumor, furthermore effectively inhibits development of chemotherapeutic-drug-resistance tumor, and has great clinical value.

Description

technical field [0001] The invention relates to a drug-loaded liposome for overcoming tumor drug resistance, a preparation method of the drug-loaded liposome, and an application of the drug-loaded liposome in preparing antitumor drugs and treating tumors. Background technique [0002] 1. Tumor drug resistance [0003] At present, in the treatment of many tumors, the poor effect of conventional chemotherapy and poor prognosis are important clinical problems, and tumor multidrug resistance (MDR) is the key factor for the failure of tumor chemotherapy. After treatment, the remaining tumor stem cells develop drug resistance, which often leads to decreased sensitivity to certain drugs, and causes tumor recurrence or even metastasis. The drug resistance of human malignant tumors to chemotherapy can be divided into congenital drug resistance (nature resistance) and acquired drug resistance (acquired resistance); Drug resistance (multidrug resistance, MDR). PDR is only resistant ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/337A61K47/34A61P35/00A61K31/047
CPCA61K9/127A61K31/05A61K31/337A61K9/1271A61K47/34A61P35/00A61K2300/00
Inventor 杨先达孟洁王琛
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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