Compound drug-carrying liposome as well as preparation method and application thereof

A technology of liposomes and long-circulation liposomes, which is applied in liposome delivery, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of poor curative effect, achieve small side effects, high clinical application value, and inhibit chemotherapeutic drug resistance. The effect of drug-induced tumors

Inactive Publication Date: 2014-03-26
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0013] The purpose of the present invention is to overcome the defects that anthracycline antibiotics and anthracycline antibiotics used in combination with other anticancer drugs have poor curative effects on drug-resistant tumors in the prior art, and provide a drug-resistant tumor that has a relatively low curative effect on drug-resistant tumors. Composite drug-loaded liposome with good and less side effects, preparation method and application thereof

Method used

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  • Compound drug-carrying liposome as well as preparation method and application thereof
  • Compound drug-carrying liposome as well as preparation method and application thereof
  • Compound drug-carrying liposome as well as preparation method and application thereof

Examples

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preparation example Construction

[0031] The invention provides a method for preparing a composite drug-loaded liposome, which is characterized in that the method comprises, using a thin film-ultrasonic method, combining liposome source, distearoylphosphatidylethanolamine-methoxypolyethylene glycol 2000 and pharmaceutical active components to prepare the complex drug-loaded liposome, the pharmaceutical active components are anthracycline antibiotics and resveratrol.

[0032] According to the method of the present invention, in the pharmaceutical active component, the molar ratio of anthracycline antibiotics and resveratrol can be adjusted as required, preferably, the molar ratio of the anthracycline antibiotics and resveratrol is 1:0.01-100, more preferably 1:1-80, more preferably 1:3-40, most preferably 1:5-20.

[0033] In the present invention, the anthracycline antibiotics may be various anthracycline antibiotics commonly used in the art. Since anthracycline antibiotics all have the structural skeleton of ...

Embodiment 1

[0054] This example is used to prepare composite drug-loaded liposome: ADR+Res liposome-1.

[0055] (1) Put 4×10 -2 mol soybean lecithin, 10 -2 mol cholesterol, 2×10 -3 mol distearoylphosphatidylethanolamine-methoxy polyethylene glycol 2000 is mixed with 150ml of absolute ethanol, and after dissolving, add 1.2×10 -3 mol resveratrol to obtain the first mixed solution,

[0056] (2) Evaporate and remove the absolute ethanol in the first mixed solution to form a thin film,

[0057] (3) Put 3×10 -4 mol of anthracycline antibiotics was mixed with 5ml of normal saline, added to the film and sonicated to obtain composite drug-loaded liposomes, ie ADR+Res liposome-1.

[0058] 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

[0060] This example is used to prepare composite drug-loaded liposome: ADR+Res liposome-2.

[0061] (1) Put 4×10 -2 mol soybean lecithin, 10 -2 mol cholesterol, 2×10 -3 mol distearoylphosphatidylethanolamine-methoxy polyethylene glycol 2000 is mixed with 200ml of absolute ethanol, and after dissolving, add 3.6×10 -3 mol resveratrol to obtain the first mixed solution,

[0062] (2) Evaporate and remove the absolute ethanol in the first mixed solution to form a thin film,

[0063] (3) Put 3×10 -4 mol of anthracycline antibiotics was mixed with 4ml of normal saline, added to the film and sonicated to obtain composite drug-loaded liposomes, ie ADR+Res liposome-2.

[0064] 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 discloses a compound drug-carrying liposome as well as a preparation method and application thereof. The compound drug-carrying liposome comprises a long-circulating liposome and medicinal active ingredients coated by the long-circulating liposome, wherein the long-circulating liposome is a liposome of which the surface is modified by distearoyl phosphoethanolamine-methoxy polyethylene glycol 2000; the medicinal active ingredients refer to anthracycline antibiotics and resveratrol. The preparation method of the compound drug-carrying liposome comprises preparing a liposome source, the distearoyl phosphoethanolamine-methoxy polyethylene glycol 2000 and the medicinal active ingredients into the compound drug-carrying liposome, wherein the medicinal active ingredients refer to anthracycline antibiotics and resveratrol. The compound drug-carrying liposome disclosed by the invention has inhibitory activity on the development of drug-sensitive tumors, can effectively inhibit the development of chemotherapeutic drug-tolerant tumors and is small in side effect, thereby achieving a great clinical application value.

Description

technical field [0001] The invention relates to a composite drug-loaded liposome and its preparation method and application, more precisely to a composite drug-loaded liposome for overcoming tumor drug resistance, its preparation method and application. 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 a key factor for the failure of tumor chemotherapy. After treatment. The formation of drug resistance of residual tumor stem cells often leads to decreased sensitivity to certain drugs, and causes tumor recurrence and even metastasis. The drug resistance of human malignant tumors to chemotherapy can be divided into natural drug resistance (nature resistance) and acquired drug resistance (acquired resistance); according to the drug resistance spectrum, it can be divided into primary ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K45/00A61K31/704A61K31/05A61K47/34A61P35/00
Inventor 孟洁杨先达王琛
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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