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Drug carrier of slow-release chemotherapy target preparation in tumor operation and preparation method thereof

A tumor-targeting molecule and tumor-based technology, which is applied in the field of drug carriers and preparations of slow-release chemotherapy targeting preparations, can solve the problems of drug release, achieve balanced release speed, improve tumor microenvironment, and prevent tumor metastases Effect

Inactive Publication Date: 2019-09-13
WUHU SIMCERE ZHONGREN PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although the above-mentioned patents solve the problem of sustained release of drugs, they cannot not only release drugs locally in the primary tumor, but also prevent the formation of tumor metastases.

Method used

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  • Drug carrier of slow-release chemotherapy target preparation in tumor operation and preparation method thereof
  • Drug carrier of slow-release chemotherapy target preparation in tumor operation and preparation method thereof
  • Drug carrier of slow-release chemotherapy target preparation in tumor operation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: The following method is used to prepare the drug carrier of the chemotherapeutic targeting preparation:

[0035] (1) Preparation of the anti-tumor active ingredient solution: dissolve the cisplatin powder injection in a citric acid buffer solution with a pH of 3.5 at a ratio of 15%;

[0036] (2) the preparation of liposome microcapsule, the method is as follows:

[0037] (a) prepare a lipid composition solution comprising phosphatidylcholine, phosphatidylinositol, phosphatidylserine, phosphatidylglycerol, and phosphatidic acid in absolute ethanol; each component of the lipid composition in this embodiment can be Combine in any proportion.

[0038] (b) Mix the lipid solution with the antitumor active ingredient solution prepared in step (1) to obtain a mixed solution A; place the mixed solution A on a rotary evaporator, and evaporate to dryness under reduced pressure at a temperature of 20°C , to obtain a lipid film; place the lipid film in an aqueous sol...

Embodiment 2

[0044] Embodiment 2: The following method is used to prepare the drug carrier of the chemotherapeutic targeting preparation:

[0045] (1) Preparation of the anti-tumor active ingredient solution: dissolving cephalomannine in a citric acid buffer solution with a pH of 4.5 at a ratio of 1%;

[0046] (2) the preparation of liposome microcapsule, the method is as follows:

[0047] (a) Preparation of dilauroylphosphatidylcholine, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine, distearoylphosphatidylcholine, distearoylphosphatidylcholine in absolute ethanol Glycerol lipid composition solution; the components of the lipid composition in this example can be combined in any proportion.

[0048] (b) Mix the lipid solution with the antitumor active ingredient solution prepared in step (1) to obtain a mixed solution A; place the mixed solution A on a rotary evaporator, and evaporate to dryness under reduced pressure at a temperature of 60°C , to obtain a lipid film; plac...

Embodiment 3

[0054] Embodiment 3: The following method is used to prepare the drug carrier of the chemotherapeutic targeting preparation:

[0055] (1) Preparation of the anti-tumor active ingredient solution: dissolving or diluting paclitaxel in phosphate buffer saline (0.01M, PBS) with pH 7.0 at a ratio of 5%;

[0056] (2) the preparation of liposome microcapsule, the method is as follows:

[0057] (a) prepare the lipid composition solution comprising dipalmitoylphosphatidylglycerol, dipalmitoylphosphatidic acid, dioleoylphosphatidylcholine, dioleoylphosphatidylethanolamine, natural cephalin in absolute ethanol; this implementation The components of the lipid composition in the examples can be combined in any proportion.

[0058] (b) Mix the lipid solution with the antitumor active ingredient solution prepared in step (1) to obtain a mixed solution A; place the mixed solution A on a rotary evaporator, and evaporate to dryness under reduced pressure at a temperature of 40°C , to obtain a...

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Abstract

The invention discloses a drug carrier of a slow-release chemotherapy target preparation in a tumor operation and a preparation method thereof. The interior of the drug carrier outer membrane comprises a chemotherapeutic drug and a targeting liposome, the outer membrane is composed of a reticular high molecular polymer, tumor targeting molecules are coupled to the liposome, and the inner part of the liposome also comprises anti-tumor chemotherapeutic drug components. The drug carrier provided by the invention can effectively and slowly release the chemotherapeutic drug, controls the release ofthe drug active ingredients for a long time, reduces the toxic and side effects of the chemotherapeutic drug, strengthens the anti-tumor effect of the chemotherapeutic drug, can be specifically combined on the surface of tumor cells, can inhibit the metastasis of the tumor cells at the same time, and can be effectively applied to focus administration for treating cancer.

Description

technical field [0001] The invention relates to the field of drug slow-release preparations, in particular to a drug carrier for slow-release chemotherapy targeting preparations during tumor surgery and a preparation method thereof. Background technique [0002] In the existing chemotherapy methods for tumors, patients are generally treated by oral or intravenous injection. The disadvantage of this administration method is that the concentration of the drug at the lesion site is low. In order to achieve a certain therapeutic effect, it is necessary to increase its therapeutic dose, which will kill or inhibit tumor cells and also have an effect on normal cells throughout the body. Due to the lack of fundamental metabolic differences between tumor cells and normal cells, the therapeutic dose of drugs Often close to the poisoning dose, therefore, the existing chemotherapeutic drugs have all produced great toxic and side effects, such as gastrointestinal reactions, liver and kid...

Claims

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Application Information

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IPC IPC(8): A61K47/68A61K47/34A61K9/127A61K31/555A61K33/243A61K31/337A61K31/282A61P35/00A61P35/04
CPCA61K47/6801A61K47/34A61K9/1273A61K9/1277A61K31/555A61K33/243A61K31/337A61K31/282A61P35/00A61P35/04
Inventor 胡朝奇徐刚
Owner WUHU SIMCERE ZHONGREN PHARM
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