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Docetaxel transferrin acceptor-targeted liposome preparation

A technology of docetaxel and transferrin is applied in the field of docetaxel-transferrin receptor targeting liposome preparation, which can solve the problems of occurrence and the like

Inactive Publication Date: 2012-12-26
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, hypersensitivity and some side effects associated with Tween-80-based formulations may occur in clinical use

Method used

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  • Docetaxel transferrin acceptor-targeted liposome preparation
  • Docetaxel transferrin acceptor-targeted liposome preparation
  • Docetaxel transferrin acceptor-targeted liposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Preparation of docetaxel-transferrin receptor-targeted liposome formulation

[0020] The steps are as follows: Weigh 13.56mg of hydrogenated soybean lecithin, 35.34mg of lecithin, 35.45mg of cholesterol, 5.3mg of polyethylene glycol-distearoylphosphatidylethanolamine, mix with docetaxel (5.67mg) and spin steam, add phosphoric acid Salt buffer (pH 7.4, the same below) hydrated multilamellar liposomes, using post-embedding technology to link transferrin ligands to the surface of liposomes loaded with docetaxel, freeze-dried to obtain the product.

[0021] The specific steps for linking the transferrin ligand to the surface of the liposome containing docetaxel by the post-application embedding technology are as follows (the following examples are all the same): the transferrin is thiolated, and the hydroxyethylpiperazine Add Traut's reagent to transferrin (M Tr :M Tf =10:1), the mixture was obtained after sufficient reaction, the mixture containing transferrin...

Embodiment 2

[0022] Example 2: Preparation of docetaxel-transferrin receptor-targeted liposome formulation

[0023] The steps are as follows: Weigh 14.66 mg of hydrogenated soybean lecithin, 46.75 mg of soybean lecithin, 55.34 mg of cholesterol, and 5.4 mg of synthetic phosphatidylserine, mix with docetaxel (5.64 mg) and spin steam, add phosphate buffer to hydrate the multilamellar lipid The body is obtained by linking the transferrin ligand to the surface of the liposome loaded with docetaxel by post-embedding technology, and freeze-drying.

Embodiment 3

[0024] Example 3: Preparation of docetaxel-transferrin receptor-targeted liposome formulation

[0025] The steps are as follows: Weigh 50.44 mg of hydrogenated soybean lecithin, 70.45 mg of lecithin, 70.89 mg of cholesterol, 5.44 mg of synthetic dipalmitoylphosphatidylcholine, mix with docetaxel (10.55 mg) and spin steam, add phosphate buffer to hydrate The multi-lamellar liposome is obtained by linking the transferrin ligand to the surface of the liposome loaded with docetaxel by post-embedding technology, and freeze-drying.

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Abstract

The invention discloses a docetaxel transferrin acceptor-targeted liposome preparation. The preparation is prepared with a preparation method comprising the following steps of: mixing 55-95 parts by weight of phospholipid, 3-40 parts by weight of cholesterol and 0.05-20 parts by weight of docetaxel; dissolving into ethanol; performing rotary evaporation; adding 0.5-1.5ml of a phosphate buffer solution, and hydrating to obtain a liposome; and connecting a transferrin ligand to a liposome surface which contains docetaxel by applying a backward embedding technology to obtain a docetaxel transferrin acceptor-targeted liposome preparation, wherein the average particle diameter of the preparation is 60-100 nanometers, and the interfacial potential is -10mV to 20mV. As proved by a cytotoxicity research result, compared with a non-targeted liposome, a transferrin acceptor-targeted liposome has the advantage that: the toxicity of docetaxel on KB cells can be enhanced remarkably. The docetaxel transferrin acceptor-targeted liposome disclosed by the invention can become a novel medicament preparation for treatment cancers in future.

Description

technical field [0001] The present invention relates to docetaxel transferrin receptor targeting liposome preparation. Background technique [0002] Docetaxel is a very effective clinical chemotherapy drug for the treatment of ovarian, breast, colon, head, neck and non-small cell lung cancer. The current product, Taxotere, contains a Tween-80 / ethanol solvent to enhance the water solubility of docetaxel. However, hypersensitivity and some side effects associated with Tween-80-based formulations may occur in clinical use. Liposomes and docetaxel-loaded nanoparticles using nanotechnology have been increasingly established in reducing the toxicity of Tween-80-based vehicles. [0003] Human transferrin (Tf, molecular weight: 80kDa) is a glycoprotein with non-heme iron and high affinity for transferrin receptors, which is frequently highly expressed on tumor cells and acts through transferrin receptors. The medium is internalized by endocytic cells. Therefore, transferrin is c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/42A61P35/00
Inventor 翟光喜张海群窦金凤
Owner SHANDONG UNIV
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