Preparation method of tumor targeting nano-preparation

A nano-preparation and tumor-targeting technology, which is applied in the direction of anti-tumor drugs, pharmaceutical formulations, medical preparations with non-active ingredients, etc., can solve the problems of inability to prepare nanoparticles, achieve short preparation cycle, mild preparation process, and blood circulation time short effect

Inactive Publication Date: 2012-07-25
SOUTHEAST UNIV
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  • Abstract
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Problems solved by technology

Unfortunately, conventional preparation techniques cannot prepare nanoparticles with a core-shell structure

Method used

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Effect test

preparation example Construction

[0019] The preparation is composed of nanoparticles with a core-shell structure, and coaxial electrospray technology is used to encapsulate small molecule chemotherapy drugs in the core of the nanoparticles. The preparation method includes the following steps:

[0020] 1.) Preparation of core solution and shell solution: the solvents of core solution and shell solution are mixed by acetic acid, 2, 2, 2-trifluoroethanol and water in a volume ratio of 4:4:3, in which Contains small molecule chemotherapy drugs and chitosan, the concentration of small molecule chemotherapy drugs is 0.01%~5.0% (w / v), the concentration of chitosan is 0.5%~2.0% (w / v); the shell solution contains 0.5 ~2.0% (w / v) functionalized chitosan; after the core solution and the shell solution are prepared, they are magnetically stirred for 2~4 hours to make a homogeneous solution;

[0021] 2.) Preparation of core-shell nanoparticles: The core solution and the shell solution are respectively driven by a pressure...

Embodiment 1

[0027] The solvents of the core solution and the shell solution were mixed by acetic acid, 2, 2, 2-trifluoroethanol and water in a volume ratio of 4:4:3, and the concentrations of gemcitabine and chitosan in the core solution were 0.03 % and 1.0%; the shell solution contained 1.0% FA-PEG-Chi. Stir magnetically for 2-4 hours respectively to make a homogeneous solution.

[0028]The electric field strength is 10KV, the propulsion speed ratio of the core solution and the shell solution is 1:2.5, and the collection distance is 15cm. The core solution and the shell solution are sprayed coaxially to prepare the core-shell structure nanoparticles, which are removed by vacuum drying at 80°C for 4 hours. remaining solvent. The average diameter of the obtained nanoparticles is 230±45nm, and the average thickness of the shell layer is 60±17nm.

Embodiment 2

[0030] The solvents of the core solution and the shell solution were mixed by acetic acid, 2, 2, 2-trifluoroethanol and water at a volume ratio of 4:4:3, and the concentrations of gemcitabine and chitosan in the core solution were 5.0 % and 2.0%; the shell solution contained 2.0% FA-PEG-Chi. Separately magnetically stir for 3 hours to make a homogeneous solution.

[0031] The electric field strength is 12KV, the propulsion speed ratio of the core solution and the shell solution is 1:2, and the collection distance is 15cm. The core solution and the shell solution are sprayed coaxially to prepare the core-shell structure nanoparticles, which are removed by vacuum drying at 80°C for 4 hours. remaining solvent. The average diameter of the obtained nanoparticles is 350±30nm, and the average thickness of the shell layer is 100±25nm.

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Abstract

The invention provides a novel preparation method of a tumor targeting nano-preparation of nanoparticles based on a a core-shell structure, wherein folic acid and polyethylene glycol double-modified chitosan is used as the shell material, and a small-molecular chemotherapeutics drug is entrapped in the core by a coaxial electrospray technique. Compared with a traditional preparation method, the method provided by the invention is short in preparation period, simple, mild in preparation process, and overcomes disadvantage of conventional preparation technique that is unable to prepare nanoparticles with the core-shell structure. The nanoparticles with the core-shell structure overcomes the disadvantages that the small-molecular chemotherapeutics are adsorbed on the surfaces of the nanoparticles mainly relying on the physical interaction with chitosan, causing low drug-loading rate and entrapment efficiency, the drug is apt to burst release, the blood circulation time is short, and the drug intake is insufficient for tumor tissues; and the nanoparticles with the core-shell structure can be mediated by commonly overexpressed folate receptors of malignant tumors and are suitable for targeted therapy of various tumors.

Description

technical field [0001] The invention provides a method for preparing a tumor-targeting preparation based on core-shell nanoparticles loaded with high-efficiency small-molecule chemotherapeutic drugs. It belongs to the technical field of pharmaceutical preparations. Background technique [0002] The construction of drug preparations targeting tumor tissue is the key to targeted therapy of tumors. Tumor targeting agents are divided into two categories: passive targeting and active targeting. The former is mainly achieved by means of nanoscale drug delivery carriers, while the latter is mediated by specific receptors on the surface of tumor cell membranes. [0003] Nano-preparation achieves passive targeted drug delivery, which is closely related to the special morphology of tumor tissue. Compared with normal tissue, tumor tissue has fewer pericytes, increased vascular permeability, and larger vascular endothelial gap, usually 100-780nm. The size of the nano-preparation just...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K45/00A61K47/36A61K47/22A61K47/34A61P35/00
Inventor 许茜周家华
Owner SOUTHEAST UNIV
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