Docetaxel malignant tumor targeting microsphere as well as preparation method and application thereof
A technology for docetaxel and malignant tumors, which is applied in the field of docetaxel malignant tumor targeting microspheres and its preparation, which can solve the problems of high toxicity and side effects, poor curative effect, and poor therapeutic effect, and achieves a simple preparation method and easy promotion The effect of using
Pending Publication Date: 2022-07-22
PINGDINGSHAN UNIVERSITY
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Problems solved by technology
The global incidence of breast cancer has been on the rise since the end of the 1970s. It progresses rapidly and has poor quality of life. It is one of the malignant tumors with poor treatment effects among all tumors so far. Low rate, insensitive to systemic chemotherapy and radiotherapy, and systemic chemotherapy has disadvantages such as poor targeting, poor curative effect, and large toxic and side effects
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Embodiment 1
[0041] A preparation method of a docetaxel malignant tumor targeting preparation, specifically comprising the following steps:
[0042] (1) Buffer preparation
[0043] Preparation of Tris buffer: First, dissolve 12.11g of Tris base in 950mL~970mL deionized water, add HCl with a concentration of 4mol / L dropwise while stirring, measure the pH value of the solution to the desired pH value with a pH meter, and then add water Make up to 1L to obtain 0.1mol / L Tris-HCl buffer;
[0044] PBS buffer preparation: Weigh 8.0g NaCl, 0.2g KCl, 1.44g Na 2 HPO 4 , 0.24g KH 2 PO 4 Dissolve in 800mL of distilled water, adjust the solution to 7.4 with HCl, and finally add distilled water to 1L to obtain 0.01mol / L PBS buffer;
[0045] (2) Preparation of blank microspheres
[0046] Take 100ml of Tris buffer, add 100mg of polysorbate 20, mix with 80mL of dichloromethane containing PLGA (the volume ratio of PLGA and dichloromethane is 60:40V:V), stir at 500 / min for 2min to make W / O / w Type firs...
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Abstract
The invention discloses docetaxel malignant tumor targeting microspheres and a preparation method and application thereof, and belongs to the technical field of functional materials, and the specific preparation method comprises the following steps: (1) preparing blank microspheres; (2) preparing folic acid modified microspheres; and (3) loading the docetaxel. Meanwhile, the invention further discloses the docetaxel malignant tumor targeting microspheres prepared by the preparation method and application of the docetaxel malignant tumor targeting microspheres in preparation of anti-breast cancer drugs. The average particle size of the blank microspheres prepared by using a multiple emulsion method is 22.38 microns, and the accumulated release amount within 72 hours can reach 80% or above when the blank microspheres are measured in human plasma. In addition, the preparation method provided by the invention is simple and convenient to popularize and use.
Description
technical field [0001] The invention relates to the field of functional polymer materials, in particular to a docetaxel malignant tumor targeting microsphere and a preparation method and application thereof. Background technique [0002] Cancer has seriously endangered human health and has become one of the killers of human beings, ranking first in the common cause of death. The global incidence of breast cancer has been on the rise since the late 1970s. Its rapid progress and poor quality of life make it one of the malignant tumors with poor treatment effect among all tumors so far. It is not sensitive to systemic chemotherapy and radiotherapy, and systemic chemotherapy has disadvantages such as poor targeting, poor efficacy, and large toxic and side effects. [0003] Docetaxel, also known as Taxotere, is a taxane compound antineoplastic drug, suitable for the treatment of locally advanced or metastatic breast cancer, and also for the treatment of locally advanced or metas...
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IPC IPC(8): A61K47/69A61K47/54A61K9/50A61K31/337A61P35/00
CPCA61K31/337A61K47/6927A61K47/545A61P35/00A61K9/5089
Inventor 杜会强张利芳李玖零毛冬雪何佩娜
Owner PINGDINGSHAN UNIVERSITY