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Composition as well as nano-micelle containing composition and application thereof

A nano-micelle and composition technology, applied in the field of drug research and development, can solve the problems of drug resistance, high toxicity, and low bioavailability

Inactive Publication Date: 2018-04-17
GUANGDONG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In view of this, the present invention provides a composition, nano micelles and applications containing the composition, which are used to solve the problems of low bioavailability, high toxicity and easy Technical flaws where drug resistance emerges

Method used

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  • Composition as well as nano-micelle containing composition and application thereof
  • Composition as well as nano-micelle containing composition and application thereof
  • Composition as well as nano-micelle containing composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] After mixing 10 g of docetaxel, 5 g of traditional Chinese medicine monomer 1 and 200 g of carrier 1, they were dissolved in 50 ml of organic solvent 1 to obtain the first product 1. The organic solvent 1 of 1 in the first product was removed by rotary evaporation to obtain the second product 1, which formed a thin film on the wall of the container used for the reaction. Add 10 ml of deionized water to the second product 1, and magnetically stir at room temperature for 10 h for hydration treatment to obtain nanomicelle product 1. In the preparation of product 1, the traditional Chinese medicine monomer 1 is curcumin (CUR), and the carrier 1 is composed of 196g soloplus and 4g TPGS1000; the particle size of the obtained product 1 is 62.04±0.16nm.

[0039] After mixing 5g of docetaxel, 6g of traditional Chinese medicine monomer 2 and 150.2g of carrier 2 evenly, they were dissolved in 40ml of organic solvent 2 to obtain the first product 2. The organic solvent 2 of 2 in t...

Embodiment 2

[0045] This example is a specific example of measuring the physical properties of products 1 to 5 prepared in example 1. 2.1 Shape observation

[0046] Zeta potentials of products 1 to 5 were measured with a nanometer particle size analyzer, and the shapes of the prepared products 1 to 5 were observed with a transmission electron microscope.

[0047] 2.2 Content of docetaxel in micelles

[0048] The content of docetaxel in micelles was determined by high performance liquid chromatography. A chromatographic column (Phenomenex; 4.6 × 250 mm, 5 μm) with octadecylsilane bonded silica gel as the filler, acetonitrile-water (47:53, v / v) as the mobile phase, the temperature is 30 ° C, and the detection wavelength is 227 nm. The flow rate was determined at 1 mL / min. Precisely measure the prepared products 1 to 5, and destroy them with 9 times the volume of methanol. Take out 20μL sample and use HPLC method to determine the content of docetaxel in the micelles.

[0049] 2.3 Encapsu...

Embodiment 3

[0067] This embodiment is the determination of the cytotoxicity test of products 1 to 5.

[0068] Human-derived breast cancer MCF-7 cells in the logarithmic growth phase and drug-resistant human-derived breast cancer MCF-7 / Adr cells were digested with 0.25% trypsin, washed twice with medium, and washed 2 times with 5×10 3 The amount of cells / well (180 μL cell suspension) was inoculated on a 96-well cell culture plate, with 6 replicate wells, at 37°C, 5% CO 2 incubator for 24 hours.

[0069] Dosing in the following manner, wherein the concentration in brackets in the following content refers to the final concentration after adding to the 96-well plate and being diluted.

[0070] (a), get the same amount of culture medium without adding medicine, add it in the 96-well culture plate, as blank control;

[0071] (b), adding a series of concentrations of blank nanomicelles (Blank-TPGS-PMs) (0, 0.01, 0.1, 1, 5, 10, 20 mg / mL);

[0072] (c), adding a series of concentrations of free...

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Abstract

The invention belongs to the field of research and development of drugs and in particular relates to a composition as well as nano-micelle containing the composition and application thereof. The invention provides a composition, and the composition contains the following raw materials: docetaxel, traditional Chinese medicine monomers and a carrier, wherein the traditional Chinese medicine monomerscontains one or more of quercetin, curcumin, rheum emodin, cnidium lactone, apigenin, baicalein, kaempferol and silymarin. The invention further provides a preparation method of the nano-micelle containing the composition. The invention further provides application of the composition or the product prepared by the preparation method in inhibition of tumor cell proliferation and / or survival. According to experimental determination, the product prepared by the technical scheme provided by the invention has obvious antineoplastic activity after oral medication, is high in bioavailability and capable of obviously reducing the dosage and can overcome drug resistance produced during single use of the docetaxel.

Description

technical field [0001] The invention belongs to the field of drug research and development, and in particular relates to a composition, nano micelles containing the composition and applications. Background technique [0002] Docetaxel (DTX) is a taxane anticancer drug semi-synthesized from the precursor extracted from the needles of yew berry. It has good curative effect on various cancers such as ovarian cancer, breast cancer, non-small cell lung cancer and prostate cancer. [0003] Docetaxel has poor solubility and low oral bioavailability. The commercially available docetaxel injection (Taxotere) uses non-ionic surfactant Tween-80 and ethanol to increase its solubility, however, this solvent system can cause serious adverse reactions such as neurotoxicity, musculoskeletal toxicity, and neutropenia, while The distribution of the drug is non-selective and has relatively large toxic and side effects. [0004] Second, the poor oral bioavailability of docetaxel is a bottlen...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/337A61K47/14A61K47/34A61P35/00A61K31/352A61K31/357A61K31/37A61K31/12A61K31/122
CPCA61K9/1075A61K31/12A61K31/122A61K31/337A61K31/352A61K31/357A61K31/37A61K47/14A61K47/34A61K2300/00
Inventor 典灵辉于恩江典成阳马伟伟赵文昌
Owner GUANGDONG MEDICAL UNIV
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