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Nanocomposite carrier for double loading of peptides and chemotherapeutic drugs and its preparation and application

A chemotherapeutic drug and nano-composite technology, which is applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of difficulty in effectively penetrating cell membranes, instability, and large toxic and side effects of chemotherapy drugs, etc. problems, to achieve the effect of reducing dosage and side effects, enhancing penetration and good dispersibility

Active Publication Date: 2020-11-10
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to solve the problems of instability, inactivation, and difficulty in effectively penetrating cell membranes of peptide drugs in storage, transportation, and circulation in the body, as well as the problems that chemotherapy drugs have large toxic and side effects and are difficult to accumulate in drug-resistant cancer cells. Features, aiming to provide nano-composite carriers with dual loads of peptides and chemotherapeutic drugs and its preparation method and application, in order to release drugs at designated sites on cancer cells, and exert peptide drugs and chemotherapeutic drugs on cancer, especially drug-resistant cancers. The synergistic and efficient diagnosis and treatment effect; thus it is expected to promote the clinical application of Bcl-2 function conversion peptide in cancer treatment

Method used

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  • Nanocomposite carrier for double loading of peptides and chemotherapeutic drugs and its preparation and application
  • Nanocomposite carrier for double loading of peptides and chemotherapeutic drugs and its preparation and application
  • Nanocomposite carrier for double loading of peptides and chemotherapeutic drugs and its preparation and application

Examples

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Effect test

Embodiment 1

[0060] Example 1: Preparation of mesoporous silica-dendrimer nanocomposite carrier loaded with Bcl-2 function conversion peptide (NuBCP9) and chemotherapeutic drug DOX simultaneously

[0061] (1) Take 2g of cetyltrimethylammonium chloride and 0.18g of triethanolamine in a reaction vessel, add 80ml of deionized water at 95°C to dissolve and stir for 1h;

[0062] (2) Slowly add 1.5ml tetraethyl orthosilicate dropwise to the reaction system, continue to stir for 2h and then centrifuge, wash with a large amount of ethanol and water respectively, to obtain mesoporous silica nanoparticles containing surfactant;

[0063] (3) The mesoporous silica nanoparticles containing surfactant obtained in step (2) are placed in methanol solution containing 1% sodium chloride, ultrasonically dispersed and washed on a rotary mixer for 12 hours at room temperature, and repeated for 4 times, vacuum drying after washing with water to obtain mesoporous silica nanoparticles whose surface groups are hyd...

Embodiment 2

[0075] Example 2: Analysis of the cell-entry ability of mesoporous silica-dendrimer composite nanocarriers double-loaded with NuBCP9 anti-cancer small peptide and chemotherapy drug DOX

[0076] After co-incubating 1 μg / ml DOX and its corresponding concentration NuBCP-9-FITC and NuBCP-9-FITC@MSNs~G5~DOX with Bcl-2 stably transfected cells HeLa-Bcl2 for 10 h, the mitochondrial far-red probe was used to locate the mitochondria, Nuclei were localized with 1 μg / ml DAPI dye for confocal imaging analysis.

[0077] See the confocal image of the drug-loaded drug-loaded nano-drug complex prepared in Example 2 for hela-Bcl2 tumor cells to penetrate into the cell and distribute in the cell. Figure 7 . Free NuBCP-9 small peptides cannot enter the interior of Hela cells, and free DOX drugs can freely penetrate cancer cells and enter the nucleus; however, under the transport of composite nanocarriers, both NuBCP9 small peptides and DOX can enter the interior of cells and reach their respec...

Embodiment 3

[0078] Example 3: Analysis of the ability of mesoporous silica-dendrimer composite nanocarriers double-loaded with NuBCP9 anticancer small peptide and chemotherapeutic drug DOX to inhibit the proliferation of cancer cells

[0079] Prepare DOX concentrations of 0.1, 0.5, 1, 2, 5, 10 μg / ml or corresponding NuBCP-9 concentrations containing NuBCP-9, DOX, N9+DOX, N9@M~G5, N9@M~G5~DOX After co-cultivating with HeLa-Bcl2 cells for 48 hours, the cell viability was detected by MTT, and the cytotoxicity of different groups of drugs was obtained.

[0080] For the experimental research on the cytotoxicity of the dual drug-loaded nanocomposite carrier prepared in Example 3 to hela-Bcl2 tumor cells, see Figure 8 . Because the free small peptide itself cannot enter the cell, it has no killing effect on tumor cells; however, under the carrier of the composite nanocarrier, N9 can enter the cell and exert the function of inhibiting the growth of cancer cells. At a dose corresponding to 5 μg / ...

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Abstract

Dual-loaded peptide and chemotherapeutic drug nanocomposite carrier and preparation and application thereof. Dual-loaded peptide and chemotherapeutic drug nanocomposite carrier is prepared from mesoporous silica, dendritic macromolecule polymer, peptide anticancer drug and chemotherapeutic drug by physical embedding and electrostatic adsorption. Mesoporous silica nanoparticles with smaller size and larger pore size were synthesized by using cetyltrimethylammonium chloride as template, triethanolamine as pH regulator and TEOS as silicon source at a certain temperature and time. Double drug-loaded composite nanoparticles were prepared by group modification on mesoporous silica surface and assembled with dendrimers. The nanocomposite carrier of the double-loaded peptides and the chemotherapeutic drugs can be synergistically and efficiently used for Bcl-2 target rich in cancer drugs, also can be used in the preparation of drug-resistant cancer drugs to overcome the application.

Description

technical field [0001] The invention relates to a nanocomposite carrier double-loaded with peptides and chemotherapeutic drugs, in particular to a nanocomposite carrier double-loaded with peptides and chemotherapeutic drugs and its preparation method and application. Background technique [0002] The Bcl-2 family protein is an important protein in the apoptosis pathway. There are more than 20 Bcl-2 family proteins, and they have at least one of the four Bcl-2 homology domains. The Bcl-2 family proteins that have been discovered so far The -2 protein family can be divided into two categories according to their functions. One category has the same effect of inhibiting apoptosis as Bcl-2, such as mammalian Bcl-XL, Bcl-W, Mcl-1, A1 / Bfl-1, etc., while The other has pro-apoptotic effects, and is divided into two types: BH3-only proteins and multi-structural proteins, among which Bim, Bad, Bid, Puma and Noxa belong to BH3-only proteins, while Bax and Bak belong to multi-domain pro-...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/10A61K38/08A61K47/04A61K47/34A61P35/00A61K31/704
CPCA61K31/704A61K38/08A61K38/10A61K47/02A61K47/34A61P35/00A61K2300/00
Inventor 谢静静许卫霞张晓坤
Owner XIAMEN UNIV
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