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Inner-outer double layer stepwise stimulation response delivery nano-carrier, and preparation method and application thereof

A transmission carrier and stimuli-response technology, which is applied in the field of inner and outer double-layer stimuli-response nano-transmission carriers and its preparation, can solve the problems of early release of loaded drugs, low drug bioavailability, and small amount of intracellular drug release, and achieve improved The effect of drug bioavailability, good water dispersibility and good biocompatibility

Inactive Publication Date: 2018-02-02
GUANGDONG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, limited by the complex physiological environment in the body, mesoporous silicon nanotransport carriers are easily cleared by the immune system, early release of loaded drugs, low cell internalization rate, and low intracellular drug release, resulting in low bioavailability of drugs. , the clinical application efficiency is low

Method used

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  • Inner-outer double layer stepwise stimulation response delivery nano-carrier, and preparation method and application thereof
  • Inner-outer double layer stepwise stimulation response delivery nano-carrier, and preparation method and application thereof
  • Inner-outer double layer stepwise stimulation response delivery nano-carrier, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] (1) Dissolve 1.0g CTAB (cetyltrimethylammonium bromide) in a mixed solution of 480mL water and 3.5mL 2.0mol / L NaOH, raise the temperature to 70°C, add dropwise 5.0mL (22mmol ) TEOS (tetraethyl orthosilicate), 0.25mL (1.1mmol) APTES (γ-aminopropyltriethoxysilane) and 2.0mL 1,3,5-trimethylbenzene, keeping the reaction temperature at 70°C, stirring vigorously Reaction 2h. After completion of the reaction, the precipitate was filtered, washed with methanol, and the obtained product was dispersed in 50 mL of ethanol-HCl solution (48 mL of absolute ethanol+2 mL of concentrated hydrochloric acid with a concentration of 37% (w / v) was mixed), and the mixture was vigorously heated at 80 ° C. Stir for 10 h, remove CTAB, finally filter the precipitate, and dry in vacuum to obtain aminated mesoporous silicon nanoparticles. Disperse 0.20g of aminated mesoporous silicon nanoparticles in an aqueous solution, add 0.05g of 3,3'-dithiodipropionic acid and 0.04g of EDC, react at room temp...

Embodiment 2

[0049] (1) As a reference, an equivalent amount of succinic anhydride was used to replace 3,3'-dithiodipropionic acid, and other steps were the same as step (1) in Example 1 to prepare nanoparticles without disulfide bonds.

[0050] (2) Add 0.20 g of nanoparticles without disulfide bonds to 5 ml of PBS solution (pH 7.4) containing 0.02 g of doxorubicin hydrochloride, and stir for 24 hours to fully adsorb the doxorubicin to the mesoporous silicon nanoparticles , then add 0.10g PEI to the nanoparticle dispersion loaded with doxorubicin, then add 0.05g EDC and 0.03g NHS to catalyze the reaction. After the reaction is complete, centrifuge at 10,000 rpm for 5 minutes to remove ungrafted polymers. The product is freeze-dried to obtain the PEI / mesoporous silicon nanocarrier loaded with doxorubicin.

[0051] (3) Dissolve 0.05g of 2,3-dimethylmaleic anhydride in 10ml of DMSO, add 0.20g of PEI / mesoporous silicon nanocarrier loaded with doxorubicin, and react for 24h under nitrogen prot...

Embodiment 3

[0053] (1) The preparation process is the same as step (1) of Example 1 to obtain nanoparticles containing disulfide bonds.

[0054] (2) The second-generation polyamide-amine dendrimer (PAMAM) was prepared according to the method reported in the literature [Mesoporous siliconanoparticles with controlled loading of cationic dendrimer for gene delivery. Materials Research Express, 2014, 1:035403.].

[0055] (3) Add 0.20 g of nanoparticles containing disulfide bonds to 5 ml of PBS solution (pH 7.4) containing 0.02 g of doxorubicin hydrochloride, and stir for 24 hours to fully absorb the doxorubicin into the mesoporous silicon nanoparticles , and then add 0.10g PAMAM to the doxorubicin-loaded nanoparticle dispersion, then add 0.05g EDC and 0.03g NHS to catalyze the reaction. After the reaction is complete, centrifuge at 10,000 rpm for 5 minutes to remove ungrafted polymers. The product is freeze-dried to obtain the PAMAM / mesoporous silicon nanocarrier loaded with doxorubicin.

...

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Abstract

The invention discloses an inner-outer double layer stepwise stimulation response delivery nano-carrier, and a preparation method and an application thereof. The preparation method comprises the following steps: dispersing disulfide bond-modified MCM-41 type mesoporous silicon nano-particles in a solution, coupling the surface of the nano-particles with a cationic polymer, and then coupling the surface of the nano-particles with 2,3-DMMA through the cationic polymer to prepare the meso-porous silicon nano-carrier having double stimulation response. The nano-carrier has the outer-to-inner layerstepwise stimulation response characteristic with the outer layer corresponding to pH stimulation response and the inner layer corresponding to redox reduction stimulation response. Drug molecules can be encapsulated into the meso-pores of the nano-particles, and the cationic polymer can bind genes, so the nano-carrier is suitable for preparing drug delivery carriers, nucleic acid delivery carriers or drug-nucleic acid co-delivery carriers.

Description

technical field [0001] The invention belongs to the field of nano-pharmaceuticals, in particular to an inner and outer double-layered stepwise stimulation-responsive nano-transmission carrier, a preparation method and application thereof. Background technique [0002] In recent years, drug delivery systems (DDS) based on nanotechnology have shown remarkable achievements in cancer treatment, mainly because nano drug carriers can improve the kinetics and pharmacodynamics of drugs by enhancing the penetration and retention effect (EPR). . Among them, mesoporous silicon nanoparticles (MSNs) are nanoparticles with a porous structure. The DDS system based on MSNs has received extensive attention in the delivery and controlled release of drugs and genes. MSNs have the following advantages as nano-transport carriers: ①Good Biocompatibility, non-cytotoxicity; ②Has an ordered pore structure, huge surface area, can effectively embed small molecules and biomacromolecules inside the par...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/62A61K47/02A61K31/704A61K48/00A61P35/00
CPCA61K31/704A61K47/02A61K48/0041
Inventor 王冠海
Owner GUANGDONG MEDICAL UNIV
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