Unlock instant, AI-driven research and patent intelligence for your innovation.

A PEG vitamin E-periplocymarin conjugated nanoparticle, and preparation method and use thereof

The technology of salicyside conjugate and salicyside conjugate, which can be applied in the directions of drug combination, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve applications that do not involve anti-tumor activity, etc. To achieve the effect of enhanced tumor inhibition effect, improved stability, and improved tumor tissue distribution in vivo

Pending Publication Date: 2018-02-23
JIANGSU UNIV
View PDF1 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Chinese patent application CN201010583339.0 "A Preparation Method of Glycoside" is about the preparation method of Glycoside, and does not involve the application of the drug in anti-tumor activity

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A PEG vitamin E-periplocymarin conjugated nanoparticle, and preparation method and use thereof
  • A PEG vitamin E-periplocymarin conjugated nanoparticle, and preparation method and use thereof
  • A PEG vitamin E-periplocymarin conjugated nanoparticle, and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1. Preparation of vitamin E-baricoligoside conjugates

[0043] Weigh dithiol diglycolic acid (0.2g, 1.10mmol) into 3mL of acetic anhydride, stir and react at 30°C for 2h, add an appropriate amount of toluene after the reaction, pressurize and spin-dry toluene and acetic anhydride to obtain an oily liquid, add 2mL of Dissolve in dichloromethane with water, then add VE (0.1g, 0.23mmol) and appropriate amount of DMAP, stir the reaction at room temperature for 5min, and purify with silica gel column, the eluent is n-hexane / ethyl acetate / acetic acid=10 / 1 / 1, The product VE-S-S-COOH (114 mg) was obtained.

[0044] Weigh VE-S-S-COOH (120mg) and saccharidin (100mg), add 6mL of anhydrous dichloromethane to dissolve, add dicyclohexylcarbodiimide (DCC) (48mg) and 4-dimethylaminopyridine (DMAP) (30mg), stirred at room temperature for 2h, filtered to remove dicyclohexyl urea (DCU), purified with a silica gel column, the eluent was petroleum ether / ethyl acetate=2 / 3, and the t...

Embodiment 2

[0046] Example 2. Synthesis, purification and characterization of mPEG2000-LD

[0047] Weigh linoleic acid (500mg), mPEG (100mg), DCC (400mg) and DMAP (240mg), add 20mL of anhydrous dichloromethane, stir for 12h, filter to remove DCU, wash dichloromethane with saturated sodium chloride solution After layering, add anhydrous sodium sulfate to dry, filter the organic layer, spin dry, add petroleum ether and wash three times, filter the insoluble matter that is the target product PEG2000-LD, use 1 Characterized by H-NMR, such as figure 2 shown.

Embodiment 3

[0048] Example 3. Preparation of PPM-S-S-VE Nanoparticles (PSSV-NPs) and Novel PEGylated Vitamin E-Salidin Conjugate Nanoparticles (MPSSV-NPs)

[0049] Prepare nanoparticles by one-step nano-precipitation method, the steps are as follows: prepare PPM-S-S-VE absolute ethanol solution 20mg / mL, absorb 200uL slowly dropwise into 2mL double-distilled water under stirring conditions, spin dry to remove ethanol, and obtain PSSV -NPs. The steps of the novel PEGylated vitamin E-salicidin conjugate nanoparticles (MPSSV-NPs) are as above, except that different contents of mPEG2000-LD (mass ratio of 1: 0.1, 1:0.2, 1:0.4, 1:0.8).

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention provides a PEG vitamin E-periplocymarin conjugate nanoparticle. Dimercaptan dihydroxyacetic acid is used as bonding agent; periplocymarin and vitamin E are conjugated to form pro-drug; and the pro-drug can be self-assembled to be nanoparticle in water media. The invention also discloses the PEG vitamin E-periplocymarin conjugate nanoparticle. Based on disulfide bond-S-S-conjugated vitamin E and periplocymarin, and by use of the self-assembled PEG vitamin E-periplocymarin conjugate nanoparticle decorated by methoxy polyethylene glycol 2000-linoleic acid (PEG2000-LD), the nanoparticle has following functions: 1, the nano pre-drug is capable of improving inner and outer stability of prototype drug periplocymarin and prolonging inner circulation time; 2, the releasing and the degradation of the nano pre-drug are sensitive to glutathione (GSH); 3, liver / liver cancer targeting performance is high; and 4, treatment effects of liver cancer by the prototype drug periplocymarin.

Description

technical field [0001] The invention relates to a vitamin E-barer salicidin conjugate nanoparticle, a novel PEGylated vitamin E-barer salicidin conjugate nanoparticle, a preparation method thereof and an application as an antitumor drug. Background technique [0002] The application of cardiotonic steroid active ingredients in tumor treatment began in ancient China, when it was recorded that toad secretion could be used to treat cancer. It has been found that the anti-tumor component in toad secretion is bufalin, a type-a cardiotonic steroid component. Studies have reported that in patients who used digoxigenin for heart disease, it was found that the concentration of digoxigenin in the blood was significantly negatively correlated with the incidence of blood and urinary system tumors, and breast cancer patients who used digoxigenin The mortality rate of patients was significantly lower than that of patients who did not use digoxigenin. At present, the active ingredients o...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/69A61K47/54A61K31/7048A61K31/355A61K31/585A61P35/00
CPCA61K31/355A61K31/585A61K31/7048
Inventor 徐希明张辉云余江南
Owner JIANGSU UNIV