Fluorocarbon nano medicine-carrying system and preparation method thereof

A technology of fluorocarbons and nano-drug loading, which is applied in the field of chemistry and can solve problems such as no drug-targeted treatment system

Inactive Publication Date: 2009-07-22
RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to provide a fluorocarbon nanometer drug-carrying system and its preparation method. The fluorocarbon nanometer drug-carrying system should solve the problem that there is no suitable method for patients who are not suitable for intravascular treatment in the prior art. Technical Issues in Drug-Targeted Therapy Systems

Method used

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  • Fluorocarbon nano medicine-carrying system and preparation method thereof
  • Fluorocarbon nano medicine-carrying system and preparation method thereof
  • Fluorocarbon nano medicine-carrying system and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Precisely weigh 100mg of dexamethasone acetate powder or 20ml of dexamethasone sodium phosphate solution, add 5ml of gadopentetate meglumine, 0.6g of cholesterol, 1.2g of lecithin, 20mg of biotinylated phosphatidylethanolamine, and dissolve in about 30ml of three Chloromethane, fully oscillate and dissolve in a fume hood, add to a rotary evaporator to form a drug film, then add 20ml of perfluorocarbon solution and 1ml of safflower oil, add deionized water to make the volume 100ml, and ultrasonically shake in the cell disruptor Become microemulsion, put in the high pressure homogenizer then, low pressure (700 Pa) circulates 3 times, high pressure (1500 Pa) circulates 5 times, promptly obtains the present invention.

[0032] figure 1 It is a structural schematic diagram of the present invention, 1 is perfluorocarbon, 2 is lipid layer, 3 is contrast agent, 4 is glucocorticoid anti-inflammatory drug, 5 is biotinylated phosphatidylethanolamine.

[0033] After the nano-high ...

Embodiment 2

[0035] 1. Cell inhibition test of perfluorocarbon drug-loaded nanoparticles

[0036] Take the 4th generation of SMC cultured cells, put them into a centrifuge tube after trypsinization, and centrifuge at 1000rpm for 5min; discard the supernatant, add 10% fetal bovine serum culture medium, adjust the cell density to 10000 / ml; take a 96-well plate, Inoculate 100ul of cell suspension (n=5) into the wells, the outer circle is PBS control, incubate in a 5% CO2 incubator at 37°C for 1 day; drain the culture solution, add 100ul of serum-free culture medium / well, incubate in a 5% CO2 incubator at 37°C 1d; Aspirate the culture medium, add 10% FBS DMEM containing 100ul dexamethasone (concentration 10ug / ml), perfluorocarbon drug-loaded nanometer (5%, v / v), PFC (1.5%, v / v); 37 Incubate in a 5% CO2 incubator at ℃, take out the culture plate after 3 days, add cck~8 10ul to each well and incubate for 3 hours; detect the absorbance value at 450nm wavelength with a microplate reader; Analysis...

Embodiment 4

[0049] In the in vitro release system, nanoparticles loaded with dexamethasone acetate have good sustained release. Precisely measure 5ml of nanoemulsion loaded with dexamethasone acetate (n=3) and put it into the semi-permeable membrane, and clamp it with locks at both ends. The semi-permeable membrane was placed in 200ml of human albumin saline with a concentration of 0.5mg / ml, the constant temperature shaker was set at 20°C, 60rpm, the solution was extracted and replenished regularly, and the extracted solution samples were frozen at -20°C. Specimen processing: Take 0.5ml of the specimen solution, add 0.5ml of methanol, centrifuge (10000rpm, 10min) after full shaking, and perform HPLC detection on the supernatant, the chromatographic conditions are C18 column (diamonsil), detection wavelength 240nm, mobile phase: methanol / water, 74: 26. The velocity of the mobile phase is 1ml / min, and the drug retention time is 10.41min.

[0050] The concentration linearity results of dexa...

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Abstract

The invention relates to a fluorocarbon nanodrug delivery system, which comprises a superparamagnetic full fluorocarbon core and a drug delivery lipid layer, wherein the lipid layer is coated with a glucocorticoid anti-inflammatory agent, a magnetic resonance contrast agent and phosphatidylethanolamine which is connected with biotins; full fluorocarbon accounts for 26 to 32 weight percent of the nanodrug delivery system; the lipid layer accounts for 6.8 to 7.2 weight percent of the nanodrug delivery system; the balance is water; the glucocorticoid anti-inflammatory agent in the lipid layer accounts for 1.5 to 3 weight percent; the magnetic resonance contrast agent in the lipid layer accounts for 62 to 68 weight percent; the phosphatidylethanolamine which is connected with the biotins accounts for 0.5 to 1 weight percent in the lipid layer; and the balance is lipid material. Nano particles are connected with special antibodies through a biotin-avidin system and combined with antibody epi positions of target cells; the nano surface lipid layer and cell surfaces are subjected to lipid exchange to achieve the aim of slow release of medicines; the full fluorocarbon core can strengthen the strength of magnetic resonance detection signals of a paramagnetic contrast agent on the vector surface; and the fluorocarbon nanodrug delivery system can perform early diagnosis on diseases through a pathological mechanism of the diseases positioned and displayed by target molecules.

Description

Technical field: [0001] The invention relates to the field of chemistry, in particular to a method for preparing medicines, in particular to a fluorocarbon nanometer drug-carrying system and a preparation method thereof. Background technique: [0002] Endoluminal angioplasty, autogenous vein or artificial vascular bypass are the main methods for the treatment of arterial occlusive diseases, but the restenosis caused by intimal thickening is the main reason affecting the long-term patency rate of vascular reconstruction. Vascular intimal hyperplasia involves the proliferation and migration of vascular smooth muscle cells into the intima, extracellular matrix synthesis and vascular remodeling. Currently, inhibition of smooth muscle proliferation is considered to be the main strategy for the treatment and prevention of restenosis. Recently, many stent-based anti-proliferative drug delivery systems have achieved good results in inhibiting intimal hyperplasia through local admin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/10
Inventor 张纪蔚周兆熊张皓张伯根
Owner RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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