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Drug-loaded silicone grease ultrasonic contrast agent and its preparation method and use

An ultrasound contrast agent and siliceous lipid technology, which is applied in the field of nanomaterials, can solve the problems of insufficient envelope strength to encapsulate gas and drugs at the same time, enhance the ability of contrast and HIFU treatment, adverse biological effects, etc., to prolong blood circulation. time, good for accuracy, strong signal strength

Inactive Publication Date: 2015-08-12
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the research on film-forming materials of contrast agents has been reported: lipids, polymers, and mesoporous silica hollow nanoparticles, etc., but these materials have limitations: lipid-based ultrasound contrast agents have the advantage of being safe to use , but it has shortcomings such as short development time, insufficient envelope strength to wrap gas and drug at the same time, poor stability, etc., so it cannot meet the real-time continuous enhancement of contrast and the ability of HIFU treatment
The biggest disadvantage of high molecular polymers and inorganic non-metallic nanoparticles (such as silicon dioxide, carbon nanotubes, etc.) is that the material is too rigid, and imaging requires high acoustic output, which is likely to cause adverse biological effects

Method used

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  • Drug-loaded silicone grease ultrasonic contrast agent and its preparation method and use
  • Drug-loaded silicone grease ultrasonic contrast agent and its preparation method and use
  • Drug-loaded silicone grease ultrasonic contrast agent and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: Preparation and characterization of silicon lipid contrast agent loaded with doxorubicin and perfluoropentane (PFP)

[0051] Weigh 4 mg silicon lipid, 5 mol % DSPE-PEG 2000 and doxorubicin (drug-to-lipid ratio 1:25) and dissolve in 3 mL chloroform, add 1 mL PBS, vortex and mix well to obtain opalescent homogeneous dispersion. The organic solvent was removed by rotary evaporation to obtain a high viscosity gel. Add 3 mL of PBS to the above gel solution, and quickly inject 50 μL of PFP, phacoemulsify the probe in an ice bath for 3 min, work for 3 s and stop for 3 s to obtain a silicone lipid contrast agent pre-emulsion loaded with doxorubicin and PFP ( figure 1 a) Dialyze for 1 h to obtain a silicon lipid contrast agent loaded with doxorubicin and PFP, hereinafter referred to as drug-loaded silicon lipid contrast agent ( figure 1 b).

[0052] The preparation method of the nanoemulsion loaded with doxorubicin is the same as the above method, except that th...

Embodiment 2

[0055] Example 2 In vitro ultrasound imaging experiment

[0056] Take 1 mL of the drug-loaded silicone lipid contrast agent prepared in Example 1 and add it to a dropper filled with 3 mL of degassed water, and place it in a temperature-controllable water bath at a temperature of 37°C (the boiling point of PFP is 29°C). Toshiba Aplio 500 Doppler Ultrasonic Diagnostic Instrument for ultrasonic detection, set the frequency of ultrasonic detection to 3.5 MHz and the mechanical index to 0.08, and observe the in vitro imaging results of the contrast agent. Depend on Figure 4 It can be seen that the contrast agent has a continuous developing effect of up to 20 min, indicating that the contrast agent with silicone lipid as the shell material can last for ultrasound imaging. By comparing the drug-loaded silicone lipid contrast agent ( Figure 5 b) and drug-loaded distearoylphosphatidylcholine (DPPC) lipid contrast agent ( Figure 5 The ultrasound imaging signal intensity in a) show...

Embodiment 3

[0057] Example 3 HIFU synergist treatment experiment of isolated porcine liver tissue

[0058] Design pig liver experimental tank device, such as Image 6 As shown, it includes a 37°C constant temperature control circuit, a deoxygenated water circulation pump and a pig liver fixation patch, etc. Select the HIFU diagnosis and treatment equipment produced by Shenzhen Prohuiren Medical Technology Co., Ltd., and set the transducer irradiation parameters: strike frequency 1.28 MHz, strike time 0.20 seconds, interval time 0.10 seconds, strike times 15 times, strike power 210 watts.

[0059] Use the color Doppler imaging mode of the ultrasonic diagnostic instrument to locate the position of the HIFU irradiation target, such as Figure 7 As shown in a1~c1, 2 mL of PBS, drug-loaded silicone lipid nanoemulsion and drug-loaded silicone lipid contrast agent were injected into the pig liver tissue through the needle, and the ultrasound before and after the ablation of the target area was...

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Abstract

The invention provides a preparation method of a drug-loaded silicone grease ultrasonic contrast agent. The preparation method comprises fully dissolving silicone grease, polyethylene glycol phosphate derivatives and a fat-soluble anticancer drug in an organic solvent, adding water into the solution, carrying out whirling, removing the organic solvent, supplying water with a volume 3 times that of the solution into the solution, carrying out ultrasonic disintegration by an ultrasonic disintegrator, simultaneously and fast adding liquid fluorocarbon into the solution to obtain a pre-emulsion, and carrying out dialysis on the pre-emulsion in PBS for 1h to obtain a product. The preparation method has simple processes. The product has the average particle size of about 100nm and is conducive to aggregation at a tumor position by internal EPR effects. Siloxane silicone grease network distribution substantially improves structure stability and prolongs internal blood circulation time. Through HIFU, the drug-loaded silicone grease ultrasonic contrast agent release drugs at a local part of tumor tissue, drug treatment targeting is improved, HIFU treatment effects are substantially improved and HIFU-chemotherapy combined treatment is realized.

Description

technical field [0001] The invention belongs to the technical field of nanomaterials, and more specifically relates to a preparation method and application of a drug-loaded silicon lipid ultrasonic contrast agent. Background technique [0002] As a non-invasive, low-cost, real-time imaging technology, ultrasound diagnosis is currently the most widely used imaging method. Ultrasound contrast agent is a kind of diagnostic reagent that can significantly enhance the signal of medical ultrasound detection, and it is a preparation containing high concentration of microbubbles. In terms of diagnosis, it can improve the sensitivity and specificity of diagnosis and is widely used. In addition to being used as a diagnostic reagent, ultrasound contrast agents have important research and application values ​​in many fields such as drug delivery and release, promotion of thrombolysis, and gene transfection. High Intensity Focused Ultrasound (HIFU for short) is one of the emerging non-i...

Claims

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Application Information

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IPC IPC(8): A61K49/22A61K41/00A61K47/34A61K47/24A61K45/00A61P35/00
Inventor 曹众李佳罗新杨斌健陈薇玲蒋庆
Owner SUN YAT SEN UNIV
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