Solid lipid magnetic resonance nanoparticle as well as preparation method and application thereof

A nanoparticle and solid lipid technology, applied in emulsion delivery, drug delivery, etc., can solve problems such as weak affinity, achieve low toxicity, high cell survival rate, and solve the problem of burst release

Active Publication Date: 2017-05-24
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Common methods for loading Gd-DTPA into SLN include solvent diffusion method, emulsification method, and high-pressure emulsion method. Short-term burst effect due to the fact that gadopentetate dimeglumine is a hydrophilic drug with weak affinity for SLN composed of lipid materials

Method used

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  • Solid lipid magnetic resonance nanoparticle as well as preparation method and application thereof
  • Solid lipid magnetic resonance nanoparticle as well as preparation method and application thereof
  • Solid lipid magnetic resonance nanoparticle as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Embodiment 1: Preparation of solid lipid nanoparticles loaded with Gd-DTPA

[0032] (1) First weigh 54mg Tween-80 and dissolve it in 3ml water to form the water phase, and dissolve 600mg Span-80 into 30ml n-hexane to form the organic phase, and add the water phase to the organic phase under stirring at room temperature at 400rpm, Probe ultrasound to make submicron emulsion;

[0033] (2) Then weigh 62.6mg of gadopentetate meglumine and dissolve in water to obtain an aqueous solution, dissolve 18mg of octadecylamine in 3ml of ethanol to obtain an ethanol solution, then combine the two at 60°C for 30min, and spin in vacuum at 60°C The solvent is evaporated to obtain an intermediate product;

[0034] (3) Add 3ml of ethanol, 90mg of monoglyceride and 10mg of lecithin mixture to the intermediate product prepared in step (2), inject it into the submicron emulsion prepared in step (1) under heating condition at 60°C, stir at room temperature for 5min; then centrifuge at 20000r...

Embodiment 2

[0035] Embodiment 2: The physicochemical property investigation of the solid lipid nanoparticle of loading Gd-DTPA

[0036] Take the solid lipid nanoparticles prepared above, use ultrapure water as a reconstitution solvent, and use a 3000HS particle size and surface potential analyzer to measure its particle size at a concentration of 0.01 mg / ml.

[0037] The encapsulation efficiency of Gd-DTPA in solid lipid nanoparticles was determined by indirect method. Fluorescence spectrophotometry (Ex=495nm, Em=514nm, Slit=5nm) measures the fluorescence value, calculates the amount of free Gd-DTPA in the solution, and calculates the encapsulation efficiency of the fluorescent graft by (1) formula:

[0038] Gd-DTPA encapsulation efficiency = (Wo-W free) / Wo*100% (1)

[0039]Gd-DTPA drug loading is calculated according to formula (2):

[0040] Gd-DTPA drug loading = (added drug * encapsulation efficiency) / (added drug * encapsulation efficiency + carrier material amount) * 100%

[0041...

Embodiment 3

[0043] Example 3: Research on in vitro drug release behavior of solid lipid nanoparticles loaded with Gd-DTPA

[0044] A certain volume of SLN solution was pipetted, placed in a dialysis bag (MWCO 3.5KDa) and then placed into a release tube containing 25ml of release medium (pH 7.2PBS). In vitro release was carried out at 37°C and 65rpm constant temperature shaking, samples were taken at specific time points (0.5h, 1h, 2h, 4h, 6h, 8h, 12h, 24h, 36h, 48h and 72h), and all release media were replaced at the same time. Measure the drug concentration in the sample by fluorescence spectrophotometry (Ex=275nm, Em=313nm, slit=5nm, working voltage=700V), and calculate the cumulative release and cumulative release percentage of the drug. The result is as image 3 shown.

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Abstract

The invention discloses a solid lipid magnetic resonance nanoparticle as well as a preparation method and application thereof. The preparation method comprises the following steps: using glyceryl monostearate and lecithin as lipid materials; compounding octadecylamine with gadopentetate meglumine serving as a magnetic resonance contrast agent; using trehalose as a freeze-drying protective agent, thus preparing a lipid nanoparticle which is easily absorbed by an intestinal canal. The preparation method disclosed by the invention is optimized on the basis of an existing preparation method of the solid lipid nanoparticle; after a nano contrast agent is ingested by a digestive tract, the release time of the gadopentetate meglumine in the nanoparticle, which is not absorbed by in-vivo tissues in the digestive tract, is prolonged, the imaging time of an MR living body is prolonged, an imaging time window of tumors such as breast cancer is increased, and the cytotoxicity of a material is reduced.

Description

technical field [0001] The invention relates to the preparation and optimization of a solid lipid nanoparticle carrier loaded with a magnetic resonance contrast agent gadopentetate meglumine and its in vitro drug release behavior, cell pharmacodynamics research, and in vitro MRI detection. Background technique [0002] Compared with traditional imaging examination methods such as CT, PET, X-ray, etc., MRI has higher spatial resolution, good soft tissue contrast, no ionizing radiation, and can display physiological and anatomical details to a certain extent. . However, in clinical practice, it is found that between benign and malignant tumor tissues, and between tumor tissues and normal tissues, the relaxation times T1 and T2 overlap with each other, and the signal intensity is not much different. Therefore, it is necessary to use MR contrast agents to improve the images between tissues. Contrast, and then improve the sensitivity and specificity of MRI diagnosis. The MRI co...

Claims

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Application Information

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IPC IPC(8): A61K49/18
CPCA61K49/18
Inventor 孙继红袁弘刘菲陈少青
Owner ZHEJIANG UNIV
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