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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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Common methods for loading Gd-DTPA into SLN include solvent diffusion method, emulsification method, and high-pressure emulsion method. Short

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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

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

[0032] (1) First, weigh 54mg Tween-80 dissolved in 3ml water to form the water phase, 600mg Span-80 dissolved in 30ml n-hexane to form the organic phase, add the water phase to the organic phase under stirring conditions at room temperature at 400rpm. Probe ultrasound to prepare submicroemulsion;

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

[0034] (3) Add 3ml ethanol, 90mg monoglyceride and 10mg lecithin mixture to the intermediate product prepared in step (2), inject it into the submicroemulsion prepared in step (1) under heating at 60°C, stir at room temperature for 5 minutes; then centrifuge at 20,000 rpm After 20 min...

Example Embodiment

[0035] Example 2: Investigation of the physical and chemical properties of Gd-DTPA-loaded solid lipid nanoparticles

[0036] The solid lipid nanoparticles prepared above were taken, ultrapure water was used as the resolvent, and the particle size was measured with a 3000HS particle size and surface potential analyzer at a concentration of 0.01 mg / ml.

[0037] The indirect method was used to determine the encapsulation efficiency of Gd-DTPA in solid lipid nanoparticles. Fluorescence spectrophotometry (Ex=495nm, Em=514nm, Slit=5nm) was used to measure the fluorescence value, calculate the amount of free Gd-DTPA in the solution, and calculate the encapsulation rate of the fluorescent graft according to formula (1):

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

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

[0040] Gd-DTPA drug loading=(additional drug*encapsulation rate) / (additional drug*encapsulation rate+carrier material dosage)*100%

[0041...

Example Embodiment

[0043] Example 3: In vitro drug release behavior of Gd-DTPA-loaded solid lipid nanoparticles

[0044] Pipette a certain volume of SLN solution, place it in a dialysis bag (MWCO 3.5KDa), and then put it into a release tube containing 25ml of release medium (pH 7.2PBS). In vitro release was performed under constant temperature shaking at 37°C and 65 rpm, and 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 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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