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Lipidosome nano medicine delivery system as well as preparation method and application thereof

A delivery system and nano-drug technology, applied in liposome delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of limited imaging half-life, plaque rupture, large space occupation, etc., and achieve the effect of improving drug enrichment

Active Publication Date: 2018-05-04
苏州影睿光学科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main reason is that the occurrence of atherosclerosis generally has no obvious symptoms in the early and middle stages, and acute emergencies such as stroke and myocardial infarction caused by plaque rupture and shedding in the late stage are difficult to prevent in advance
Existing biomedical imaging techniques include magnetic resonance imaging (MRI), computed tomography (CT), ultrasound imaging (UI), nuclear medicine imaging (positron emission tomography [PET] and single photon emission computed tomography [SPECT] ) etc. due to their own characteristics determine that there are various limitations in the detection of atherosclerotic plaques in vivo: MRI has low spatial resolution and time-consuming and cannot be imaged in real time; CT imaging is based on X-ray intensity attenuation and is only applicable to bone Tissue imaging; ultrasound imaging cannot specifically image plaques, and the resolution and sensitivity are not high; PET and SPECT have low spatial resolution, and imaging is limited by the half-life of radiotracers
In liposomes prepared by this method, quantum dots exist in the inner cavity of the liposome, which takes up a large space and affects the targeting efficiency

Method used

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  • Lipidosome nano medicine delivery system as well as preparation method and application thereof
  • Lipidosome nano medicine delivery system as well as preparation method and application thereof
  • Lipidosome nano medicine delivery system as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0048] Near-infrared Ag Modified by Tumor Vascular Targeting Peptide 2 Preparation of S quantum dot liposome nano drug delivery system:

[0049] The liposome raw material component is hydrogenated soybean phospholipid (HSPC) / cholesterol (Chol) / distearoylphosphatidylethanolamine-polyethylene glycol complex (DSPE-mPEG) (45:45:2, molar ratio), tumor Vascular targeting peptide modified RGD distearoylphosphatidylethanolamine-polyethylene glycol complex HSPC / Chol / DSPE-mPEG / DSPE-mPEG-RGD (45:45:2:1, molar ratio). The above components were combined with dodecanethiol-modified near-infrared silver sulfide quantum dots (DT-Ag 2 S) Fully dissolve in chloroform, remove the organic solvent by rotary evaporation, add physiological saline to the lipid film, and rotate and shake in a water bath at 55°C to obtain Ag 2 S quantum dot liposome suspension. Further heating to 60° C., extruding through the membrane with a 200 nm carbonate membrane to obtain a liposome nano drug delivery system wi...

Embodiment 2

[0055] Near-infrared Ag Modified by Atherosclerotic Vulnerable Plaque Targeting Peptide VHPK 2 Preparation of Se quantum dot liposome nano drug delivery system:

[0056] The liposome raw material component is hydrogenated soybean phospholipid (HSPC) / cholesterol (Chol) / distearoylphosphatidylethanolamine-polyethylene glycol complex (DSPE-mPEG) (50:50:2, molar ratio), arterial Atheroma Vulnerable Plaque Targeting Peptide VHPK Modified Distearoylphosphatidylethanolamine-Polyethylene Glycol Complex HSPC / Chol / DSPE-mPEG / DSPE-mPEG-RGD (50:50:2:0.5, mol Compare). The above-mentioned components were fully dissolved in chloroform, and the organic solvent was removed by rotary evaporation, and silver selenide quantum dots (PEG-Ag-Ag) containing polyethylene glycol modified 2 The physiological saline of Se) was added to the lipid film, and rotated and oscillated in a water bath at 55°C to obtain Ag 2 Se quantum dot liposome suspension. Further heating to 60° C., extruding through the m...

Embodiment 3

[0062] Preparation of folic acid (FA)-modified near-infrared InAs quantum dot liposome nano-drug delivery system:

[0063] The liposome raw material components are hydrogenated soybean phospholipids (HSPC) / cholesterol (Chol) / distearoylphosphatidylethanolamine-polyethylene glycol complex (DSPE-mPEG) (60:55:1, molar ratio), folic acid Modified distearoylphosphatidylethanolamine-polyethylene glycol complex HSPC / Chol / DSPE-mPEG / DSPE-mPEG-RGD (60:55:1:0.5, molar ratio). The above components were fully dissolved in chloroform, and the organic solvent was removed by rotary evaporation, and the physiological saline containing polyethylene glycol-modified indium arsenide quantum dots (PEG-InAs) was added to the lipid film, and rotated and oscillated in a 55°C water bath , to obtain InAs quantum dot liposome suspension. Further heating to 60° C., extruding through the membrane with a 200 nm carbonate membrane to obtain a liposome nano drug delivery system with uniform particle size.

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Abstract

The invention provides a lipidosome nano medicine delivery system as well as a preparation method and application thereof. The lipidosome nano medicine delivery system comprises a quantum dot and lipidsome, wherein the quantum dot is embedded into a lipid bilayer of the lipidsome; and the lipidsome structurally comprises targeting ligand. The lipidosome nano medicine delivery system prepared by using the preparation method provided by the invention has a double-ligand targeting function, by virtue of targeting titanium of atherosclerotic plaque at different development stages, living targetingof early-stage, middle-stage and late-stage atherosclerotic plaque is achieved, the medicine enrichment of a focus area is improved, and in addition, a near-infrared developing agent can be adopted for in-vivo medicine distribution tracing and treatment effect observation on atherosclerosis.

Description

technical field [0001] The invention belongs to the field of nano-biological materials, and relates to a liposome nano-medicine delivery system and a preparation method and application thereof. Background technique [0002] Cardiovascular disease (CVD) is the primary disease that threatens human health. The World Health Organization pointed out that the number of deaths due to CVD in the world currently exceeds 17 million, and it is increasing year by year. It is estimated that by 2030, about 23 million people worldwide will die of CVD, mainly due to heart disease and stroke. [0003] Studies have shown that atherosclerosis and its complications are the most common causes of cardiovascular disease-related death. Atherosclerotic plaques are not islands but involve multiple processes such as lipid deposition, macrophage ER stress, smooth muscle cell migration, and collagen proliferation, and express proinflammatory proteins, extracellular matrix proteins, and proteases Wait....

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K49/00A61P9/10
CPCA61K9/127A61K47/24A61K49/0019A61K49/0067
Inventor 王强斌李春炎张叶俊陈光村
Owner 苏州影睿光学科技有限公司
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