Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Artemisinin-encapsulated heme nanometer vesicle, preparation method and purpose

A technology of nanovesicles and artemisinin, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve the problems of lack of verification, improve encapsulation efficiency, increase target Effects of tropism, weak drug systemic toxicity

Pending Publication Date: 2021-06-04
CHINA PHARM UNIV
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it lacks furth

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Artemisinin-encapsulated heme nanometer vesicle, preparation method and purpose
  • Artemisinin-encapsulated heme nanometer vesicle, preparation method and purpose
  • Artemisinin-encapsulated heme nanometer vesicle, preparation method and purpose

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0058] Example 1: Synthesis and Characterization of Lipid-Hemin

[0059] 1, method:

[0060] 1-tattol-SN-propanediol-phosphate (Lyso 16:0) added to 50 ml round bottom flask, dissolved with anhydrous dichloromethane, add 0.5 equivalent hemin, 0.75 equivalent 4-two Metaminopyridine (DMAP), 3 equivalents of 1- (3-dimethylaminopropyl) -3-ethyl carbon diimide (EDC), if necessary, 1 ml N, N-dimethylformamide ( DMF) Help. The mixture was stirred for 48 hours under anhydrous oxygen-free dark conditions to complete the esterification reaction. Dry repeatedly. Further, the purified lipid-hemin was obtained by the column chromatography chromatography.

[0061] The reaction steps are as follows:

[0062]

[0063] 2, result

[0064] HPLC-MS characterization was performed on purified lipid-hemin, figure 1 As shown in, 1130.06 is LiPid-Hemin + H + , Indicating successful synthesis of lipid-hemin. In the infrared spectrum, through LiPID free hydroxyl restriction (wide peak, 3500 ~ 4000cm -1 ), ...

Example Embodiment

[0065] Example 2: Preparation method and characterization of FA-HEMESME-ART

[0066] 1, method:

[0067] According to the molar ratio of lipid-hemin-peg2000-fa = 85:13: 2, dissolved in chloroform: mixed solvents of methanol = 2: 1 (v: V); 10 mole% ART added In the above, in the above-mentioned phospholipid mixed liquid, the phospholip film is evaporated to give a phospholip film; 5 mL of phosphate buffer salt solution (PBS, pH 7.4), hydration of 1 h, freeze-thaw cycle; over 0.1 μm polycarbonate film The extruder is extruded, a 0.22 μm filter, ultrafiltration centrifugation 3000 rpm, 20 minutes, and purified FA-HeMesome-Art NPS.

[0068] 2, result

[0069] Its TEM morphology observation image 3 As shown, there is a spherical structure in size.

Example Embodiment

[0070] Example 3: Fa-Hemesome-ART nanoholic stability

[0071] 1, method

[0072] Under the conditions of PBS, SGF, SIF and medium (DMEM, 10% serum), in the process of incubation 48h, measurement of the hydrated particle size of FA-Hemesome-ART nanocolis (LiteSizer) during the corresponding time point (LiteSizer TM 500, Anton Paar, Austria.

[0073] 2, result

[0074] Under different environmental conditions, the particle size of FA-HEMESOME-ART NPS increases with incubation time as Figure 4 Indicated. Under the conditions described above, there was no significant change in particle size, which proved the stability of the nanocarburities in the gastrointestinal tract and blood. In addition, the size is slightly large in SIF and SGF, possibly due to increased particle size of the protein in the nanocarburization and the medium, but in an acceptable range, the intake of nanohububs and the in vivo absorption have little effect.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Diameteraaaaaaaaaa
Login to View More

Abstract

The invention discloses an artemisinin-encapsulated heme nanometer vesicle, a preparation method and a purpose. The vesicle comprises an inner nuclear layer and an outer shell layer, wherein the outer shell layer consists of phospholipid-hemin conjugate and other phospholipids and is coated to the outer surface of the inner nuclear layer, and the diameter of the vesicle is 100-200nm. The nanometer vesicle prepared by the invention can carry out targeted accumulation on a tumor position, in addition, under a tumor microenvironment, the heme is released, and meanwhile, the artemisinin is stimulated to perform an anti-tumor function so as to realize a tumor curing effect. In addition, the nanometer vesicle has high oral bioavailability, in addition, tumor cells can generate immunogenic cell death (ICD), and organism immunoreaction is aroused to further kill tumor cells. Due to the excellent targeting ability and cancer treatment effect of the artemisinin-encapsulated heme nanometer vesicle, the artemisinin-encapsulated heme nanometer vesicle can be used as a novel oral anti-cancer agent without side effects.

Description

technical field [0001] The invention relates to nanomaterials, preparation methods and uses, in particular to heme nanovesicles encapsulating artemisinin, preparation methods and uses. Background technique [0002] The current treatment methods for cancer include radiotherapy, surgery, and systemic therapy, among which systemic therapy includes chemotherapy, hormone therapy, immunotherapy, and targeted therapy. Chemotherapy is the most commonly used clinical treatment, but its toxic and side effects have become an important factor hindering its development. Therefore, it is urgent to develop a natural drug and treatment method with good therapeutic effect, high biological safety and low cost. [0003] Studies have shown that artemisinin (artemisinin, ART) and its derivatives, in addition to strong antimalarial activity, also have obvious anticancer activity, and have no obvious side effects. It is generally believed that its mechanism of action is due to the activation and ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/366A61K31/555A61K45/06A61K47/54A61K9/127A61P35/00
CPCA61K31/366A61K31/555A61K45/06A61K47/544A61K9/1273A61P35/00A61K2300/00
Inventor 孙晓莲王晴郭敬儒
Owner CHINA PHARM UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com