Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Lipid-mixed poly (lactic-co-glycolic acid) (PLGA) nanoparticle having high drug loading amount and active targeting effect

An active-targeting, high-drug-loading technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and drug combinations, can solve the problem of reducing drug delivery efficiency and curative effect, and reducing tumor targeting , poor hydrophilicity and other problems, to achieve the effect of increasing drug loading, improving curative effect and increasing intake

Inactive Publication Date: 2015-03-25
FOURTH MILITARY MEDICAL UNIVERSITY
View PDF1 Cites 15 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

PLGA has the characteristics of non-immunogenicity and biodegradability, and is widely used in various targeted drug delivery systems, but PLGA nanoparticles still have the following problems: (1) low drug loading, usually less than 3%; (2) affinity Poor water quality, easy to be cleared by the immune system in blood circulation, and reduced tumor targeting; (3) PLGA nanoparticles are difficult to escape from lysosomes, and the loaded drugs are easily stored in lysosomes or directly transported out of cells , reducing drug delivery efficiency and efficacy

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
  • Lipid-mixed poly (lactic-co-glycolic acid) (PLGA) nanoparticle having high drug loading amount and active targeting effect
  • Lipid-mixed poly (lactic-co-glycolic acid) (PLGA) nanoparticle having high drug loading amount and active targeting effect
  • Lipid-mixed poly (lactic-co-glycolic acid) (PLGA) nanoparticle having high drug loading amount and active targeting effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0015] In vivo and in vitro antitumor activity of doxorubicin-loaded lipid-mixed PLGA nanoparticles

[0016] 1 Objective: To evaluate the anti-tumor activity of DOX-loaded lipid-mixed PLGA nanoparticles through in vivo and in vitro experiments.

[0017] 2 Research methods:

[0018] 2.1 Determination of encapsulation efficiency and drug loading

[0019] Configure DMSO solutions of 0.1, 0.4, 1.0, 2.0, 5.0, 10.0, 15.0, and 25.0 μg / ml DOX, set the excitation wavelength of the fluorescence spectrophotometer to 470nm, and set the emission wavelength to 597nm, respectively measure the fluorescence intensity of the solution, and take the fluorescence intensity as The ordinate, the DOX concentration is the abscissa, and the standard curve is drawn. Weigh the DOX-loaded nanoparticles with a weight of M, dissolve them in 3ml DMSO, measure the fluorescence intensity, and calculate the DOX concentration C. The theoretical drug loading is the drug loading of 100% encapsulation of the dru...

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

No PUM Login to View More

Abstract

The invention provides a lipid-mixed poly (lactic-co-glycolic acid) (PLGA) nanoparticle having a high drug loading amount and an active targeting effect. The nanoparticle is of a core-shell structure, wherein the core is a poly (lactic-co-glycolic acid) (PLGA), and distearoyl-phosphatidylethanolamine-polyethylene glycol-folic acid and cholesterol-arginine-histidine methyl ester are embedded in the surface of the core. The nanoparticle disclosed by the invention can be used for remarkably improving the drug loading amount and the encapsulation efficiency of adriamycin, enhancing the cytotoxicity of the adriamycin to tumor cells and presenting a certain anti-multidrug resistance activity; the nanoparticles loaded with the adriamycin are mainly concentrated in tumor tissues after entering a body, so that the anti-tumor effect of the adriamycin is improved, and toxic and side effects are remarkably reduced; and a new strategy for the development of antitumor pharmaceutical preparations is provided.

Description

technical field [0001] The invention relates to a prescription composition and an application scheme of novel lipid-mixed polylactic acid-glycolic acid copolymer (PLGA) nanoparticles. Background technique [0002] Tumors seriously threaten human health. Doxorubicin (DOX) is a commonly used first-line chemotherapy drug with definite curative effect and low price. However, long-term use of doxorubicin is prone to drug resistance and side effects on normal tissues and organs, such as heart and kidney damage, bone marrow suppression, etc., which limit the further application of doxorubicin. Constructing a new tumor-targeted drug delivery system can increase the enrichment of doxorubicin in tumor tissues and reduce the distribution of doxorubicin in normal tissues, which can effectively improve the efficacy of doxorubicin and reduce the side effects. [0003] Nanoparticles can deliver small molecule drugs, vaccines and biomacromolecular drugs to some special organs or cells in v...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/34A61K47/28A61K31/704A61P35/00
Inventor 周四元滕增辉杜江波宦梦蕾成颖刘苗张邦乐
Owner FOURTH MILITARY MEDICAL UNIVERSITY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap 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