Invisible nano-liposome injection for encapsulating USPIO (Ultra-small Super Paramagnetic Iron Oxide) and preparation method and application thereof

A technology of nano-liposome and stealth liposome, applied in the field of medicine

Inactive Publication Date: 2014-07-02
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no literature report on a USPIO preparation with good target tissue selectivity in vivo, high distribution concentration in target tissue, and high MR imaging sensitivity. In one, nano-stealth liposomes that encapsulate USPIO and anti-tumor drugs are prepared at the same time, integrating tumor diagnosis and treatment, and improving the efficiency of tumor diagnosis and treatment

Method used

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  • Invisible nano-liposome injection for encapsulating USPIO (Ultra-small Super Paramagnetic Iron Oxide) and preparation method and application thereof
  • Invisible nano-liposome injection for encapsulating USPIO (Ultra-small Super Paramagnetic Iron Oxide) and preparation method and application thereof
  • Invisible nano-liposome injection for encapsulating USPIO (Ultra-small Super Paramagnetic Iron Oxide) and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Embodiment 1: Adriamycin Hydrochloride Stealth Liposome Intravenous Injection Encapsulating USPIO

[0081] Composed of:

[0082]Soy lecithin 500mg, phosphatidylethanolamine 100mg, cholesterol 300mg, polyethylene glycol-distearoylphosphatidylethanolamine 100mg, USPIO 15mL, doxorubicin hydrochloride 100mg.

[0083] Preparation:

[0084] Take the USPIO solution and mix it with a phosphate buffer solution with pH=6, add 300 mg of sodium periodate, mix and oxidize for 30 min, add 200 mg of ethylene glycol to terminate the reaction, and pass through a Sephadex-G25 column for desalting and purification. Dissolve soybean lecithin, phosphatidylethanolamine, cholesterol, and polyethylene glycol-distearoylphosphatidylethanolamine in 30 mL of chloroform according to the above ratio, and put it in a rotary evaporator at 37°C for 40 minutes to remove the organic solvent to obtain lipid Plasma membrane; add USPIO solution to it and vortex for 20min, continue to add 20mL of phosphate...

Embodiment 2

[0085] Embodiment 2: Adriamycin Hydrochloride Stealth Liposome Intravenous Injection Encapsulating USPIO

[0086] Composed of:

[0087] Yolk lecithin 500mg, phosphatidylethanolamine 100mg, dioleoylphosphatidylethanolamine 100mg, cholesterol 400mg, polyethylene glycol-dipalmitoylphosphatidylcholine 150mg, USPIO 15mL, doxorubicin hydrochloride 100mg.

[0088] Preparation:

[0089] Take the USPIO solution and mix it with a phosphate buffer solution with pH=6, add 300 mg of sodium periodate, mix and oxidize for 30 min, add 200 mg of ethylene glycol to terminate the reaction, and pass through a Sephadex-G25 column for desalting and purification. Dissolve egg yolk lecithin, phosphatidylethanolamine, dioleoylphosphatidylethanolamine, cholesterol, polyethylene glycol-dipalmitoylphosphatidylcholine in 50mL of ether according to the above ratio, and put it in a rotary evaporator at 40°C. 30min, remove organic solvent to obtain lipid film; Add USPIO solution wherein and vortex 20min, c...

Embodiment 3

[0090] Embodiment 3: Adriamycin Hydrochloride Stealth Liposome Intravenous Injection Encapsulating USPIO

[0091] Composed of:

[0092] Egg yolk lecithin 300mg, hydrogenated soybean lecithin 300mg, dimyristoyl phosphatidylethanolamine 150mg, cholesterol 400mg, polyethylene glycol-polyglycolide lactide 150mg, USPIO 20mL, doxorubicin hydrochloride 100mg.

[0093] Preparation:

[0094] Take the USPIO solution and mix it with pH=6 phosphate buffer, add 300 mg of sodium periodate, mix and oxidize for 40 min, add 300 mg of ethylene glycol to terminate the reaction, and pass through a Sephadex-G25 column for desalting and purification. Dissolve egg yolk lecithin, hydrogenated soybean lecithin, dimyristoyl phosphatidylethanolamine, cholesterol, polyethylene glycol-polyglycolide lactide in 30 mL of chloroform according to the above ratio, and put it in a rotary evaporator at 37 °C Rotary steam for 40 minutes, remove the organic solvent to obtain a lipid film; add USPIO solution to it...

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Abstract

The invention relates to the technical field of medicine. At present, a USPIO (Ultra-small Super Paramagnetic Iron Oxide) preparation which has high in-vivo target tissue selectivity, high target tissue distribution concentration and high MR (Magnetic Resonance) imaging sensitivity is not reported. A stable and effective invisible nano-liposome preparation is prepared by taking an invisible nano-liposome as a vector, combining MR diagnosis with treatment and carrying USPIO and an anti-tumor medicament simultaneously. Due to the adoption of the invisible nano-liposome injection preparation serving as an MR contrast agent, the in-vivo tissue selectivity of the USPIO can be increased, the sensitivity is increased, and early diagnosis of diseases is facilitated; meanwhile, the invisible nano-liposome injection preparation is taken as a means for evaluating the curative effect of tumor therapy, so that the curative effect of tumor chemotherapy is monitored in real time, overtreatment of a patient is reduced, toxic and side effects are reduced, and the curative effect of tumor chemotherapy is improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a stealth nanoliposome injection encapsulating USPIO, a preparation method and application thereof. Background technique [0002] At present, tumor is still one of the causes of the highest mortality in the world, and about 10 million people develop tumor every year, and the treatment of tumor is currently mainly a combination of surgery, radiotherapy and chemotherapy. Although about 90 chemotherapeutic drugs have been approved by the US FDA for clinical treatment of cancer, the use of chemotherapeutic drugs is severely limited due to their toxic side effects and excessive damage to patients. These toxic side effects are mainly due to poor targeting and individualization of chemotherapy drugs. With the gradual understanding of the mechanism of tumor occurrence and development, the "heterogeneity" of tumors is gradually recognized. The same type of tumor may have different molec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/18A61K9/127A61K9/10A61K45/00A61K31/704A61K31/337A61K31/352A61P35/00
Inventor 邓莉陈建明柯兴发何志颖丛锐军张佳良王鹏龙
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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