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Brain-targeted liposome containing cholinesterase heavy activator as well as preparation method and application of brain-targeted liposome

A cholinesterase and liposome preparation technology, applied in the field of medicine, can solve the problem of difficulty in reactivating cholinesterase, and achieve the effect of relieving symptoms of central poisoning

Active Publication Date: 2022-04-01
ACADEMY OF MILITARY MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The present invention aims to solve the problem that cholinesterase reactivators are difficult to penetrate the blood-brain barrier and enter the central nervous system

Method used

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  • Brain-targeted liposome containing cholinesterase heavy activator as well as preparation method and application of brain-targeted liposome
  • Brain-targeted liposome containing cholinesterase heavy activator as well as preparation method and application of brain-targeted liposome

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preparation example Construction

[0083] In other embodiments, the present invention provides a method for preparing brain-targeted liposomes containing a cholinesterase reactivator, comprising:

[0084] Add PBS to DSPE-PEG2K-MAL, and add RTB solution containing TCEP to prepare RTB-DSPE-PEG2K;

[0085] Add dichloromethane to egg yolk lecithin E80:cholesterol:DOPS:DSPE-mPEG2K with a mass ratio of 58:20:10:4, spin dry, add PAM solution to dissolve, then add RTB-DSPE-PEG2K and nucleic acid adapter Body, oscillating reaction, namely liposome. The obtained liposomes were characterized by particle size potential. The particle size of the liposome is between 130-160nm, and the zeta potential is between-53--29mV.

[0086] In other embodiments, the present invention provides a method for preparing brain-targeted liposomes containing a cholinesterase reactivator, comprising:

[0087] Add PBS to DSPE-PEG2K-MAL, and add RTB solution containing TCEP to prepare RTB-DSPE-PEG2K;

[0088] Cholesterol accounted for 20, DOPS...

Embodiment 1

[0116] Embodiment 1: the preparation of liposome

[0117] (1) Preparation of RTB-DSPE-PEG2K:

[0118] At room temperature, dilute TCEP (Alpha Aesar (China) Chemical Co., Ltd.) with PBS, shake and mix to obtain 10 mM TCEP solution. Add 8 μL of 10 mM TCEP solution to 0.8 mL of RTB aqueous solution (Vector Company, containing 1 mg of RTB per mL), and shake and react for 45 min in the dark. Add 1.2mL PBS buffer (Gibco, USA) to 68.46mg DSPE-PEG2K-MAL (Xi'an Ruixi Biotechnology Co., Ltd.), shake and mix well, add the RTB solution containing TCEP after the above reaction, and shake for 24 hours in the dark , to produce RTB-DSPE-PEG2K.

[0119] (2) Preparation of liposomes

[0120] At room temperature, dichloromethane (5 mL) was added to a mixture of egg yolk lecithin E80, cholesterol, DOPS, and DSPE-mPEG2K in a mass ratio of 60:20:10:4 (wherein the mass of DSPE-mPEG2K was 0.4 mg) to dissolve, After drying by rotary evaporation, add 0.5mL 2mg / mL PAM solution (PBS as solvent) to di...

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Abstract

The invention relates to a brain-targeted liposome containing a cholinesterase heavy activator as well as a preparation method and application of the brain-targeted liposome, in particular to a cholinesterase heavy activator liposome preparation which is a phytolectin / nucleic acid aptamer dual-targeted liposome with a long-circulation function. The drug can realize central targeted delivery of cholinesterase heavy activators, can be used for emergency treatment during organophosphorus poisoning, and especially can relieve symptoms of central poisoning.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a brain-targeted liposome containing a cholinesterase reactivator, a preparation method and application thereof. Background technique [0002] At present, cholinesterase reactivator is a specific antidote for organophosphate poisoning, mainly used for the rescue of moderate and severe organophosphate poisoning, and can fundamentally restore the activity of acetylcholinesterase, thereby maintaining the function of the cholinergic nervous system normal. However, cholinesterase reactivators are mostly quaternary ammonium salts, which are highly hydrophilic and difficult to pass through the blood-brain barrier. They cannot reverse the activity of acetylcholinesterase in the central nervous system, and thus have poor effects on fatal central poisoning symptoms. [0003] Therefore, making the cholinesterase reactivator penetrate the blood-brain barrier and enter the central nervous system is t...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/64A61K47/54A61K31/4425A61P39/02
CPCY02A50/30
Inventor 申辽蔡啟梅王永安全东琴冯数橙王涛
Owner ACADEMY OF MILITARY MEDICAL SCI
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