Nano-drug as well as preparation method and medical application thereof

A technology of nano-medicine, cholesterol, applied in the field of medicine

Active Publication Date: 2021-01-08
ACADEMY OF MILITARY MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most AChE reactivators contain quaternary ammonium groups and oxime groups. These two groups are not only necessary for reactivation, but also key groups that limit AChE reactivators from penetrating the BBB. Therefore, so far, by Structural modification or transformation has not been able to obtain a heavy activator with both good reactivation performance and good BBB penetration performance

Method used

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  • Nano-drug as well as preparation method and medical application thereof
  • Nano-drug as well as preparation method and medical application thereof
  • Nano-drug as well as preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] (1) Dissolve egg yolk lecithin, cholesterol, dioleoylphosphatidylserine (DOPS), distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) at a molar ratio of 36:20:20:4 In an organic solvent, a solution with a concentration of 10 mg / mL was obtained, and was rotated at 40°C at 120 rpm to remove the organic solvent to obtain a phospholipid film. The organic solvent was a mixture of chloroform and methanol with a volume ratio of 70:30;

[0089] (2) Dissolve 10 mg of bisphosphorus (LuH-6) in 1 mL of water to form an aqueous solution, dissolve the phospholipid film in the aqueous solution, the weight ratio of the aqueous solution to the phospholipid film is 1:10, and then mix at 25 ° C for 2 hours to obtain drug-loaded mixture;

[0090] (3) The modified transferrin receptor nucleic acid aptamer SEQ ID NO: 6, whose 5' end is modified with cholesterol to ensure that it can be inserted into the phospholipid hydrophobic layer, and the 3' end is modified with inv...

Embodiment 2

[0095] (1) Dissolve soybean lecithin, cholesterol, dipalmitoylphosphatidylserine (DPPS), distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) at a molar ratio of 45:20:10:5 In an organic solvent, a solution with a concentration of 20 mg / mL was obtained, and the phospholipid film was obtained by rotary evaporation at 40° C. at 150 rpm to remove the organic solvent. The organic solvent was a mixture of chloroform and methanol with a volume ratio of 50:50;

[0096] (2) Dissolve 20mg of bisphosphorus (LuH-6) in 1mL of water to form an aqueous solution, dissolve the phospholipid film in the aqueous solution, the weight ratio of the aqueous solution to the phospholipid film is 1:5, and then mix at 25°C for 3h to obtain drug-loaded mixture;

[0097] (3) The modified transferrin receptor nucleic acid aptamer SEQ ID NO: 6, whose 5' end is modified with cholesterol to ensure that the nucleic acid can be inserted into the phospholipid hydrophobic layer, and the 3' e...

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Abstract

The invention belongs to the field of medicine, and particularly relates to a nano-drug. The nano-drug comprises liposome and cholesterol molecule modified aptamer; the cholesterol molecule modified on the aptamer is partially inserted into the liposome, the aptamer is the aptamer of a transferrin receptor, and an acetylcholinesterase heavy activator is wrapped in the liposome, wherein the molar ratio of the liposome to the cholesterol molecule modified aptamer is (5-150): 1; the liposome comprises the following components in parts by molar weight of 25-120 parts of phospholipid, 0.5-30 partsof distearoyl phosphatidyl ethanolamine-polyethylene glycol and 3-45 parts of cholesterol. The invention also relates to the preparation method and application of the nano-drug. The nano-drug disclosed by the invention can be specifically combined with the surface of BBB, effectively penetrates through a blood-brain barrier and releases the drug in the center, and the nano-drug is high in drug loading capacity, good in biocompatibility, high in bioavailability and free of cytotoxicity, and can be used for military protection for treating organophosphorus pesticide poisoning and nerve poisoningagent attack.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a nano-medicine, a preparation method and a medical application of the nano-medicine. Background technique [0002] Organophosphorus (OP) is one of the most toxic chemical agents, and it is also the main component of organophosphorus pesticides and nerve agents. About three million people in the world are poisoned every year due to exposure to OP, which poses a serious threat to human health and even life safety. When OP enters the body, it will quickly inhibit the central and peripheral acetylcholinesterase (AChE) activity, making it lose the ability to hydrolyze acetylcholine (ACh), causing convulsions, convulsions, respiratory depression and other poisoning symptoms, and eventually leading to rapid death or severe, Irreversible brain damage. At present, the main organophosphorus poisons include paraoxon, parathion, soman, sarin, tabun and Novichok. In order to treat OP p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/54A61P25/00A61P39/02B82Y5/00B82Y30/00B82Y40/00A61K31/444A61K31/4425
CPCA61K47/6911A61K47/549A61P39/02A61P25/00B82Y5/00B82Y30/00B82Y40/00A61K31/444A61K31/4425
Inventor 全东琴王永安张亚丹申辽王涛
Owner ACADEMY OF MILITARY MEDICAL SCI
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