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A stealthy brain-targeted triptolide nanoliposome and its preparation method

A technology of nanoliposome and triptolide, applied in the field of medicine, can solve the problems of large side effects, multi-organ toxicity and limited clinical application, etc., and achieves the effects of high encapsulation rate, good repeatability and simple detection operation.

Active Publication Date: 2021-02-23
深圳市锦泰医药科技合伙企业有限合伙 +1
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Problems solved by technology

[0008] Senile dementia cannot be cured at present, and the existing therapeutic drugs can only temporarily relieve the symptoms of AD, and the side effects are large; in the prior art, there is no combination of the active ingredient triptolide of natural Chinese medicine and modern advanced drug-loading technology to prepare a drug with cerebral palsy. Targeted stealth nanoliposomes are used in the prevention and treatment of AD; and TP is widely distributed in the body, resulting in multi-organ toxicity that limits its clinical application

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  • A stealthy brain-targeted triptolide nanoliposome and its preparation method
  • A stealthy brain-targeted triptolide nanoliposome and its preparation method
  • A stealthy brain-targeted triptolide nanoliposome and its preparation method

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preparation example Construction

[0059] The embodiment of the present invention provides a preparation method of invisible triptolide nanoliposome PEG-TP, including: selective film dispersion-ultrasonic method; phospholipid / cholesterol ratio of 2:1; chloroform dosage of 20ml; drug loading temperature 40 ℃; drug loading time is 60min; drug-to-lipid ratio is l:50.

[0060] The preparation method of the stealth triptolide nanoliposome PEG-TP adopts thin film distribution-ultrasonic method, specifically comprising:

[0061] According to the mass ratio of HSPC: Chol: DSPE-PEG2000 = 4: 2: 1, respectively weigh hydrogenated soybean lecithin, cholesterol, polyethylene glycol 2000-distearoylphosphatidylethanolamine as the membrane material for preparing liposomes, and Triptolide that is 1 / 50 of the total mass of phospholipids;

[0062] Dissolve in 20ml of chloroform / methanol mixed solvent with a volume ratio of 2 / 1; place the mixed solvent in a 100ml ground-mouthed round bottom flask, and evaporate under reduced pres...

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Abstract

The invention belongs to the technical field of medicine, and discloses a stealthy brain-targeted triptolide nano-liposome and a preparation method thereof. The nano-triptolide liposome is used as a drug carrier; polyethylene glycol PEG is used for stealth Stealthized triptolide nano-liposomes were prepared by chemical modification; the brain-targeting ligand Lf was connected to the surface of PEG-TP nano-liposomes by covalent coupling method to prepare stealthy brain-targeted triptolide nano-liposomes. Liposomes. Through the optimization of the preparation process, the present invention successfully prepared stealth brain-targeted triptolide nanoliposomes with uniform particle size distribution, high encapsulation efficiency and good stability, and the relevant results have not been reported in the literature; the prepared The average particle diameter of Lf‑PEG‑TP nano liposomes is 105.98±2.65nm, the encapsulation efficiency is 55.96±2.13%, and the Lf even percentage is 79.26±3.57%.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a stealthy brain-targeted triptolide nano-liposome and a preparation method thereof. Background technique [0002] Alzheimer's disease (AD) is the most common degenerative disease of the central nervous system, characterized by progressive memory loss, cognitive impairment, and personality changes. The cause of death ranks fourth after cardiovascular disease, cerebrovascular disease and malignant tumors. According to the "World Alzheimer's Disease Report 2015", there are about 46.8 million dementia patients in the world, and 9.9 million new cases are newly diagnosed every year (1 new case is added every 3 seconds in the world); billion to $818 billion in 2015, an increase of 35.4%, and AD has become one of the biggest global public health and social care challenges facing humanity today and in the future. The number of patients with Alzheimer's disease in China ran...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/64A61K47/60A61K31/585A61P25/28G01N30/02
CPCA61K31/585G01N30/02
Inventor 吴正治王林
Owner 深圳市锦泰医药科技合伙企业有限合伙
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