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Invisible brain-targeted triptolide nano-liposome and 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 achieve the effects of high encapsulation rate, good repeatability and high precision

Active Publication Date: 2018-04-13
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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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 The temperature is 40°C; the drug loading time is 60min; the drug-to-lipid ratio is 1:50.

[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 e...

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Abstract

The invention belongs to the technical field of medicines and discloses invisible brain-targeted triptolide nano-liposome and a preparation method. The preparation method comprises the following steps: using nano triptolide lipidosome as a medicine carrier, and performing invisibility modification on the medicine carrier by using polyethylene glycol PEG (Polyethylene Glycol), so as to obtain invisible triptolide nano-liposome; connecting brain-targeted ligand Lf with the surface of the PET-TP nano-liposome by adopting a covalent coupling method, thereby obtaining the invisible brain-targeted triptolide nano-liposome. Through optimization of preparation processes, the invisible brain-targeted triptolide nano-liposome which is uniform in particle size distribution, relatively high in packaging rate and good in stability is successfully prepared, and related results are not available in document reports; the average particle size of the prepared Lf-PEG-TP nano-liposome is 105.98+ / -2.65nm,the packaging rate of the nano-liposome is 55.96+ / -2.13%, and the Lf coupling percentage of the nano-liposome 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 Applications(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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