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Targeting ginkgolide B solid lipid nanoparticle and preparation method thereof

A technology of solid lipid nanometer and ginkgolide, which is applied in the field of medicine, can solve the problems such as the inability of effective treatment of brain diseases, and achieve the effects of strong affinity, prolonging circulation time and treating brain diseases.

Inactive Publication Date: 2012-07-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the problem that the drug cannot enter the brain tissue due to the resistance of the blood-brain barrier to exogenous substances, so that brain diseases cannot be effectively treated, the invention designs a drug-loaded solid lipid modified by folic acid targeting materials Nanoparticles, using folic acid receptors on the surface of brain endothelial cells to specifically recognize folic acid ligands and receptor-mediated phagocytosis, and lipid nanoparticle materials have strong affinity with brain cell membranes and nanoparticle phagocytosis and transmembrane pathways to help drug-loaded solids Lipid nanoparticles effectively enter the brain to exert drug effects

Method used

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  • Targeting ginkgolide B solid lipid nanoparticle and preparation method thereof
  • Targeting ginkgolide B solid lipid nanoparticle and preparation method thereof
  • Targeting ginkgolide B solid lipid nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Synthesis of FA-Pluronic F68: (1) 1.15 g of p-toluenesulfonyl chloride (TsCl) and 800 μl of triethylamine were placed in a three-necked flask, and an appropriate amount of anhydrous dichloromethane was added to dissolve. The methylene chloride solution in which 5.00 g of Pluronic F68 is dissolved is added dropwise, and the reaction is magnetically stirred for 12 hours under nitrogen protection at room temperature. After the product is concentrated, it is precipitated in an appropriate amount of ice ether, and filtered with suction to obtain a precipitate. The precipitate was dissolved twice, and the precipitate was dried under vacuum for 24 hours to obtain F68-OTs. (2) Take 0.91 g of potassium phthalimide (PI) and place it in a three-necked flask, add an appropriate amount of anhydrous N,N-dimethylformamide (DMF), stir, disperse and dissolve at 120°C; drip into it Add 4.00g of F68-OTs in DMF solution, react at 120°C under nitrogen protection for 6 hours. After the prod...

Embodiment 2

[0028] Preparation of targeted ginkgolide B solid lipid nanoparticles: Take 150mg of glycerol monostearate and 30mg FA-Pluronic F68 in a water bath and heat it to 60℃ to melt, and gradually add 7.5mg of ginkgolide B in methanol solution. , Keep 60℃, magnetically stir for 2h, make the medicine and lipid material mix uniformly, until the methanol evaporates. Add 15ml of an aqueous solution of 45mg Pluronic F68 heated to 60°C, magnetically stir for 2h to obtain colostrum, disperse the colostrum at a high speed of 7500r / min at 60°C for 6min, immediately place it in an ice water bath at 4°C, solidify for 5min, and extrude over 0.8μm Filter the membrane for 5 times to obtain a solid lipid nanoparticle solution targeting ginkgolide B. The particle size is 125.8nm and the polydispersity coefficient is 0.380.

Embodiment 3

[0030] Preparation of targeted ginkgolide B solid lipid nanoparticles: Take 150mg of glycerol monostearate and 30mg FA-Pluronic F68 in a water bath and heat to 80 degrees Celsius to melt, and gradually add 7.5mg of ginkgolide B in methanol solution. , Keep at 80℃, magnetically stir for 2h, make the medicine and lipid material mix uniformly, until the methanol evaporates. Add 15ml of an aqueous solution of 45mg Pluronic F68 heated to 80°C, magnetically stir for 2h to obtain colostrum, 80°C, 7500r / min high-speed dispersion of colostrum for 6min, immediately place it in an ice water bath at 4°C, solidify for 5min, and squeeze 0.8μm Filter the membrane for 5 times to obtain a solid lipid nanoparticle solution targeting ginkgolide B. The particle size is 125.4nm and the polydispersity coefficient is 0.319.

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Abstract

The invention discloses a targeting ginkgolide B solid lipid nanoparticle and a preparation method thereof. The ginkgolide B solid lipid nanoparticle targeting a blood brain barrier is prepared with an oil-in-water emulsion process by taking a ginkgolide B as a treating medicament, taking a solid lipid material as a carrier, taking a folic acid-modified surfactant as a targeting material and taking a mixture obtained by mixing a surfactant with the folic acid-modified surfactant in a certain ratio as an emulsifier. The particle diameter is 80-200 nanometers, and the polydispersion coefficient is 0.30+ / -0.10. According to the solid lipid nanoparticle, a brain targeting effect is achieved by using the folic acid-mediated phagocytosis on the surfaces of brain cells and the phagocytosis way of adsorption of a brain cell membrane by using the nanoparticle.

Description

Technical field [0001] The invention belongs to the field of medicine, and specifically relates to a ginkgolide B solid lipid nanoparticle targeted to the blood-brain barrier and a preparation method thereof. Background technique [0002] Alzheimer's disease (AD) is a common chronic degenerative neurological disease in the elderly, with atrophy of brain tissue, especially loss of hippocampus and pre-basal neurons. Patients with Alzheimer’s disease have two major pathological characteristics: the formation of extracellular senile plaques (SP) with the core component of β-amyloid (Aβ), and the formation of intrafibrillary tangles in diseased neurons with hyperphosphorylated Tau protein as the main component Knots (NFTs). Pathologists speculate that the two pathological features eventually cause neuron / axonal disorder or axonal death, which leads to brain cell apoptosis and eventually dementia symptoms. Currently, there are only 5 drugs approved by the FDA and the European Agency ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/14A61K31/365A61K47/34A61P25/28
Inventor 栾立标胡娟
Owner CHINA PHARM UNIV
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