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Liposome able to transmit blood and brain screen, medicinal compositions using hiposome as carrier and its preparation method

A blood-brain barrier and liposome technology, applied in the field of medicine, can solve problems such as instability, unsuitability for filtration, and difficulty in obtaining uniform liposomes with bioavailability, so as to improve bioavailability and clinical indication range, good therapeutic effect

Inactive Publication Date: 2008-08-20
四环生物产业集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the liposomes obtained by these methods are not suitable for filtration, unstable, and cannot remove residual organic solvents well, and it is also difficult to obtain uniform liposomes suitable for injection and with good bioavailability

Method used

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  • Liposome able to transmit blood and brain screen, medicinal compositions using hiposome as carrier and its preparation method
  • Liposome able to transmit blood and brain screen, medicinal compositions using hiposome as carrier and its preparation method
  • Liposome able to transmit blood and brain screen, medicinal compositions using hiposome as carrier and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1: The liposome containing GM1 sodium salt is a carrier, and the pharmaceutical composition coated with NGF

[0052] Weigh various lipids according to the percentage of liposome molar content, DMPC 50%, CH 20%, GM1 sodium salt 10%, NPPE 20%, among them, DMPC, NPPE and CH were purchased from Lipoid Company, and GM1 sodium salt was purified by itself income. The liposomes were dissolved into a clear solution with 5 times the volume of solvent (chloroform:methanol, volume ratio 2:1). The above solution was placed in a rotary evaporating flask, and the solvent was evaporated to dryness under reduced pressure to form a lipid film attached to the wall of the evaporating flask. Take a flask containing a lipid film, fill it with nitrogen (the following operations will always be filled with nitrogen), add an organic solvent (ether) to a final concentration of lipids of 100 μm / ml, dissolve and become an organic phase solution. Nerve growth factor was taken and dissol...

Embodiment 2

[0053] Embodiment 2: The liposome containing GM1 sodium salt is a carrier, and the pharmaceutical composition coated with methylcobalamin

[0054] Weigh various lipids according to the percentage of liposome molar content, DMPC 50%, CH 30%, GM1 sodium salt 5%, NPPE 15%, among them, DMPC, NPPE and CH were purchased from Lipoid Company, and GM1 sodium salt was purified by itself income. The liposomes were dissolved into a clear solution with 7.5 times the volume of solvent (chloroform:methanol, volume ratio 1:1). The above solution was placed in a rotary evaporating flask, and the solvent was evaporated to dryness under reduced pressure to form a lipid film attached to the wall of the evaporating flask. Take a flask containing a lipid film, fill it with nitrogen (the following operations will always be filled with nitrogen), add an organic solvent (diethyl ether) until the final concentration of lipids is 100 μm / ml, and dissolve and become an organic phase solution. Take methy...

Embodiment 3

[0055] Embodiment 3: The liposome containing GM1 sodium salt is a carrier, and the pharmaceutical composition coated with citicoline sodium

[0056] Various lipids were weighed according to the percentage of liposome molar content, DMPC 60%, CH 10%, GM1 sodium salt 5%, NPPE 25%, among them, DMPC, NPPE and CH were purchased from Lipoid Company, and GM1 sodium salt was purified by itself The obtained solution was dissolved into a clear solution with a solvent (chloroform) 10 times the volume of the liposome. The above solution was placed in a rotary evaporating flask, and the solvent was evaporated to dryness under reduced pressure to form a lipid film attached to the wall of the evaporating flask. Take a flask containing a lipid film, fill it with nitrogen (the following operations will always be filled with nitrogen), add an organic solvent (tetrahydrofuran) to a final concentration of lipids of 100 μm / ml, dissolve and become an organic phase solution. Get citicoline sodium, ...

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Abstract

A liposome able to pass through blood brain barrier contains the blood brain barrier anchor site (5-15 mol %), the phosphatide with high phase-change temp, cholesterol and fusion aid. A composite medicine using said liposome as carrier for passing through blood brain barrier for treating the diseases in central nerve system and its preparing process are also disclosed.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to a liposome which can penetrate the blood-brain barrier, and also relates to a pharmaceutical composition using the liposome as a carrier and a preparation method thereof. It specifically relates to a liposome containing a blood-brain barrier anchor point, a pharmaceutical composition in which an effective amount of medicine for treating the central nervous system is coated with the liposome as a carrier, and a preparation method thereof. The pharmaceutical composition has longer blood circulation time and can actively penetrate the blood-brain barrier and enter the central nervous system to achieve the effect of treating central nervous system diseases. Background technique [0002] The blood-brain barrier (BBB) ​​is a barrier between blood and brain tissue formed by capillary endothelial cells. It provides a relatively stable internal environment for brain tissue and ensures the nor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/24A61P25/00
Inventor 陈亚李汝霖汤华东陈煌
Owner 四环生物产业集团有限公司
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