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High-entrapment efficiency long-acting nerve growth factor liposome and preparation method thereof

A liposome preparation and liposome technology are applied in the field of high encapsulation rate and long-acting nerve growth factor liposomes, which can solve the problems of difficulty in encapsulating liposomes, NGF water-soluble and easy to leak, etc., so as to improve the encapsulation efficiency. rate, improving in vivo stability, and the effect of improving stability

Inactive Publication Date: 2012-06-06
陈春园 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] There are also a large number of research papers and patents at home and abroad to encapsulate peptide drugs in liposomes to achieve the effect of improving in vivo stability, but the molecular weight of the peptides is limited to below 10KD, while the molecular weight of the commonly used β-NGF (2.5SNGF) It is 26KD, and because of its water solubility, it is difficult to encapsulate it into liposomes, and the encapsulated NGF is also easy to leak due to its water solubility

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0034] Weigh 400mg of lecithin, 80mg of cholesterol, 108mg of DSPE-PEG, 108mg of DSPE-PEG-Mal and dissolve in 10-20ml of chloroform solution to obtain a liposomal liquid. Rotate evaporation in a water bath at 55°C to make a uniform film, and continue to depressurize at 55°C Evaporated for 30 min to remove the chloroform to obtain a thick gum.

[0035] Add an appropriate amount of ammonium sulfate solution (123mmol / L pH5.4), cool in a water bath and ultrasonically elute for 20 minutes, add NGF to the obtained liposome suspension, the amount is equivalent to 1-1 / 4 of the molar number of DSPE-PEG-Mal, room temperature Incubate for 4-10 hours.

[0036] The NGF reaction rate was 74%, the average particle size was 140nm, and VC=0.590.

[0037] After passing through the membrane, liposomes with different particle size ranges can be obtained.

[0038] The upper column separates free NGF, and the encapsulation rate of the finished product can be higher without leakage.

example 2

[0040] The molar ratio of DSPE-PEG-SC to NGF was 3:1, dissolved in pH7.5 HEPES [N-(2-hydroxyethyl)piperazine-N-2-ethanesulfonic acid] buffer, and the former was added dropwise to the latter buffer, stirred gently at 4°C for 4 hours, purified by dialysis and then freeze-dried to obtain DSPE-PEG-NGF. Using DSPE-PEG-NGF as a part of the membrane material, liposomes were prepared using Example 1 or other conventional methods.

example 3

[0042] Prepare common long-circulation liposomes not containing active fat by the method of Example 1, prepare DSPE-PEG-NGF by the method of Example 2, mix and incubate the two, utilize the hydrophobicity of the latter to insert in the bimolecular layer of the former liposome.

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PUM

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Abstract

The invention relates to a high-entrapment efficiency long-acting nerve growth factor (NGF) liposome, belonging to the technical field of protein polypeptide drugs. The invention further discloses a preparation method of the high-entrapment efficiency long-acting nerve growth factor liposome, characterized by bonding NGF and an active membrane material of the liposome and then using a routine method and using the bonded material and other liposome components to prepare a long-circulating liposome. According to the invention, by bonding -SH, -NH2 in NGF molecules with the special active membrane material, that is, active lipid of the liposome, the entrapment efficiency is greatly increased, the internal stability is raised under the protection of long-chain PEG in the active lipid, and the key problem of the NGF application is solved.

Description

technical field [0001] The invention relates to a long-acting nerve growth factor liposome with high encapsulation rate, and belongs to the technical field of protein and polypeptide drugs. Background technique [0002] Nerve Growth Factor (NGF) is one of the most important biologically active substances in the human nervous system. It has been proven to have dual functions of promoting neurite growth and nourishing nerves, and can significantly repair central and peripheral nervous system damage. Two foreign scientists (Levi-Montaleini and S. Cohen) won the Nobel Prize in Medicine in 1986 for their discovery and purification of NGF. NGF has three subunits (αβγ). Currently, NGF usually refers to the β subunit with biological activity. According to the sedimentation coefficient, it is also called 2.5S NGF, with a molecular weight of 26KD and an isoelectric point of 9.3. It consists of two identical single chains containing 118 amino acids composition. [0003] In 2001, my c...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K38/18A61K47/34A61P25/00
Inventor 陈春园陈春在陈骐于彬
Owner 陈春园
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