Lipid nano particles containing amphiphilic polymer and its preparing method

A technology of amphiphilic polymers and lipid nanoparticles, applied in medical preparations containing active ingredients, liposome delivery, pharmaceutical formulations, etc., can solve the problems of no discovery, reduced safety, etc., and achieve the retention time Prolonged, enhanced hydrophilicity, good sustained-release effect

Inactive Publication Date: 2007-04-11
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The amount of commonly used surfactants in these methods is about 1.5 times that of lipids, which reduces the safety of this type of preparation in clinical application
[0005] This patent is a related patent of Chinese patent 200610030517.0 (application number), and there is no report on the application of amphiphilic polymers such as polyethylene glycol-polyester to lipid nanoparticles in the literature search

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Components:

[0027] All-trans tretinoin 10mg

[0028] Glyceryl monostearate 400mg

[0029] Amphiphilic polymer 100mg

[0030] Tween 80 50mg

[0031] Soy Lecithin 250mg

[0032] Propylene glycol 0.2ml

[0033] water 15ml

[0034] The amphiphilic polymer refers to polyethylene glycol-polycaprolactone copolymer.

[0035] Described polyethylene glycol is monomethoxy polyethylene glycol ether.

[0036] The molecular weight of the amphiphilic polymer is as follows: the weight average molecular weight of polyethylene glycol is 2000, and the weight average molecular weight of polycaprolactone is 200.

[0037] Take all-trans retinoic acid, glyceryl monostearate, amphiphilic polymer, Tween 80, soybean lecithin, and propylene glycol in a 60°C water bath to melt and dissolve, and mix well, then add 60°C water, Stir to disperse evenly to obtain a concentrated microemulsion. Take another 10 times the amount of water and cool in an ice bath. The 60°C concentrated microemuls...

Embodiment 2

[0040] Components:

[0041] All-trans tretinoin 10mg

[0042] Stearic acid 200mg

[0043] Amphiphilic polymer 20mg

[0044] Sodium cholate 50mg

[0045] Dipalmitoylphosphatidylcholine 150mg

[0046] Macrogol 400 0.2ml

[0047] water 20ml

[0048] The amphiphilic polymer refers to polyethylene glycol-polycaprolactone lactide copolymer.

[0049] The polyethylene glycol is polyethylene glycol with hydroxyl groups at both ends.

[0050] The molecular weight of the amphiphilic polymer is as follows: the weight average molecular weight of polyethylene glycol is 5000, and the weight average molecular weight of polycaprolactone lactide copolymer is 600.

[0051] Take all-trans retinoic acid, stearic acid, amphiphilic polymer, sodium cholate, dipalmitoylphosphatidylcholine, and polyethylene glycol 400 in a 75°C water bath to melt and dissolve, mix well, add 75 ℃ water, stirring, so that the dispersion is uniform, and the preparation of a concentrated microemulsion. Take another ...

Embodiment 3

[0054] Components:

[0055] 9-nitrocamptothecin 1mg

[0056] Glyceryl Monopalmitate 100mg

[0057] Amphiphilic polymer 500mg

[0058] Hydrogenated egg yolk lecithin 100mg

[0059] Sodium Taurocholate 50mg

[0060] water 10ml

[0061] The amphiphilic polymer refers to polyethylene glycol-polylactide copolymer.

[0062] Described polyethylene glycol is monomethoxy polyethylene glycol ether.

[0063] The molecular weight of the amphiphilic polymer is as follows: the weight average molecular weight of polyethylene glycol is 6000, and the weight average molecular weight of polylactide is 4000.

[0064] Take 9-nitrocamptothecin, glyceryl monopalmitate, amphiphilic polymer, hydrogenated egg yolk lecithin, and sodium taurocholate in a 70°C water bath to melt and dissolve, and mix well, then add 70°C water , Stir to disperse evenly and obtain a concentrated microemulsion. Take another 50 times of water and cool in an ice bath. The 70°C concentrated microemulsion is slowly adde...

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PUM

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Abstract

A lipid nanometer pellet containing amphibious polymers and preparation belongs to the technological field of medicinal medication. In said invention, the percent scope between lipid of lipid nanometer pellet and amphibious polymers is from 10:1 to 1:5,the other components, including medicine, emulsifying agent, also including assistant for emulsifying agent might be added . Its preparation is,taking medicine, lipid, amphibious polymers, emulsifying agent assistant for emulsifying agent and putting into warm water till becoming solution, mixing evenly, adding warm water, mixing again and spreading evenly, thus to obtain concentrated micro emulsion. Taking slightly warm thereof and dropping slowly into ice bathing water adding while mixing, thus to obtain lipid nanometer pellet spreading in said water. Through ultra -filtering and getting rid of excessive water, adding freeze-dried protective agent or isotonic regulator for freezing and drying to prepare into freeze-dried powder injection.

Description

technical field [0001] The invention relates to a composition and a preparation method thereof, which belong to the technical field of pharmaceutical preparations, in particular to a lipid nanoparticle containing an amphiphilic polymer and a preparation method thereof. Background technique [0002] Lipid nanoparticle is a colloid drug delivery system with a particle size between 50 and 1000nm made by using solid or semisolid natural or synthetic lipids as carriers, encapsulating drugs in lipid cores through different methods. Compared with liposomes and microemulsions, drugs achieve better controlled and sustained release effects because they are encapsulated in the physiologically compatible framework of lipid nanoparticles. [0003] Amphiphilic polymers are obtained by copolymerization of polyethylene glycol and polyester. Among them, polyesters include polycaprolactone, polylactide, polylactide-glycolide copolymer, polycaprolactone-lactide copolymer, etc., because these ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/19A61K45/00
Inventor 任福正陈佳蕾景秋芳崔景斌沈永嘉
Owner EAST CHINA UNIV OF SCI & TECH
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