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Nanoparticles modified with polyethylene glycol vitamin E succinate and calreticulin and preparation method thereof

A technology of succinate and polyethylene glycol, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pharmaceutical formulations, etc., can solve limitations, small molecular weight of phospholipids, and insufficient stability of nano-formulations, etc. problem, to achieve the effect of enhanced targeting, improved stability, small changes in particle size and polydispersity coefficient

Inactive Publication Date: 2015-11-25
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the molecular weight of phospholipids is small, and the stability of the formed nano-preparation is not enough, which is greatly limited in the application of long-circulation, sustained-release, absorption and targeting materials.

Method used

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  • Nanoparticles modified with polyethylene glycol vitamin E succinate and calreticulin and preparation method thereof
  • Nanoparticles modified with polyethylene glycol vitamin E succinate and calreticulin and preparation method thereof
  • Nanoparticles modified with polyethylene glycol vitamin E succinate and calreticulin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Prescription: 1mg betulinic acid, 20mg soybean lecithin, 2mg sophorolipid, 1mg calreticulin, 5mg polyethylene glycol vitamin E succinate.

[0020] Preparation Process:

[0021] (1) dissolve betulinic acid, soybean lecithin and sophorolipid with 10ml ethanol;

[0022] (2) Ethanol was removed by vacuum rotary evaporation, and vacuum-dried for 4 hours to obtain a dry film;

[0023] (3) Dissolve polyethylene glycol vitamin E succinate and calprotectin in 10 ml of pure water, and add them to the dry film to fully dissolve the film;

[0024] (4) Filtrate through a 0.22 μm microporous membrane to obtain the product.

Embodiment 2

[0026] Prescription: 1mg morin, 40mg soybean lecithin, 4mg sophorolipids, 2mg calreticulin, 10mg polyethylene glycol vitamin E succinate.

[0027] Preparation Process:

[0028] (1) dissolve morin, soybean lecithin and sophorolipid with 10ml ethanol;

[0029] (2) Ethanol was removed by vacuum rotary evaporation, and vacuum-dried for 8 hours to obtain a dry film;

[0030] (3) Dissolve polyethylene glycol vitamin E succinate and calprotectin in 10 ml of pure water, and add them to the dry film to fully dissolve the film;

[0031] (4) Filtrate through a 0.22 μm microporous membrane to obtain the product.

Embodiment 3

[0033] Prescription: 1mg paclitaxel, 30mg egg yolk lecithin, 3mg sophorolipids, 1.5mg calreticulin, 8mg polyethylene glycol vitamin E succinate.

[0034] Preparation Process:

[0035] (1) Mix paclitaxel, egg yolk lecithin and sophorolipid, add 10ml ethanol to dissolve;

[0036] (2) Ethanol was removed by vacuum rotary evaporation, and vacuum-dried for 6 hours to obtain a dry film;

[0037] (3) Dissolve polyethylene glycol vitamin E succinate and calprotectin in 10 ml of pure water, and add them to the dry film to fully dissolve the film;

[0038] (4) Filtrate through a 0.22 μm microporous membrane to obtain the product.

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Abstract

The invention discloses polyethylene glycol vitamin E succinate and calprotectin modified nanoparticle and a preparation method thereof. The polyethylene glycol vitamin E succinate and calprotectin modified nanoparticle is prepared from the following raw materials in parts by weight: 1 part of active medicine, 20 to 40 parts of phospholipid, 2 to 4 parts of sophorolipid, 1 to 2 parts of calprotectin, and 5 to 10 parts of polyethylene glycol vitamin E succinate. Compared with the prior art, the nanoparticle modified by olyethylene glycol vitamin E succinate, sophorolipid and calprotectin has the advantages that (1) the preparation process is simple and controllable; (2) the stability of the nanoparticle is greatly improved, and the nanoparticle can be stabilized in a solution for up to 6 months; (3) a freeze-drying protective additive is not needed for freezing and drying; the obtained freeze-dried powder dissolved again shows small change on particle size and polydispersity index compared with freeze-dried powder without being dissolved; (4) the targeting for tumor cells is enhanced.

Description

technical field [0001] The invention relates to a nanoparticle and a preparation method thereof, in particular to a nanoparticle modified with polyethylene glycol vitamin E succinate and calreticulin and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] In pharmacy, nano-preparations include nanocapsules, nanospheres, lipid nanoparticles, liposomes, nanoemulsions and polymer micelles, etc., which are the hotspots of current pharmacy research. Due to the rising incidence of cancer and the low bioavailability and large side effects of most anti-tumor drugs, the nano drug delivery system has the advantages of improving drug targeting and reducing toxic and side effects, thus becoming the first choice for anti-tumor drug research. object. [0003] Phospholipids are commonly used materials for nano-preparations and are components of biological membranes. There are related decomposing enzymes in the organism, which ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K47/42A61K47/24A61K47/34A61K31/337A61K31/352A61K31/56A61P35/00
Inventor 吕慧侠郑立发张振海周建平
Owner CHINA PHARM UNIV
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