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Functional nano-carrier with escape capability of lysosome and preparation method of same

A lipid nanocarrier and functional technology, applied in the field of pharmaceutical preparations, can solve the problems of narrow application range of lysosome escape method, inability to be extended to other nanocarriers, etc., and achieve the effect of simple construction method and wide application range.

Inactive Publication Date: 2013-07-10
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to solve the shortcomings of the current lysosome escape method, which has a narrow application range and cannot be extended to other nanocarriers, and provide a method for constructing a nanocarrier with lysosome destructive ability with wide application value, so as to prevent it from being destroyed or degradation, to protect the active substance to reach the target and exert its efficacy

Method used

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  • Functional nano-carrier with escape capability of lysosome and preparation method of same
  • Functional nano-carrier with escape capability of lysosome and preparation method of same
  • Functional nano-carrier with escape capability of lysosome and preparation method of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Preparation of functional drug-loaded lipid nanocarriers

[0057] Weigh 4mg of paclitaxel, 1mg of decanyl arginine, 75mg of phospholipids, and 25mg of medium-chain fatty acid glycerides, dissolve in 3mL of methanol, evaporate under reduced pressure in a 37°C water bath to form a film, and add 2.3mg / mL of bovine serum albumin aqueous solution 4mL, hydrated for 15min, sonicated with an ice bath probe (200w×300 times), squeezed through a 0.22μm microporous filter membrane, and obtained a functional drug-loaded lipid nanocarrier with an average particle size of 80-100nm and an encapsulation efficiency of 98.6%. .

Embodiment 3

[0061] Preparation of functional drug-loaded liposomes

[0062] Weigh 5 mg of doxorubicin, 2 mg of lauryl arginine, and 100 mg of phospholipids, dissolve them in 3 mL of ethanol, slowly drop them into 5 mL of distilled water while ultrasonicating, evaporate the ethanol under reduced pressure, and ultrasonicate with an ice-bath probe (200w×300 times) , extruding through a 0.22 μm microporous membrane to prepare functional drug-loaded liposomes with an average particle size of 60-80 nm and an encapsulation efficiency of 97.9%.

Embodiment 4

[0064] Weigh 100 mg of phospholipid, 5 mg of lauryl arginine and dissolve in 6 mL of ether, weigh 4 mg of mitoxantrone and dissolve in 2 mL of distilled water, slowly add to the ether solution while ultrasonicating to form a water-in-oil emulsion, evaporate under reduced pressure to Invert the phase to become an oil-in-water emulsion, add 2mL of distilled water, continue to evaporate under reduced pressure to remove ether, and replenish water to 4mL, ultrasonically (200w×300 times) with an ice-bath probe, squeeze through a 0.22μm microporous filter membrane, and dextran gel The column removes free mitoxantrone to prepare liposomes with a particle size of 60-80nm and an encapsulation efficiency of 99.2%.

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Abstract

The invention relates to the field of pharmaceutical preparation and the technical field of biological medicine, and particularly relates to a functional nano-carrier with a escape capability of lysosome and a preparation method of same. The functional nano-carrier is characterized in that the functional nano-carrier comprises arginine alkyl alcohol ester, medicament, carrier material and water. The functional nano-carrier has intense destructive effect on biological films in the condition of low pH value, so that the functional nano-carrier can rapidly destroy lysosome films in the conditionof acidic condition and rapidly escape into cytoplasm, is prevented from being destroyed by various enzymes and acid environment in lysosome, and is good for the exerting of the drug efficacy.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations and the field of biomedicine technology, in particular to a lysosome disrupting agent and a drug-loaded nanocarrier with lysosome disrupting ability constructed on the basis thereof. Background technique [0002] Nano drug delivery systems including liposomes, micelles, lipid nanocarriers, nanoparticles, etc. have been extensively studied in recent years. Most of the nanocarriers are endocytosed into the cells through the endosome-lysosome pathway, and the lysosome is an acidic environment with a pH of 5-6, and contains a large number of enzymes, which will lead to the degradation and destruction of the endocytosis, thereby Lead to the inactivation of the loaded drug (SahayG, AlakhovaDY, KabanovAV. Endocytosis of nanomedicines. Journal of Controlled Release 2010, 145: 182-195.). Therefore, it is necessary to take necessary measures to allow the nanocarriers to quickly escape from the ly...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/16A61K47/24A61K47/36A61K9/00A61K9/127A61K9/14
Inventor 平其能李赛张灿肖衍宇苏志桂
Owner CHINA PHARM UNIV
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