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Macromolecular phosphatidylglycerol nanoliposome, and preparation methods and applications thereof

A technology of molecular phosphatidylglycerol and nano-liposomes, which is applied in liposome delivery, preparations for in vivo tests, medical preparations of non-active ingredients, etc., can solve the problems of high cytotoxicity and unstable characteristics, The requirements for the conditions are not high, the preparation process is simple and easy, and the effect of meeting the needs of magnetic targeting

Inactive Publication Date: 2014-02-12
SHANGHAI SENNA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, cationic polymer liposomes still have many disadvantages, such as unstable properties in saline solution caused by high cytotoxicity and high positive charge, so it is necessary to develop a more stable and low-toxic polymer liposome. liposome system

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: the preparation of phosphatidylglycerol chitosan

[0029] Dissolve 100 mg of phosphatidylglycerol (PG) in 50 mL of DMSO, blend in 50 mL of borate buffer solution with pH=6, add 4.0 mg of zinc tetrafluoroborate as a catalyst, and then add tissue cross-linking agent Denacol EX521 (mass concentration 1% -50%) solution 10ml, stirred and reacted for 24 hours, extracted and collected the reaction product epoxide-modified PG; reacted epoxide-modified PG with oxycarboxymethyl chitosan in pH=6 boric acid buffer 24 hours, lyophilized after dialysis for 48 hours to obtain phosphatidylglycerol chitosan.

Embodiment 2

[0030] Example 2: This example discusses the effect of different ratios of phosphatidylglycerol chitosan and cholesterol on the particle size of macromolecular phosphatidylglycerol nanoliposomes when the reverse evaporation method is used.

[0031]Co-dissolve phosphatidylglycerol chitosan (with a weight average molecular weight of 20,000) and cholesterol in dichloromethane in different proportions, and mix well to obtain solution I; prepare deionized aqueous solution II, wherein the ratio of solution I to solution II is 1:2; After mixing the two solutions, fully ultrasonic emulsification, and distilled off the dichloromethane under reduced pressure on a rotary evaporator to obtain a macromolecular phosphatidylglycerol nanoliposome solution. As can be seen from Table 1, adjusting the mass ratio of phosphatidylglycerol chitosan and cholesterol can obtain macromolecular phosphatidylglycerol nanoliposomes of different particle sizes, and the macromolecular phosphatidylglycerol nano...

Embodiment 3

[0032] Embodiment 3: This embodiment is a discussion on the use of macromolecular phosphatidylglycerol nanoliposomes to entrap water-soluble substances using the film dispersion method.

[0033] Weigh 15 mg of phosphatidylglycerol chitosan (weight average molecular weight 2000), 12 mg of cholesterol, dissolve in 3 ml of dichloromethane, oscillate evenly to obtain solution I, then put it into an eggplant-shaped bottle, and distill under reduced pressure on a rotary evaporator , and nitrogen was introduced from time to time until the dichloromethane was completely volatilized, and then vacuum-dried at room temperature for 24 hours; weighed 3.0mg vincristine and dissolved it in 5ml PBS (pH=7.4) buffer solution, and shaken to fully dissolve vincristine to obtain Aqueous solution II; then add the above-mentioned 5.0ml vincristine solution II into an eggplant-shaped bottle, and allow the lipid film to be fully hydrated under ultrasonic conditions. After ultrasonication for 10 minutes...

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Abstract

The invention discloses a macromolecular phosphatidylglycerol nanoliposome, and preparation methods and applications thereof, and belongs to liposome preparation and application technologies. The phosphatidylglycerol nanoliposome is vesicles having a bilayer lipid membrane structure prepared by using phosphatidylglycerol chitosan to substitute phosphatide as a primary membrane material. The phosphatidylglycerol chitosan has a weight average molecular weight of above 2000, can be dissolved in organic solvents comprising chloroform, ethanol and the like, and contains a carboxyl or amino group. The preparation methods of the nanoliposome adopt common liposome preparation methods comprising a membrane dispersion method and an inverted evaporation method. The surface of like liposomes can be connected with a plurality of targeting preparations, and can simultaneously and respectively entrap water-soluble, oil-soluble or amphiphilic substances comprising medicines, proteins, genes, nutrients, vitamins, magnetic particles, quantum dots and the like. The methods have the advantages of high entrapment rate, simple operation, strong applicability and low cost, and the dressed macromolecular liposome has the advantages of uniform particle size distribution, adjustability in a range of 10-5000nm, stable system and strong slow release function.

Description

technical field [0001] The invention relates to the preparation and application of a macromolecular phosphatidylglycerol nano-liposome. The invention belongs to the preparation and application technology of liposome. Background technique [0002] As a drug carrier, liposome is a new type of targeting agent that has been clinically applied earlier and is the most mature; it is a particle composed of a lipid bilayer, which can mediate genes to pass through the cell membrane, and is an excellent gene and drug carrier. Drug carrier. Liposomes are widely used, the preparation process is simple, and the methods are diverse. Its particle size is in the nanoscale mesoscopic range, and has many unique physical and chemical properties. The particle size can also be controlled according to needs; it can be used for the preparation of nanoparticles, Clinical testing and diagnosis, control of catalytic reactions, simulated membrane research, delivery of genes or other substances into c...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/36A61K47/24A61K47/42A61K48/00A61K49/00
Inventor 王桂荣李国党
Owner SHANGHAI SENNA IND CO LTD
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