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Carrier of liposome medication, and preparation method

A liposome and drug technology, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve liposomes that are not easy to sterilize, high equipment requirements, low drug inclusion rate, etc. question

Active Publication Date: 2010-05-19
ZHEJIANG GLLION BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The production process is complex and requires high equipment
Moreover, the current production process cannot control the size of the liposome and the structure of the compartment, so that the liposomes produced are not uniform in size and the structure of the compartment is varied.
[0008] Second, the poor stability of liposomes cannot guarantee the stability requirements of drug development
[0009] Third, liposomes are not easy to be sterilized, especially the sterilization of large-capacity liposomes is a big challenge, and sterility is a necessary way for drug production
Of these methods only sterile ultrafiltration is suitable for sterilizing liposomes, which has proven to be difficult
[0010] Fourth, liposomes are very easy to adsorb, aggregate and fuse with each other
During the storage of liposomes, or when encountering temperature changes and adding different additives or excipients, liposomes may adsorb, aggregate and fuse with each other, resulting in liposome instability.
[0011] Fifth, the encapsulation rate is low
At present, liposomes with phospholipids as the main raw material have a low encapsulation rate for drugs, especially for some water-soluble drugs, and the drugs are easy to leak from liposomes

Method used

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  • Carrier of liposome medication, and preparation method
  • Carrier of liposome medication, and preparation method
  • Carrier of liposome medication, and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Preparation of spontaneous liposomes

[0044] The main component of the liposome, polyethylene glycol diglyceride, will be described by taking polyethylene glycol diglyceride as an example. Liposomes form spontaneously when polyethylene glycol diolein is mixed with an aqueous solution. Polyethylene glycol 200, 400, 600, 800 and 1500 glyceryl dioleate was synthesized from DuPont R&D Center (Wimington, Delaware, USA), and the water was purified water. The lipid and water were preheated to the design temperature (see Table 1), and then various polyethylene glycol diolein lipids were slowly added to the stirred aqueous solution, and then stirred for two hours or until the equilibrium was reached. At room temperature, the formation of liposomes was observed with optical microscope and electron microscope respectively. The final concentration of polyethylene glycol diolein was 10%. At room temperature (20° C.), polyethylene glycol 200, 400, and 600 diolein all spontaneously...

Embodiment 2

[0050] Preparation of Spontaneous Liposomes of Polyethylene Glycol Diacylglycerides with Different Fatty Acid Chains

[0051] To illustrate that other polyethylene glycol diglycerides also spontaneously form liposomes, stearic acid (stearic acid), palmitic acid (palmitic acid), myristic acid (myristic acid), lauric acid (dodecanoic acid) and their respective combinations with oleic acid (octadecenoic acid), using polyethylene glycol 600 as an example to synthesize polyethylene glycol diglyceride (provided by the DuPont R&D Center in the United States), to observe its Case of spontaneous liposome formation. The synthetic lipids and purified water were equilibrated to the designed temperature, and then the lipids were slowly added to the stirring water, and then stirred for two hours or until the equilibrium reached room temperature, and the liposomes were observed with an optical microscope and an electron microscope, respectively. Formation. The final concentration of polyet...

Embodiment 3

[0055] Phospholipid spontaneous liposomes

[0056] Take polyethylene glycol 600 glyceryl diolein as an example, mix with different concentrations of phosphates to verify the effect of phosphates on the formation of spontaneous liposomes of polyethylene glycol diolein, and the phosphates are POPC( 1-palmitoyl, 2-oleoylphosphorylcholine) were purchased from Sigma, and water was purified water. The ratios of POPC to polyethylene glycol 600 diolein were 5%, 10%, 15%, 20%, 30%, and 50%, respectively. POPC and Polyethylene Glycol 600 Diolein were first stirred and mixed evenly in proportion, and the mixed lipid and water were preheated to the required temperature (room temperature, 37°C and 50°C, Table 3), and then the mixed fat was slowly Slowly add to the stirring water, continue to stir for two hours or until room temperature, take a sample under the light microscope and electron microscope to observe the formation of liposomes, the final lipid concentration in this experiment i...

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Abstract

A liposome as the medicine carrier with high biocompatibility, and stability contains polyethanediol biglyceride, phosphate, and mycose and antioxidizing amino acid. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to a liposome drug carrier, and also relates to a preparation method of the liposome drug carrier. Background technique [0002] Liposome is a directional drug carrier formed by wrapping drug molecules with vesicles formed by phospholipid bilayer membranes, and belongs to a new dosage form of targeted drug delivery system. It can embed the solution or the active substance in the solution in the particles with a diameter of nanometer. At present, the main raw material of liposome is phospholipid, which is the main chemical component of liposome, and the most representative one is lecithin. Cholesterol is also another important component of liposomes. It does not form a membrane structure itself, but can be inserted into the phospholipid membrane at a molar ratio of 1:1 or even 2:1. Adding cholesterol can change the phase transition temperature of the lipid membrane, thereby affecting the permeability and fluidity of the membrane,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/24A61K47/36A61K47/16A61K9/127
CPCA61K9/127A61K47/14A61K47/183A61K47/26A61K47/20
Inventor 郭宏亮
Owner ZHEJIANG GLLION BIOTECH CO LTD
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