Thrombus-targeted long-cycle sustained release liposome and preparation method thereof

A long-circulation, slow-release lipid technology, applied in liposome delivery, biochemical equipment and methods, blood diseases, etc., can solve the problem of slow-release effect, unsatisfactory encapsulation rate and drug loading rate, and unsatisfactory thrombus targeting , drug release too fast and other problems, to achieve the effect of maintaining effective drug concentration, improving medication compliance, and reducing toxic and side effects

Inactive Publication Date: 2019-01-08
HUBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still some shortcomings and problems that need to be solved urgently in the current research: ① Thrombolytic drug sustained-release preparations prepared using traditional polylactic acid (unfunctionalized) or poly(lactic-co-glycolic acid) (PLGA) as carriers are due to self-catalysis Effect (degradation too fast) cause

Method used

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  • Thrombus-targeted long-cycle sustained release liposome and preparation method thereof
  • Thrombus-targeted long-cycle sustained release liposome and preparation method thereof
  • Thrombus-targeted long-cycle sustained release liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] 1. Feeding: Prepare materials according to the quality of each material in Table 1

[0029] The feeding quality of each material in Table 1 and the percentage of the total mass (by preparing 100mg)

[0030]

[0031] 2. Preparation method

[0032]Step 1: Prepare drug-loaded long-circulation sustained-release liposome suspension by reverse-phase evaporation method: Weigh soybean phospholipids, cholesterol and star-shaped cholic acid functionalized polylactic acid, and dissolve them all in a certain amount of mixed solvent of chloroform and methanol (1:4, V / V); dissolve urokinase in barbiturate buffer (0.01mol / L, pH=7.4), add it to the above solution, mix and shake, and ultrasonicate in a water bath for 4 to 6 minutes to obtain The emulsion was rotated under reduced pressure on a rotary evaporator to remove the organic solvent, probe-type ultrasound for 1 min, added distearoylphosphatidylethanolamine-polyethylene glycol solution, and incubated in a water bath at 5-8°C ...

Embodiment 2

[0060] 1. Feeding: Prepare materials according to the quality of each material in Table 2

[0061] Table 2 The feeding quality of each material and the percentage of the total mass (based on the preparation of 100mg)

[0062]

[0063]

[0064] 2. Preparation method

[0065] The preparation method is the same as in Example 1.

[0066] 3. Characterization

[0067] Characterization observation method is the same as embodiment 1, and the results are as follows:

[0068] (1), the surface morphology is spherical, and the size distribution is relatively uniform. For details, see figure 2 .

[0069] (2), the average particle size is 91.5nm; the polydispersity coefficient is 0.203.

[0070] (3), encapsulation efficiency and drug loading

[0071] Determination results: the drug loading is 4.7%; the encapsulation efficiency is 80.6%. The drug-loading capacity of the liposome (other components are the same) without star-shaped cholic acid functionalized polylactic acid is 3....

Embodiment 3

[0081] 1. Feeding: Prepare materials according to the quality of each material in Table 3

[0082] Table 3 The feeding quality of each material and the percentage of the total mass (based on the preparation of 100mg)

[0083]

[0084] 2. Preparation method

[0085] Preparation method is the same as embodiment 1

[0086] 3. Characterization

[0087] Characterization observation method is the same as embodiment 1, and the results are as follows:

[0088] (1), the surface morphology is spherical, and the size distribution is relatively uniform. For details, see image 3 .

[0089] (2), the average particle size is 91.5nm; the polydispersity coefficient is 0.203.

[0090] (3), encapsulation efficiency and drug loading

[0091] Determination results: the drug loading is 6.3%; the encapsulation efficiency is 82.5%. The drug-loading capacity of the liposome without adding star-shaped cholic acid-functionalized polylactic acid (other components are the same) is 4.5%, and the...

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Abstract

The invention discloses a thrombus-targeted long-cycle sustained release liposome and a preparation method thereof and belongs to the technical field of drug controlled release and biological materials. The thrombus-targeted long-cycle sustained release liposome comprises a drug-loading sustained release liposome as well as a platelet membrane and distearoyl phosphoethanolamine-polyethylene glycol, wherein the drug-loading sustained release liposome is composed of a thrombolytic drug, star cholic acid functionalized poly(lactic acid), soyabean lecithin and cholesterol; the platelet membrane and distearoyl phosphoethanolamine-polyethylene glycol cover the drug-loading sustained release liposome in a staggered manner. The preparation method disclosed by the invention comprises the followingsteps: introducing the star cholic acid functionalized poly(lactic acid) into a thrombolytic drug long-cycle liposome, and modifying the platelet membrane and distearoyl phosphoethanolamine-polyethylene glycol, thereby obtaining the thrombus-targeted long-cycle sustained release liposome. The defects that the conventional thrombosis drug needs frequent dosing, the curative effects are poor and thecost is high are overcome, and the thrombus-targeted long-cycle sustained release liposome has the advantages of being excellent in thrombus targeting property, excellent in sustained release effect,long in half-life in vivo, obvious in thrombolytic effect, high in stability, excellent in biocompatibility and the like.

Description

technical field [0001] The invention belongs to the technical field of drug controlled release and biomaterials, in particular to a thrombus-targeted long-circulation slow-release liposome modified with platelet membrane and distearoylphosphatidylethanolamine-polyethylene glycol and a preparation method thereof Background technique [0002] The formation of atherosclerotic plaque is due to the metabolic disorder of the inner wall of the blood vessel caused by coronary artery and cerebrovascular diseases, which leads to thickening of the arterial blood vessel wall. Among them, due to the accumulation of oxidized LDL (low-density lipoprotein), it causes an inflammatory response, and the inflammatory response causes single cells to differentiate into phagocytic cells, which phagocytize LDL, causing positive feedback regulation, leading to more immune cells coming to this area. In the area, the phagocytes that ingest LDL burst and die, and accumulate on the inner wall of the blo...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/46A61K47/24A61K47/10A61K47/28A61K47/34A61K38/49A61K38/48A61P7/02
CPCA61K9/1272A61K9/1277A61K38/484A61K38/49A61K47/10A61K47/24A61K47/28A61K47/34A61K47/46A61P7/02C12Y304/21007C12Y304/21073
Inventor 刘红秦吟王宗春陈勇
Owner HUBEI UNIV
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