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Rapamycin nanoparticle for use in porous percutaneous transluminal angioplasty

An angioplasty, rapamycin technology, applied in cardiovascular system diseases, catheters, capsule delivery and other directions, can solve problems such as increased inflammatory response, low drug utilization, loss of drugs, etc., to prevent vascular restenosis, preparation method Simple, Affinity Enhancement Effect

Inactive Publication Date: 2020-11-24
LEPU MEDICAL TECH (BEIJING) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the clinical application of rapamycin is often plagued by poor water solubility, first-pass metabolism, P-glycoprotein efflux pump transport, limited oral bioavailability, and non-specific distribution at off-target sites
[0003] The main treatment methods currently used for angioplasty include implantation of bare stents, implantation of biodegradable stents, and implantation of drug-eluting stents. Stenosis of existing problems, new problems that may also increase inflammatory response and rapid proliferation of intracellular membranes
Although coatable balloons have appeared in recent years for the treatment of angioplasty, some drugs will be lost when the balloon enters the lesion, and the remaining drugs in the balloon cannot be fully recovered during balloon inflation. The drug is wasted due to the transfer to the lesion site, and the utilization rate of the drug in this treatment method is low

Method used

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  • Rapamycin nanoparticle for use in porous percutaneous transluminal angioplasty
  • Rapamycin nanoparticle for use in porous percutaneous transluminal angioplasty
  • Rapamycin nanoparticle for use in porous percutaneous transluminal angioplasty

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Using acetonitrile as the organic phase to prepare rapamycin lipopolymer hybrid nanoparticles, the particle size is about 365.6nm, spherical nanoparticles with a potential of about -20.2mV, see figure 1 and figure 2 . The encapsulation rate is 91.5%, and the specific implementation method is as follows:

[0029] (1) Dissolve 0.02 g of rapamycin and 0.16 g of polylactic acid in 32 mL of acetonitrile as an oil phase. Dissolve 0.01 g of DPPC and 0.006 g of PEGylated phospholipids in 320 mL of 4% aqueous ethanol and heat to 65° C. to ensure that all lipids are dissolved as the aqueous phase.

[0030] (2) Add the oil phase dropwise into the preheated lipid solution at a certain speed to form an O / W single emulsion. Using an ultrasonic cell disruptor, sonicate in an ice bath to form a homogeneous emulsion with smaller particle size.

[0031] (3) The organic solvent is evaporated to dryness, and the organic solvent can be recycled. The precipitate was centrifuged and was...

Embodiment 2

[0033] Using dichloromethane as the organic phase to prepare rapamycin lipopolymer hybrid nanoparticles, the obtained particle size is about 280.1nm, PDI is 0.089, and the potential is a spherical nanoparticle of -13.5mV, see image 3 and Figure 4 . The encapsulation rate is 89.6%, and the specific implementation method is as follows:

[0034] (1) Dissolve 0.02 g of rapamycin, 0.16 g of polylactic acid, 0.01 g of DPPC, 0.003 g of PEGylated phospholipid, and 0.003 g of cationic phospholipid in 32 mL of dichloromethane as an oil phase. Prepare 1% PVA aqueous solution, take 320mL as the water phase for later use.

[0035] (2) Add the oil phase dropwise into the stirring water phase at a certain speed to form an O / W single milk emulsion. Under ice bath, use a high-pressure homogenizer to form a uniform emulsion with smaller particle size.

[0036] (3) The organic solvent is evaporated to dryness, and the organic solvent can be recycled. The precipitate was centrifuged and wa...

Embodiment 3

[0038] Using the method in Example 2, two types of polylactic acid were used as polymers to prepare lipopolymer nanoparticles, and the in vitro release rule was investigated.

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Abstract

The invention discloses a rapamycin nanoparticle for use in porous percutaneous transluminal angioplasty. The invention also relates to a preparation method of the rapamycin nanoparticles. The rapamycin nanoparticle disclosed by the invention comprises a polymer core and a phospholipid shell, wherein the polymer core is formed by polymerizing rapamycin and non-biodegradable macromolecules. The advantages of different materials are utilized, slow in-vivo delivery of indissolvable drugs is achieved, and the affinity of the nanoparticles to diseased region tissue is improved. By cooperatively combining with a perforated balloon and combining the advantages of balloon dialation for the treatment of arterial embolism and the targeted action of anti-intimal hyperplasia drugs on local vessels toprevent restenosis, the rapamycin nanoparticle disclosed by the invention can effectively play a good treatment effect in the aspect of cardiovascular intervention treatment. The preparation method provided by the invention is simple, and can realize both small-scale production and large-scale production in a laboratory.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to the use method and preparation method of rapamycin nanoparticles and their application in the cardiovascular field. Background technique [0002] Rapamycin (also known as sirolimus) is an inhibitor of the mammalian target of rapamycin (mTOR) with immunosuppressive, antiproliferative, antiangiogenic, antifungal, antirestenotic and antiinflammatory properties, among others. It is often used as a drug to maintain the immunity of transplanted organs (especially kidney transplantation) to slow down the immune rejection after organ transplantation. Additionally, rapamycin-eluting stents have been shown to be highly effective in reducing coronary restenosis, re-intervention rates, and other adverse cardiac events in patients with coronary artery disease. However, the clinical application of rapamycin is often plagued by poor water solubility, first-pass metabolism, P-glycoprotein efflux pump tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61L29/08A61L29/14A61L29/16A61K9/52A61K31/436A61K47/42A61K47/36A61K47/34A61P9/10
CPCA61K9/5123A61K9/5153A61K9/5161A61K9/5169A61K31/436A61L29/08A61L29/085A61L29/148A61L29/16A61L2300/216A61L2300/416A61L2300/602A61L2300/606A61L2300/624A61P9/10
Inventor 黄慧玲魏潇萌李泳郭欲晓
Owner LEPU MEDICAL TECH (BEIJING) CO LTD
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