AST (astaxanthin)-supported phospholipid nanoparticles as well as preparation method and application thereof

A penicillin phospholipid and nanoparticle technology, which is used in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve unfavorable medicines, increase the probability of human trauma and infection, To reduce the frequency of administration, improve biocompatibility, and improve water solubility

Active Publication Date: 2019-02-26
SHANGHAI NINTH PEOPLES HOSPITAL SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies on the use of astaxanthin for ototoxicity such as hearing loss caused by oxidative stress in the inner ear have not been reported.
The reasons may be as follows: 1) Astaxanthin is fat-soluble and slightly soluble in water, which is not conducive to making medicines; 2) The inner ear is a semi-closed structure with double barrier protection of blood-brain and blood-labyrinth, systemic Medication is difficult to reach the lesion
However, local inner ear medication is usually lost through the eustachian tube, requiring repeated medication, which easily increases the probability of artificial trauma and infection

Method used

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  • AST (astaxanthin)-supported phospholipid nanoparticles as well as preparation method and application thereof
  • AST (astaxanthin)-supported phospholipid nanoparticles as well as preparation method and application thereof
  • AST (astaxanthin)-supported phospholipid nanoparticles as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1: Preparation of astaxanthin phospholipid nanoparticles (AST-LPN) by nanoprecipitation method

[0052] 30mg MPEG-PLA (polymer) and 2-5mg AST were dissolved in 1mL acetonitrile solution as the organic phase; 3mg DMPC (phospholipid) was dissolved in 10mL 4% ethanol solution as the water phase. The water phase was preheated to 65°C and stirred at 900 rpm until DMPC was completely dissolved. The organic phase containing the drug was added dropwise, and the dripping was completed within 3 minutes, and the stirring was continued for 2 minutes, the stirring speed was adjusted to 300 rpm, and the organic phase was stirred gently overnight until the organic phase was completely volatilized. Use a Millipore 10kDa centrifugal concentration tube to centrifuge at 4000g, 4°C for 40min to remove unencapsulated drugs and organic solvents, and centrifuge twice continuously to obtain about 500μL nanoparticle concentrate. The mass ratio of DMPC to MPEG-PLA is 1:0, 1:1, 1:5, 1:10...

Embodiment 2

[0057] Embodiment 2 Emulsion solvent volatilization method prepares astaxanthin phospholipid nanoparticles (AST-LPN)

[0058] Analysis of the main reasons for the low encapsulation efficiency and drug loading of astaxanthin lipid nanoparticles prepared by nanoprecipitation method may be due to the low solubility of AST in acetonitrile. The same mass of AST was dissolved in acetonitrile and dichloromethane. After vortex dissolving, the dichloromethane solution became clearer and brighter. It is speculated that the solubility of AST in dichloromethane is higher than that of acetonitrile solution. Therefore, dichloromethane was used instead of acetonitrile to dissolve AST and MPEG-PLA, and 4% (volume ratio of methanol to water) methanol aqueous solution was used to dissolve DMPC to prepare AST-LPN. The detailed steps are as follows: 30mg MPEG-PLA and 2-5mg AST were dissolved in 1mL dichloromethane as the organic phase; 3mg DMPC was dissolved in 3mL 4% aqueous methanol as the aque...

Embodiment 3

[0061] Example 3 Investigation of the sustained release characteristics of AST-LPN in inner ear lymph fluid

[0062] Such as Figure 9 As shown, AST-LPN was sustained release in artificial lymph fluid for 15 days in vitro. In addition, if Figure 10 As shown, the experimental results of drug concentration detection in inner ear lymph fluid proved that after AST solution (6 μg) was administered through the round window membrane, the lymph fluid was taken 30 minutes after administration for mass spectrometry analysis, and the AST content was not detected. The results suggest that fat-soluble AST cannot enter the inner ear through the round window membrane. Based on this, we determined that AST administered through the round window membrane could not exert the protective effect of cisplatin ototoxicity. see Figure 10 , after guinea pigs were given AST-LPN through the round window membrane (RWM) (AST concentration: 1.0mg / mL, 6μL), the concentration in the lymph fluid reached ...

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Abstract

The invention discloses AST (astaxanthin)-supported phospholipid nanoparticles and a preparation method thereof. The phospholipid nanoparticles are obtained by mixing an organic phase in which a highmolecular polymer and astaxanthin are dissolved and a water phase in which phospholipid are dissolved by emulsion solvent volatilization, wherein the high molecular polymer is single MPEG-PLA (methoxypoly(ethylene glycol)-poly(lactide) copolymer), and phospholipid is DMPC (1,2-dimyristoyl-sn-glycero-3-phosphocholine). Astaxanthin is subjected to entrapment modification of the phospholipid nanoparticles, the dissolution characteristic and size of astaxanthin are changed, and water solubility of lipid-soluble drug astaxanthin is greatly improved; meanwhile, astaxanthin is endowed with slow release characteristic by the phospholipid nanoparticles, that is, the drug is continuously and slowly released after entering cells of pathological changes, so that the administration frequency can be reduced, and the treatment effect can be enhanced.

Description

technical field [0001] The invention relates to a phospholipid nanoparticle loaded with a drug with high antioxidant activity, in particular to a preparation method and application of the phospholipid nanoparticle loaded with astaxanthin. Background technique [0002] The common pathogenic mechanism of inner ear diseases such as noise-induced and drug-induced deafness involves the increase of reactive oxygen species (ROS) in the microenvironment of the inner ear and the decrease of antioxidant stress. A large number of small molecular compounds with antioxidant activity have been proven to prevent and antagonize ototoxicity caused by elevated ROS in in vivo and in vitro experimental studies, and some drugs have entered the clinical trial stage. However, due to the special structure of the inner ear, small molecule compounds that are often administered systemically cannot enter the lesion site, resulting in failure of clinical trials. [0003] Astaxanthin has strong antioxid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/24A61K47/34A61K31/122A61P27/16
CPCA61P27/16A61K9/5015A61K9/5031A61K31/122
Inventor 於得红汪雪玲吴皓陈聿名童玲顾佳怡
Owner SHANGHAI NINTH PEOPLES HOSPITAL SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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