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A kind of astaxanthin-loaded phospholipid nanoparticles and its preparation method and application

A penicillin phospholipid and nanoparticle technology, which can be applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. To reduce the frequency of administration, improve biocompatibility, and improve water solubility

Active Publication Date: 2021-01-26
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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  • A kind of astaxanthin-loaded phospholipid nanoparticles and its preparation method and application
  • A kind of astaxanthin-loaded phospholipid nanoparticles and its preparation method and application
  • A kind of astaxanthin-loaded phospholipid nanoparticles and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0052] 30mg MPEG-PLA (polymer) and 2-5mg AST were dissolved in 1mL acetonitrile solution as organic phase; 3mg DMPC (phospholipid) was dissolved in 10mL 4% ethanol solution as water phase. The aqueous phase was preheated to 65°C and stirred at 900 rpm until the DMPC was completely dissolved. The organic phase containing the drug was added dropwise, the dripping was completed within 3 min, the stirring was continued for 2 min, the stirring speed was adjusted to 300 rpm, and the organic phase was gently stirred overnight until the organic phase was completely volatilized. Centrifuge for 40 min at 4000g and 4°C with a Millipore 10kDa centrifugal concentrator to remove unencapsulated drugs and organic solvents, and centrifuge for 2 consecutive times to finally obtain about 500 μL of nanoparticle concentrate. The mass ratios of DMPC and MPEG-PLA were 1:0, 1:1, 1:5, 1:10, 1:20, ...

Embodiment 2

[0057] Example 2 Preparation of astaxanthin phospholipid nanoparticles (AST-LPN) by emulsification solvent evaporation method

[0058] The main reason for the low encapsulation efficiency and drug loading of astaxanthin lipid nanoparticles prepared by nanoprecipitation method may be the low solubility of AST in acetonitrile. The same mass of AST was dissolved in acetonitrile and dichloromethane. After vortexing, the dichloromethane solution was more clear and translucent. It is speculated that the solubility of AST in dichloromethane is higher than that in 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: 30 mg of MPEG-PLA and 2-5 mg of AST were dissolved in 1 mL of dichloromethane as the organic phase; 3 mg of DMPC was dissolved in 3 mL of a 4% methanol aqueous solut...

Embodiment 3

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

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

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Abstract

The invention discloses a phospholipid nanoparticle loaded with astaxanthin (AST) and a preparation method thereof. The phospholipid nanoparticle is obtained by mixing an organic phase in which a polymer and astaxanthin are dissolved with an aqueous phase in which a phospholipid is dissolved. Obtained by emulsified solvent evaporation method, in which the polymer is monomethoxypolyethylene glycol-polylactic acid (MPEG-PLA), and the phospholipid is dimyristoylphosphatidylcholine (DMPC). The invention changes the solubility and size of astaxanthin by carrying out phospholipid nanoparticles loading modification on astaxanthin, greatly improves the water solubility of fat-soluble drug astaxanthin, and at the same time, the phospholipid nanoparticles endows astaxanthin with slow-release characteristics , that is, the drug is released slowly after entering the cells of the lesion, which can reduce the frequency of administration and enhance the therapeutic effect.

Description

technical field [0001] The invention relates to a phospholipid nanoparticle loaded with high antioxidant active drugs, in particular to a preparation method and application of the astaxanthin-loaded phospholipid nanoparticle. 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 inner ear microenvironment and the decrease of anti-oxidative stress. A large number of small molecule compounds with antioxidant activity have been confirmed in vitro and in vivo to prevent and antagonize ototoxicity caused by elevated ROS, and some drugs have entered the clinical trial stage. However, due to the special structure of the inner ear, systemically administered small-molecule compounds often fail to enter the lesion site, resulting in failure of clinical trials. [0003] Astaxanthin has strong antioxidant activity and has been proven to be useful f...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K47/24A61K47/34A61K31/122A61P27/16
CPCA61K9/5015A61K9/5031A61K31/122A61P27/16
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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