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Microliposome composition

A composition and phospholipid technology, applied in the directions of drug combination, liposome delivery, medical preparations of inactive ingredients, etc., can solve the problems of difficult and difficult treatment of brain diseases, and achieve the regulation of neuroplasticity and the promotion of synapses. Generate effect, enhance the effect of loop

Active Publication Date: 2019-06-04
张正风 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the blood-brain barrier shields most drugs, with only about 25 percent able to enter the brain, making treatment extremely difficult
[0004] Known drugs for the treatment of central nervous system diseases enter the brain through the nasal cavity and other mucosal tissues, but the multi-layer tissue in the nasal cavity prevents macromolecular drugs from entering the brain including bones, dura mater and arachnoid (blood-brain barrier), This is the root cause of brain diseases that are hard to treat

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] [Example 1]-Mobility test of administration liposome composition

[0076] Four first-generation mice born in the same littermate and raised in the animal room for 8 months were subjected to a preliminary cylinder test, in which a wild-type mouse of a healthy model and a transgenic mouse of a disease model were administered with the mouse of Comparative Example 1 Mixed solution, the other two transgenic mice of the disease model were administered with Embodiment 1. Three tests were performed per mouse.

[0077] refer to Figure 5 , which shows the average number of forelimb-wall contacts and error bars for these mice within five minutes. In the mouse group administered with Comparative Example 1, the activity of the disease model mice was significantly lower than that of the littermate healthy model mice (P=0.018). The activity of the disease model mice administered with Embodiment 1 was significantly higher than that of the disease model mice administered with Compar...

Embodiment 2

[0078] [Example 2]-administration of activity tests containing liposome compositions with different nutrients

[0079] Two first-generation mice born in the same littermate and raised in the animal room for 8 months were subjected to a preliminary cylinder test. One of the transgenic mice of the disease model was administered with Comparative Example 2, and the other transgenic mouse of the disease model was administered with Implementation Pattern 1. Three tests were performed per mouse.

[0080] The results are shown in Table 1 below. The activity of the disease model mice administered with Embodiment 1 was higher than that of the disease model mice administered with Comparative Example 2. In other words, among the mice that are also disease models, the PD symptoms (increased activity) of the mice administered with Embodiment 1 were significantly improved (increased in activity) compared with the mice administered with Comparative Example 2. Therefore, the liposome composit...

Embodiment 3

[0083] [Example 3] - Survival analysis

[0084] In order to test the lethal side effects of the present invention on mice, in Example 3, the disease model mice and the healthy model mice in the same litter were fed with Embodiment 1 and Comparative Example 1 respectively.

[0085] refer to Image 6 , which shows the survival analysis results. The results showed that all other healthy and disease models administered with Embodiment 1 or Comparative Example 1 died after 10 weeks of continuous treatment with Embodiment 1 (10 mg / day for two consecutive weeks) except one disease model mouse. All mice survived, and no immediate treatment-related death, nor apparent abnormal behavior was observed in the surviving mice. This result indicated that administration of Embodiment 1 for continuous treatment (10 mg / day for two consecutive weeks) did not result in immediate death of the mice.

[0086] In summary, the double-layer phospholipid layer and the special targeting substance of th...

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Abstract

The invention provides a microliposome composition comprising a microliposome, a nutrient and a target substance; the microliposome is surrounded by a double-layer phospholipid layer, and the inner side of the double-layer phospholipid layer has an accommodating space; the nutrient is located in the accommodating space, wherein the nutrient comprises glutamic acid, docosahexaenoic acid (DHA) and lecithin; the target substance is embedded in or bound to the microliposome. The double-layer phospholipid layer of the microliposome composition and the special target substance can release the nutrient containing glutamic acid through a blood-brain barrier in a human body, so as to activate neuroglial cells and enable the neuroglial cells to obtain calcium ions, and achieve the efficacies of promoting synaptogenesis, controlling neuronal plasticity and synaptic transmission, and improving the glutamic acid-glutamic acid cycle.

Description

technical field [0001] The invention relates to a liposome composition, in particular to a liposome composition for improving Parkinson's disease and Alzheimer's disease. Background technique [0002] Parkinson's disease (PD) is a degenerative disease of the central nervous system caused by defects in the formation and action of dopamine, which can cause damage to human movement and language abilities. Alzheimer's disease (Alzheimer's disease, AD) is a degenerative disease of the brain. It is a persistent neurological dysfunction that will worsen over time. exception etc. Although many teams have conducted in-depth research on central nervous diseases such as Parkinson's and Alzheimer's, there is still no cure for these diseases, and most of the symptomatic treatments have side effects or unsatisfactory effects. [0003] The main reason is that the human body has a self-protection mechanism, the blood-brain barrier (BBB), which is located between blood vessels and the brai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K45/06A61K31/685A61K31/202A61K31/198A61P25/16
Inventor 龚蕙
Owner 张正风
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