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Nanoliposome composition, preparation method thereof and eye drops

A nano-liposome and composition technology, which is applied in liposome delivery, drug combination, drug delivery, etc., can solve the problems of time-consuming and solvent-consuming, low availability of wild chrysanthemum drugs, and poor bioavailability, so as to improve solubility and stability, improve bioavailability, and improve the effect of bioavailability

Inactive Publication Date: 2019-09-20
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the above-mentioned operation process is complicated and easily destroys the compound structure, so that the drug concentration of each active ingredient in the existing wild chrysanthemum eye drops may be low, and the operation process is complicated, the cycle is long, time-consuming and solvent-consuming, resulting in wild chrysanthemum eye drops. Chrysanthemum has a low drug utilization, resulting in a large amount of waste of raw materials, and there is a phenomenon that a large amount of raw materials are invested, but the yield is very small
[0005] In addition, Menghuaside has the characteristics of low solubility and low permeability, the equilibrium solubility in water is 0.059μg / mL, it is almost insoluble in water, the solubility in alkaline solution increases, and its fat solubility is poor, so it is difficult to be absorbed by the body. Absorption, resulting in poor bioavailability
At present, there are very few studies on the preparation of mongoside, which greatly limits its clinical application.

Method used

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  • Nanoliposome composition, preparation method thereof and eye drops
  • Nanoliposome composition, preparation method thereof and eye drops
  • Nanoliposome composition, preparation method thereof and eye drops

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] The preparation of embodiment 1 nano liposome composition

[0060] 1 # Nanoliposome composition

[0061] a) Weighing 1.00 mg of basil extract, 8.00 mg of cholesterol, and 35.00 mg of lecithin into a 50 mL eggplant-shaped bottle, adding 10 mL of absolute ethanol to dissolve to obtain a solution;

[0062] b) In a water bath at 45°C, place the above solution on a rotary evaporator for rotary evaporation. After the absolute ethanol is completely recovered, a layer of evenly distributed milky white lipid film is formed on the inner wall of the eggplant-shaped bottle;

[0063] c) Add 10mL of ultrapure water to the above-mentioned uniform lipid film, heat and stir in a water bath at 40°C, the stirring rate is 500rpm, and after uniform mixing, a milky white uniform suspension is obtained, which is passed through a 0.45μm microporous membrane to obtain nano liposome composition;

[0064] d) Store at 4°C for later use.

[0065] 2 # Nanoliposome composition

[0066] 2 #...

experiment example 1

[0072] The characterization of experimental example 1 nano liposome composition

[0073] Drug loading and encapsulation efficiency

[0074] With the 1 prepared in embodiment 1 # ~3 # The nanoliposome composition is typical, and adopts 1100LC high-performance liquid phase method (HPLC) to measure its drug loading and encapsulation efficiency, and the assay method is specifically:

[0075] Drawing of the standard curve of mongoside: take 1mg of the raw material drug in a beaker, add appropriate amount of methanol to dissolve, transfer the solution to a 10mL volumetric flask, dilute the methanol to the mark, and prepare a 0.1mg / mL mother solution of mongoside in methanol. Draw a certain amount of mother liquor into a 10mL volumetric flask, dilute to volume with methanol, and prepare standard solutions with concentrations of 0.01mg / mL, 0.02mg / mL, 0.04mg / mL, 0.06mg / mL, and 0.08mg / mL, respectively. Measured by HPLC, the measuring wavelength is 326nm, the concentration is taken ...

experiment example 2

[0084] The stability of experimental example 2 nano liposome composition

[0085] With the 3 prepared in embodiment 1 # The nanoliposome composition is placed in an environment of 25±2°C, and its appearance is observed on the 0th, 1st, 3rd, 5th, 7th, and 9th day of storage, and the particle size and potential are measured to investigate the stability of the preparation. , the results are shown in Table 1. From the data in the table, it can be seen that after being placed for 9 days, the appearance of the nanoliposome composition did not change visible to the naked eye, and remained as a milky white homogeneous solution. The microscopic particle size and drug loading Also maintained good stability.

[0086] Table 1 nano liposome composition stability

[0087]

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Abstract

The invention relates to a nanoliposome composition, a preparation method thereof and eye drops. The nanoliposome composition comprises a nanoliposome and an active component loaded on the nanoliposome; the active component is selected from linarin or a linarin extract; and the drug loading amount of the nanoliposome is 0.05 mg / mL-0.1 mg / mL. The nanoliposome composition is suitable for drug loading, the solubility and stability of the linarin are improved, high anti-inflammatory concentration can be achieved, the bioavailability of the linarin is greatly improved, and the nanoliposome composition can be used for eye drops. The preparation method of the nanoliposome composition is simple and efficient to operate and short in period, the utilization amount of a solvent is small, the solvent can be recycled, and damage to the active ingredient compound structure in a preparation process can be avoided effectively.

Description

technical field [0001] The invention relates to the field of nano-liposomes, in particular to a nano-liposome composition, a preparation method thereof and eye drops. Background technique [0002] As a biodegradable and biocompatible functional ingredient drug carrier, liposome has certain targeting and sustained release properties. It has received extensive attention in recent years due to the following advantages: (1) Increased hydrophobicity (2) increase the stability of the drug in the body; (3) prolong the release time of the therapeutic agent; (4) reduce the uptake of the drug by normal tissues and reduce the side effects of the therapeutic agent to a certain extent; (5) ) through the functional modification of the liposome, thereby increasing the sensitivity of the diseased part to the drug, releasing the drug at a fixed point, and increasing the phagocytosis of the drug by the cell. The vesicles formed by liposomes in water generally have a diameter between 25-500nm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61P27/02
CPCA61K9/0048A61K9/127A61K31/7048A61P27/02
Inventor 刘洋张启蒙王童
Owner ZHENGZHOU UNIV
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