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Fenofibrate-containing nano-liposome as well as preparation method and application thereof

A nano-liposome and fenofibrate technology, applied in the field of medicine, can solve problems such as poor fluidity and dispersibility, increased surface energy of drug powder, and small drug loading, so as to achieve good fluidity and dispersibility, improve Bioavailability, the effect of reducing adverse reactions

Inactive Publication Date: 2016-07-27
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above new formulation types have certain limitations
Although the micronized preparation increases the specific surface area of ​​the drug, this increase increases the surface energy of the drug powder, thereby making the powder in an unstable state, easy to aggregate, and poor in fluidity and dispersion. Such as tablets and capsules) are more difficult and have a certain impact on absorption; nanocrystals may cause cytotoxicity and immune reactions due to the particle size being at the nanometer level; Disadvantages of poor stability in dispersed state and difficulty in industrialization; a large amount of surfactants in the self-emulsifying drug delivery system have certain toxic and side effects on the gastrointestinal tract

Method used

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  • Fenofibrate-containing nano-liposome as well as preparation method and application thereof
  • Fenofibrate-containing nano-liposome as well as preparation method and application thereof
  • Fenofibrate-containing nano-liposome as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1, the preparation of fenofibrate nano liposome

[0043] Accurately weigh fenofibrate, phospholipids and cholesterol, and place them in a 50mL eggplant-shaped bottle. The mass ratio of phospholipids and cholesterol is 9:1, the drug-to-lipid ratio (mass ratio) is 1:10 (the lipid mass is the total mass of phospholipids and cholesterol), and the mass of fenofibrate is 25 mg. Add 3mL of chloroform and shake fully to dissolve the drug and lipid completely. The film was formed by rotary evaporation under reduced pressure at 37° C., and vacuum-dried overnight at room temperature (25° C.), so that the film formed on the bottle wall was evenly dried. Add 6 mL of PBS buffer solution (the specific formula is NaCl137mmol / L, KCl2.7mmol / L, NaCl2.7mmol / L, NaCl2. 2 HPO 4 10mmol / L, KH 2 PO 4 2mmol / L, the PBS buffer concentration is 0.01mmol / L), the hydration temperature is 37°C, and the hydration time is 30min; the probe is ultrasonicated in an ice-water bath to reduce the...

Embodiment 2

[0044] Embodiment 2, the preparation of fenofibrate nano liposome

[0045] Accurately weigh fenofibrate, phospholipids and cholesterol, and place them in a 50mL eggplant-shaped bottle. The mass ratio of phospholipids and cholesterol is 4:1, the drug-to-lipid ratio (mass ratio) is 2:75 (the lipid mass is the total mass of phospholipids and cholesterol), and the mass of fenofibrate is 6 mg. Add 3mL of chloroform and shake fully to dissolve the drug and lipid completely. The film was formed by rotary evaporation under reduced pressure at 37°C, and dried in vacuum at room temperature overnight, so that the film formed on the bottle wall was evenly dried. Add 10mL of PBS buffer solution (the specific formula is NaCl137mmol / L, KCl2.7mmol / L, NaCl2.7mmol / L, NaCl2. 2 HPO 4 10mmol / L, KH 2 PO 4 2mmol / L, PBS buffer concentration is 0.01mmol / L), the hydration temperature is 37°C, and the hydration time is 30min. In an ice-water bath, the probe is ultrasonicated to reduce the particle...

Embodiment 3

[0046] Embodiment 3, the quality evaluation of fenofibrate nano liposome

[0047] 1. Determination of particle size and Zeta potential: Take the fenofibrate nanoliposome of Example 1 of the present invention, measure it with a Malvern laser particle size analyzer, and record the average particle size, polydispersity index (PDI) and Zeta potential. The average particle size is 122.1±1.40nm, the PDI is 0.293; the Zeta potential is -2.92mV, slightly electronegativity (as shown in Table 1).

[0048] Table 1. Characterization of Fenofibrate Nanoliposomes (n=3)

[0049]

[0050] 2. Determination of encapsulation efficiency and drug loading:

[0051] The method for measuring the encapsulation efficiency of the present invention is an ultracentrifugation method.

[0052] Precision measures the fenofibrate nanoliposome 1mL of embodiment 1, with PBS damping fluid (prescription is NaCl137mmol / L, KCl2.7mmol / L, NaCl2.7mmol / L, NaCl2. 2 HPO 4 10mmol / L, KH 2 PO 4 2mmol / L, the final c...

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Abstract

The invention discloses fenofibrate-containing nano-liposome as well as a preparation method and application thereof. The fenofibrate-containing nano-liposome comprises fenofibrate and nano-liposome, wherein the nano-liposome is composed of phospholipid and cholesterol, and the mass ratio of the cholesterol to the phospholipid is equal to 1: (3-15); the mass ratio of the fenofibrate to the phospholipid is equal to 1: (4-40). The preparation method comprises the following steps: (1) dissolving the phospholipid, the cholesterol and the fenofibrate into a solvent, mixing, and then removing the solvent to obtain a mixture; (2) hydrating the mixture obtained in the step (1) with a buffer solution to obtain a nano-liposome system; (3) carrying out probe ultrasonic processing on the nano-liposome system obtained in the step (2), and then filtering to obtain the fenofibrate-containing nano-liposome. The fenofibrate-containing nano-liposome is applied to preparation of medicine for treating non-alcoholic fatty liver disease. The fenofibrate-containing nano-liposome can improve the bioavailability of fenofibrate oral administration.

Description

technical field [0001] The invention relates to a fenofibrate nano liposome and a preparation method and application thereof, belonging to the technical field of medicine. Background technique [0002] Nonalcoholic fatty liver disease (NAFLD) is a clinicopathological syndrome characterized by excessive fat deposition (imaging or histological evidence) in hepatocytes caused by causes other than alcohol and other clear liver injury factors. NAFLD is the most common chronic liver disease in the West; in my country, with the increase in the number of obese people, the incidence of NAFLD is also on the rise. Patients with NAFLD often suffer from metabolic diseases such as obesity, diabetes, and dyslipidemia. Many studies have shown that excessive fat deposition in non-adipose tissue is toxic. According to the "second hit" hypothesis, excessive lipids act as a "first hit", which can cause "second hits" such as oxidative stress, mitochondrial dysfunction, and inflammation, so tha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/28A61K47/24A61K31/216A61P1/16
CPCA61K9/127A61K9/1277A61K31/216A61K47/24A61K47/28
Inventor 祁荣曹旖旎
Owner PEKING UNIV
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