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Preparation method of PEG nano-liposomes for embedding salidroside

A nano-liposome and salidroside technology, which is applied in liposome delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of frequent taking, low bioavailability, To avoid problems such as large doses, achieve the effects of stable blood drug concentration, avoid immune response, and prolong the action time

Inactive Publication Date: 2018-04-13
福建省中医药科学院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the disadvantages of the above-mentioned salidroside-related products, such as large dosage, many times of taking, low bioavailability in vivo, and general liposomes are easily cleared by the immune system, the present invention provides a PEGylated nano Preparation method of liposome; the feature of this method is that DSPE-PEG2000 is embedded in the cholesterol component of liposome, which can prevent plasma protein from being adsorbed on the surface of liposome, avoiding the generation of immune response, thereby prolonging the salidroside lipid In order to enhance the pharmacological efficacy of salidroside and improve the bioavailability

Method used

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  • Preparation method of PEG nano-liposomes for embedding salidroside
  • Preparation method of PEG nano-liposomes for embedding salidroside

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Experimental program
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Effect test

Embodiment 1

[0017] Accurately weigh 881.95 mg of soybean lecithin, 368.05 mg of cholesterol, and 50 mg of DSPE-PEG2000 into a 250ml round-bottomed flask, add 15ml of ethanol, dissolve in a water bath at 45°C, rotate and evaporate at a speed of 100rpm, and then continue vacuuming for 30min at a water bath temperature of 50°C . Take 24ml of PBS buffer solution with pH 7.0 (ionic strength 20mmol / L), add 0.36g of salidroside, stir to dissolve and add to the round bottom flask, shake for 3min and then sonicate for 20min to completely hydrate the lipid film. The hydration temperature is 30-40°C. Homogenize with a high-pressure homogenizer for 5 minutes at a pressure of 800bar-850bar. After homogenization, extrude with an extruder (ATS), filter twice with 400nm and 200nm polycarbonate membranes, and extrude at a pressure of 5-7bar , the extrusion temperature is 50° C., and the PEGylated salidroside nanoliposome colloidal solution is obtained.

Embodiment 2

[0019] Accurately weigh 932.81 mg of soybean lecithin, 317.19 mg of cholesterol, 50 mg of DSPE-PEG2000, and 0.36 g of salidroside into a 250ml round-bottom flask, add 15ml of ethanol, dissolve in a water bath at 45°C, and continue pumping after complete rotary evaporation at 100rpm. Vacuum for 30min, water bath temperature 50°C. Take 24ml of PBS buffer solution with pH 7.0 (ionic strength 20mmol / L) into the round bottom flask, shake for 3min and then sonicate for 20min to completely hydrate the lipid film, the hydration temperature is 30-40℃. Homogenize with a high-pressure homogenizer for 5 minutes at a pressure of 800bar-850bar. After homogenization, extrude with an extruder (ATS), filter twice with 400nm and 200nm polycarbonate membranes, and extrude at a pressure of 5-7bar , the extrusion temperature is 50° C., and the salidroside PEGylated nano-liposome colloidal solution is obtained.

Embodiment 3

[0021] Accurately weigh 1025.77 mg of soybean lecithin, 224.23 mg of cholesterol, 50 mg of DSPE-PEG2000, and 0.36 g of salidroside into a 250ml round bottom flask, add 15ml of ethanol, dissolve in a water bath at 45°C, and continue to Vacuumize for 30 minutes, and the temperature of the water bath is 50°C. Take 24ml of PBS buffer solution with pH 7.0 (ionic strength 20mmol / L) into the round bottom flask, shake for 3min and then sonicate for 20min to completely hydrate the lipid film, the hydration temperature is 30-40℃. Homogenize with a high-pressure homogenizer for 5 minutes at a pressure of 800bar-850bar. After homogenization, extrude with an extruder (ATS), filter twice with 400nm and 200nm polycarbonate membranes, and extrude at a pressure of 5-7bar , the extrusion temperature is 50° C., and the salidroside PEGylated nano-liposome colloidal solution is obtained.

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Abstract

The invention provides a preparation method of PEG nano-liposomes for embedding salidroside. The preparation method comprises the following steps: dissolving cholesterol, soybean lecithin, 1,2-distearoyl-SN-glycerol-3-phosphoethanolamine-N-maleimide-polyethylene glycol 2000 (DSPE-PEG2000) and the salidroside in absolute ethyl alcohol, and forming a lipid membrane through evaporating under reducedpressure; adding a phosphate buffering solution for hydrating fully, performing oscillating and ultrasonic dispersing to obtain a suspension liquid; extruding to obtain a PEG salidroside nano-liposomecolloidal solution. According to the preparation method, the average particle size of the PEG salidroside nano-liposomes is less than 100 nm; the Zeta potential is -33.4 mV; the encapsulation rate ofthe salidroside is 50 to 60 percent. Common liposomes have relatively high lipid solubility and can start immune response so as to be cleaned quickly by macrophages. The salidroside PEG nano-liposomes are prepared with the preparation method; the problem that the salidroside nano-liposomes are quickly cleaned because of high lipid solubility can be solved; the effective plasma concentration timeof the salidroside in vivo is prolonged; the bioavailability is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a method for preparing PEGylated nano liposomes embedding salidroside. Background technique [0002] Rhodiola belongs to the genus Rhodiola (Sedum sedum) Rhodiola L. ) is a perennial herbaceous plant, which is a traditional Tibetan medicinal plant in my country, which is recorded in "Sibu Medical Code" and "Compendium of Materia Medica". Studies have shown that rhodiola rosea has an "adaptation-like" effect similar to ginseng and eleuthero, that is, it can strengthen the body's adaptability and non-specific resistance, and restore the normal function of the body. Salidroside is the main active ingredient in the rhizome of Rhodiola rosea. Pharmacological experiments have found that it not only has significant curative effects in preventing and treating cardiovascular diseases, but also has many functions such as anti-neuron cell apoptosis, promoting nerve repair, and re...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K31/7032A61P9/00A61P25/00
CPCA61K9/127A61K31/7032A61K47/24
Inventor 肖庆胡娟陈立典韩静钟志凤
Owner 福建省中医药科学院