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Curcumin coated liposome preparation and preparation method thereof

A technology of liposome preparation and curcumin, which is applied in the field of medical applications, can solve the problems of low oral bioavailability, low absorption, poor fat solubility, etc., and achieve the effects of promoting dissolution and absorption, improving stability, and simple preparation

Inactive Publication Date: 2012-07-18
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, curcumin is almost insoluble in water and poor in fat solubility, so it has little absorption through the gastrointestinal tract and low oral bioavailability

Method used

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  • Curcumin coated liposome preparation and preparation method thereof
  • Curcumin coated liposome preparation and preparation method thereof
  • Curcumin coated liposome preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Accurately weigh 10mg curcumin, 100mg soybean lecithin, 10mg cholesterol, add to 20ml absolute ethanol, remove ethanol under reduced pressure at 40°C, dry overnight in a vacuum oven, add 20ml phosphate buffer saline (PBS, pH 5~ 7) Carry out hydration, centrifuge to remove the decrystallization drug, filter the obtained liposome suspension A through a 0.8 μm microporous membrane, homogenize, and drop the obtained liposome suspension B into the TMC solution In C (0.1%, w / v), incubate for 1 h to obtain curcumin-coated liposome suspension D of the present invention.

[0037] The encapsulation efficiency of the obtained liposome was 9.21%, and the drug loading capacity was 0.445%.

Embodiment 2

[0039]Accurately weigh 10 mg of curcumin, 200 mg of soybean lecithin, and 10 mg of cholesterol, add them to 30 ml of absolute ethanol, remove the ethanol by rotary evaporation under reduced pressure at 40 ° C, dry in a vacuum oven overnight, add 20 ml of phosphate buffer saline (PBS, pH 5-7) Carry out hydration, centrifuge to remove the crystalline drug, filter the obtained liposome suspension A through a 0.8 μm microporous membrane, homogenize, and drop the obtained liposome suspension B into the TMC In solution C (0.2%, w / v), incubate for 1 h to obtain curcumin-coated liposome suspension D of the present invention. Take 2ml of the prepared suspension D, add mannitol (1%, w / v), put it into a vial, pre-freeze in the refrigerator at -80°C for 24h, and then put it in a freeze dryer at -40°C, 0.10mbar for 48h A lyophilized preparation is obtained.

[0040] Take an appropriate amount of the suspension, drop it on the copper grid, carry out negative staining with 2% phosphotungsti...

Embodiment 3

[0042] Accurately weigh 10mg of curcumin, 400mg of soybean lecithin, 20mg of Pluronic F127 (PF127), add to 20ml of ethyl acetate, remove the organic solvent by rotary evaporation under reduced pressure at 40°C, dry in a vacuum oven overnight, add 20ml of phosphoric acid Salt buffer solution (PBS, pH 5-7) was hydrated, centrifuged to remove crystalline drug, and the obtained liposome suspension A was filtered through a 0.8 μm microporous membrane, homogenized, and the obtained liposome suspension was B was added dropwise into TMC solution C (0.5%, w / v), and incubated for 2 hours to obtain curcumin-coated liposome suspension D of the present invention. Take 2ml of the prepared suspension D, add sucrose (4%, w / v), put it into a vial, pre-freeze in the refrigerator at -80°C for 24h, and then put it in a freeze dryer at -40°C, 0.10mbar for 48h A lyophilized preparation is obtained.

[0043] The zeta potential measurement results showed that the coated liposome was +15.64mV, and th...

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Abstract

The invention relates to a curcumin coated liposome preparation and a preparation method thereof. The curcumin coated liposome preparation consists of curcumin, phospholipids, cholesterol, water-soluble vitamin E and trimethyl chitosan, and can be prepared into freeze-dried powder applied to oral administration. The gastrointestinal absorption efficiency of the curcumin coated liposome is significantly higher than that of the traditional curcumin liposome preparation, so the curcumin coated liposome further improves the oral absorption of the curcumin and improve the oral bioavailability.

Description

technical field [0001] The invention relates to a curcumin-coated liposome preparation and a preparation method thereof, belonging to the technical field of medical application. Background technique [0002] Curcumin (curcumin) is a natural active ingredient extracted from the rhizomes of turmeric, curcuma, turmeric, etc. 21 h 20 o 6 . Pharmacological experiments have shown that in addition to anti-inflammatory, anti-cancer, and anti-oxidative effects, curcumin also has various pharmacological effects such as protecting the kidney, inhibiting pulmonary fibrosis, inhibiting liver fibrosis, helping muscle damage repair, treating cataracts, and anti-parasitic diseases , and the toxic and side effects are small, safe to use, and have good prospects for clinical application. However, curcumin is almost insoluble in water and poor in fat solubility, so it has little absorption through the gastrointestinal tract and low oral bioavailability. Therefore, improving the oral absor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/12A61K47/36A61K47/28A61K47/24A61P1/16A61P11/00A61P13/12A61P21/00A61P27/12A61P33/14A61P29/00A61P35/00A61P39/06
Inventor 翟光喜陈焕蕾
Owner SHANDONG UNIV
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