Borneol-curcumin liposome and preparation method and application thereof

A technology of curcumin fat and curcumin, which is applied in the field of medicine, can solve the problems of difficulty in clinical application of curcumin, poor water solubility of curcumin, and easy oxidation, etc., so as to improve the central drug effect and bioavailability, have no toxic side effects, good effect

Active Publication Date: 2013-01-30
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, curcumin has poor water solubility, is easily oxidized in vitro, and is difficult to pass through the blood-brain barrier and enter the brain parenchyma. Most curcumin administered orally is metabolized in the gastrointestinal tract, which brings certain difficulties to the clinical application of curcumin in the prevention and treatment of HAND.

Method used

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  • Borneol-curcumin liposome and preparation method and application thereof
  • Borneol-curcumin liposome and preparation method and application thereof
  • Borneol-curcumin liposome and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The preparation of embodiment 1 Borneolum-curcumin liposome

[0031] Dissolve 3g of lecithin, 1g of cholesterol, 10mg of curcumin, 1mg of borneol and 100mg of vitamin E in absolute ethanol, and spin evaporate on a rotary evaporator in a constant temperature water bath at 35°C until the absolute ethanol is completely volatilized to form a uniform film; Add 5mL of 0.03mol / L PBS (pH 7.0), incubate at 35°C for 3h, rotate and hydrate on a rotary evaporator at 35°C in a constant temperature water bath to form a milky solution; ultrasonicate the milky solution at 80KHz for 10min, and then pass through a 0.45μm micro The whole particle of pore filter membrane obtains borneol-curcumin liposome. The encapsulation efficiency of the obtained borneol-curcumin liposome was determined to be about 75% by spectrophotometry (detection wavelength: 424nm).

Embodiment 2

[0032] Embodiment 2 different preparation medicine enters the comparison of SD rat blood and brain tissue speed

[0033] Sprague-Dawley (SD) adult male and female rats were divided into curcumin group, curcumin liposome group and borneol-curcumin liposome group, with 8 male and half male rats in each group, and curcumin monomer was administered by intragastric administration respectively (10mg curcumin is dissolved in the PBS of 5mL pH 7.0,0.03mol / L to obtain curcumin), curcumin liposomes (prepared by the conditions of Example 1 without borneol to obtain curcumin liposomes), borneol-curcumin lipid Plastids (prepared in Example 1), 5mL / piece. 15, 30, 45, 60, 90, 120, 150min after the administration, the tail was docked to take blood and the concentration of curcumin in the blood was measured by high performance liquid chromatography, with time as the abscissa and the concentration of curcumin in the blood as the ordinate, to prepare Drug concentration-time curve. The result i...

Embodiment 3

[0039] Example 3 Effects of Different Preparation Drugs on Learning and Memory Impairment in Rats Caused by gp120

[0040] The spatial learning ability of the rats in each group was detected by using the Morris water maze. The experimental animals were SD adult male and female rats, 15 in each group, randomly selected, and grouped as follows:

[0041] Control group: no intubation in the lateral ventricle + gavage with double distilled water;

[0042] Sham operation group: lateral ventricle intubation + artificial rat cerebrospinal fluid + double distilled water gavage;

[0043] Model group (gp120): lateral ventricle intubation + gp120 + double distilled water gavage;

[0044] gp120+ curcumin monomer group: lateral ventricle intubation + gp120+ curcumin monomer gavage;

[0045] gp120+ curcumin liposome group: lateral ventricle intubation + gp120+ curcumin liposome gavage;

[0046] gp120+borneol-curcumin liposome group: lateral ventricle intubation+gp120+borneol-curcumin lipo...

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Abstract

The invention belongs to the medicine field and provides a borneol-curcumin liposome, a preparation method of the borneol-curcumin liposome and an application of the borneol-curcumin liposome in preparing medicines for preventing human immunodeficiency virus-1(HIV-1) associated neurocognitive disorder. The borneol-curcumin liposome is prepared by, by mass, 270-330 parts of lecithin, 90-110 parts of cholesterol, 0.9-1.1 parts of curcumin and 0.09-0.11 part of borneol. The preparation method includes that the components and 0-11 parts by mass of oxidation protection agents are dissolved by absolute ethyl alcohol, a mixture is subjected to rotary evaporating on a rotary evaporator until ethanol is volatilized to form uniform films, a defined amount of phosphate buffer solution is added, the incubation is performed for three hours, a hydration reaction is undertaken to form an emulsion, then the ultrasound is performed for 10 minutes, and the emulsion passes through a 0.45 micrometer millipore filter to obtain uniform particles so that the borneol-curcumin liposome is obtained. The borneol-curcumin liposome can be prepared to various dosage forms of HIV-associated neurocognitive disorder (HAND) resistant medicines which are peroral, and the pertinence of the borneol-curcumin liposome for treating HAND is high, and the effect is good.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a drug for resisting HIV-1-related neurocognitive disorders, in particular to a borneol-curcumin liposome and its preparation method and its use in the preparation of anti-HIV-1-related neurocognitive disorder drugs Applications. Background technique [0002] The World Health Organization (WHO) believes that HIV (human immunodeficiency virus) disease is currently the greatest threat to public health. At present, there are about 60 million HIV-infected people in the world, and 25 million people have died of AIDS-related diseases. According to the evaluation results of the Ministry of Health, UNAIDS, and WHO, as of the end of 2011, there were about 780,000 living infected and patients in my country, including about 154,000 patients and about 80,000 deaths. In the global AIDS caused by HIV-1, due to the existence of progressive viral infection, about 40-60% of HIV patients develop HIV-associ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/12A61K47/10A61K47/28A61P25/28
Inventor 董军邓钦莹
Owner JINAN UNIVERSITY
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