CN107582524A - The preparation method of PluronicF87 curcumin liposomes - Google Patents
The preparation method of PluronicF87 curcumin liposomes Download PDFInfo
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- CN107582524A CN107582524A CN201710931002.6A CN201710931002A CN107582524A CN 107582524 A CN107582524 A CN 107582524A CN 201710931002 A CN201710931002 A CN 201710931002A CN 107582524 A CN107582524 A CN 107582524A
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- curcumin
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Abstract
The invention belongs to biomedicine field, more particularly to a kind of preparation method of Pluronic F87 curcumin liposomes, it is using phosphatide, cholesterol, Pluronic F87 and curcumin as raw material, using film dispersion method combination dynamic high-pressure microjet, the Pluronic F87 curcumin liposomes prepared through processing such as dissolving, film forming, aquation and dynamic high-pressure microjets.The particle diameter of Pluronic F87 curcumin liposomes prepared by the method is 59.0 ± 1.8nm, the coefficient of dispersion is 0.296 ± 0.001, envelop rate is 87.5 ± 2.6%, the curcumin liposome has particle diameter small, dispersion range is narrow, the advantages of stability is good, and there is good storage-stable, and the external digestion stability and bioavailability of traditional curcumin liposome can be improved.
Description
Technical field
The invention belongs to biomedicine field, and in particular to a kind of Pluronic F87 curcumin liposomes and its preparation side
Method.
Background technology
Curcumin (curcumin) is a kind of active skull cap components extracted from turmeric.In recent years research shows, turmeric
Element has extensive pharmacological action, such as antitumor, improvement cardiovascular function, anti-inflammatory, antiviral, liver protection, strengthen immunity, tool
Have good pharmacological activity and an application prospect, but curcumin exist poor poorly water-soluble, stability, oral bioavailability rate rate,
And the defects of being easily metabolized in vivo, therefore limit its application clinically.It is to improve turmeric using nanometer technology delivery
One of plain stability and the effective means of bioavailability.Wherein liposome is a kind of more carrier systems of research.
The inside that liposome is made up of amphiphilic material such as phosphatide is aqueous phase, has the bilayer of class membrane structure
Close vesica.Liposome has the advantages that slow release, cellular affinity and good biocompatibility, in biological medicine, food
The fields such as nutrition, cosmetics are widely used.Liposome can be used to improve the stability of medicine, bioavailability etc..But pass
There is unstability in system liposome, have the problems such as particle buildup, particle diameter change are big, drug leakage in storage.Therefore, carry
The stability of high liposome is one of current study hotspot.
The content of the invention
The invention aims to improve the stability and bioavailability of curcumin, there is provided a kind of practicality, safety, system
The preparation method of standby simple Pluronic F87 curcumin liposomes.
The concrete technology step of the present invention is as follows：
(1) mass ratio of each raw material is：Phosphatide：Cholesterol：Pluronic F87：Curcumin is 20:4:10:1；
(2) phosphatide, cholesterol and Pluronic F87 and curcumin are weighed by above-mentioned mass ratio, at a temperature of 50 DEG C, used
20mL absolute ethyl alcohols are completely dissolved each component；
(3) solution in step 2 being removed into absolute ethyl alcohol in revolving on Rotary Evaporators, each group forms uniform film, its
Middle bath temperature is 45 DEG C；
(4) add pure water progress aquation and wash film 30min, bath temperature is 45 DEG C, forms thick Liposomal suspensions；Add pure water
Phosphatide mass-volume concentration is that 2-2.5mg/mL is preferably 2.03mg/mL afterwards；
(5) the thick Liposomal suspensions 2 times in dynamic high-pressure microjet DHPM processing steps 4 are used, operating pressure is
120MPa, produce Pluronic F87 curcumin liposomes.
The present invention is using Pluronic F87 as dressing agent, using traditional film dispersion method combination dynamic high-pressure microjet skill
Art prepares Pluronic F87 curcumin liposomes, to improve the stability of curcumin liposome and bioavailability.
The beneficial effects of the invention are as follows：
(1) particle diameter and polydispersity：Conventional unmodified curcumin liposome (cur-Lps) average grain diameter for 95.4 ±
2.6nm, the coefficient of dispersion are 0.362 ± 0.026；Invented liposomes (cur-F87-Lps) are 59.0 ± 1.8nm, the coefficient of dispersion
Cur-Lps particle diameter and the coefficient of dispersion is can obviously reduce for 0.296 ± 0.001, Pluronic F87 modifications.
(2) envelop rate：The envelop rate of curcumin is up to 87.5 ± 2.6% in invented liposomes cur-F87-Lps.
(3) microscopic appearance：By transmission electron microscope observing invented liposomes cur-F87-Lps microscopic appearance, such as Fig. 1 institutes
Show.Cur-F87-Lps structure is spherical, and is evenly distributed.
(4) external digestion stability：Using curcumin as hydrophobicity model drug, by determining curcumin liposome and Ben Fa
Bright liposome Pluronic F87 nanocurcumins liposomes are through Mouthsimulator (10min), stomach (2h), small intestine (2h) digestion process
Retention rate is found, after simulating external digestion, the conversion ratio of curcumin liposome, the acceptable rate of biology and bioavailability divide
Not Wei 31.6 ± 4.0%, 73.3 ± 3.5% and 26.9 ± 2.6%, and invented liposomes Pluronic F87 modification curcumin
The conversion ratio of liposome, the acceptable rate of biology and bioavailability be respectively 37.2 ± 2.9%, 86.1 ± 3.8% and 32.7 ±
1.5%.Thus can find, Pluronic F87 can improve stability and biological utilisation of the liposome in vitro in digestion process
Rate.
Brief description of the drawings
Fig. 1 is the process route chart for preparing Pluronic F87 curcumin liposomes；
Fig. 2 is the grain size distribution of Pluronic F87 curcumin liposomes；
Fig. 3 is the transmission electron microscope picture of Pluronic F87 curcumin liposomes；
Fig. 4 is bioavailability of the Pluronic F87 curcumin liposomes in simulation external digestion.
Embodiment
Embodiment 1
1st, it is complete that 0.1015g phosphatide, 0.0201g cholesterol, 0.0239g Pluronic F87 and 0.0050g curcumins are weighed
Fully dissolved removes absolute ethyl alcohol in 20mL absolute ethyl alcohols, in 45 DEG C of water bath condition rotary evaporations, forms uniform film.Add
50mL deionized waters carry out aquation 30min, and the suspension of formation is thick liposome.The suspension carries out to dynamic high-pressure is micro- penetrates
Flow DHPM to handle 2 times, pressure 120Mpa, produce Pluronic F87 curcumin liposomes.
2nd, particle diameter and dispersiveness are investigated：With laser nano particle size analyzer determination particle diameter and dispersiveness.As a result show cur-Lps's
Average grain diameter is 94.9nm, and the coefficient of dispersion 0.371, cur-F87-Lps average grain diameter is 59.6nm, and the coefficient of dispersion is
0.297, as a result as shown in Figure 2.
3rd, the measure of curcumin envelop rate：Cur-F87-Lps is centrifuged into 10min under 8000rpm rotating speeds, takes supernatant to use
After ethanol dilution, absorbance is determined in 420nm with uv-spectrophotometric, calculating curcumin according to curcumin ethanol standard curve contains
Amount, the results showed that the envelop rate of curcumin is up to 89.3%.
4th, microscopic pattern is observed：Pluronic F87 nano-lipid liquid solutions are dripped on sealed membrane, copper mesh is placed in
Take out after 3min in drop, then taken out after being placed in 1% sodium phosphotungstate solution negative staining 2min, solution is sucked from edge with filter paper,
Dry, observed under transmission electron microscope (TEM) at room temperature.From electromicroscopic photograph, Pluronic F87 curcumin liposomes are in
Spherical, size is homogeneous.As a result it is as shown in Figure 3.
5th, external digestion stability：Oral digestion：Simulate saliva (simulated saliva fluid, SSF) (3mL) in
With curcumin Pluronic F87 nano liposomes (3mL) with 1 after 37 DEG C of preheating 5min:1 mixing, it is fast with 1.0mol/L hydrochloric acid
Mixed system is adjusted to pH 6.8 by speed, digests 10min in 37 DEG C of stirring in water bath (100rpm).Peptic digest：Simulate the gastric juice
(simulated gastric fluid, SGF) (6mL) 37 DEG C preheat 5min after, with the sample (6mL) after oral digestion with
1:1 mixing, is adjusted to pH 2.5, in 37 DEG C of stirring in water bath by mixed system rapidly with 1.0mol/L sodium hydroxide
(100rpm) digests 2h.Intestinal digestion：Simulated intestinal fluid (simulated intestine fluid, SIF)；Trypsin solution 24mg/
mL；Cholate solution 50mg/mL.12mL PBS (pH 6.8) and SIF (1.2mL) are after 37 DEG C preheat 5min, with above-mentioned digestive juice
Mixing, then it is separately added into 2.8mL cholate solution and 2mL trypsin solutions are well mixed, adjust pH with 1.0mol/L sodium hydroxide
To 7,2h is digested in 37 DEG C of stirring in water bath (100rpm).Postdigestive end-product centrifuges 30min under 15000rpm, takes supernatant
The content of its curcumin is determined with HPLC.External digestion experiment is simulated to show, Pluronic F87 nanocurcumin liposomes
The acceptable rate of conversion ratio, biology and bioavailability are respectively 39.5%, 86.9% and 34.3%.As a result it is as shown in Figure 4.
Claims (2)
1. a kind of preparation method of Pluronic F87 curcumin liposomes, it is characterised in that according to following steps：
(1) mass ratio of each raw material is：Phosphatide：Cholesterol：Pluronic F87：Curcumin is 20:4:10:1；
(2) phosphatide, cholesterol and Pluronic F87 and curcumin are weighed by above-mentioned mass ratio, at a temperature of 50 DEG C, uses 20mL
Absolute ethyl alcohol is completely dissolved each component；
(3) step 2 resulting solution is removed into absolute ethyl alcohol in revolving on Rotary Evaporators, forms uniform film；
(4) add pure water progress aquation and wash film 30min, bath temperature is 45 DEG C, forms thick Liposomal suspensions；Phosphorus after addition pure water
Fat mass-volume concentration is 2-2.5mg/mL；
(5) the thick Liposomal suspensions 2 times, operating pressure 120MPa in dynamic high-pressure microjet DHPM processing steps 4 are used, i.e.,
Obtain Pluronic F87 curcumin liposomes.
2. preparation method according to claim 1, it is characterised in that：Step (3) the outstanding steaming bath temperature is 45 DEG C.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109512785A (en) * | 2019-01-16 | 2019-03-26 | 江西科技师范大学 | A kind of preparation method of folic acid-Pluronic F87 modification curcumin nano-lipid body |
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2017
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109512785A (en) * | 2019-01-16 | 2019-03-26 | 江西科技师范大学 | A kind of preparation method of folic acid-Pluronic F87 modification curcumin nano-lipid body |
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