CN108096218A - A kind of nano particle for carrying saikosaponin-a and preparation method thereof - Google Patents
A kind of nano particle for carrying saikosaponin-a and preparation method thereof Download PDFInfo
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/51—Nanocapsules; Nanoparticles
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- A61K9/513—Organic macromolecular compounds; Dendrimers
- A61K9/5146—Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
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- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
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Abstract
The invention discloses a kind of nano particles for carrying saikosaponin-a and preparation method thereof, and carrying saikosaponin-a nano particle includes carrier and drug saikosaponin-a, wherein the carrier is the block copolymer of PCL and PEG.The particle diameter distribution of present invention gained load SSa nano particles is measured with dynamic light scattering (DLS) and shows charge, and it observes the size of nano particle with scanning electron microscope (SEM) and shows pattern, it can be seen that diameter of carrier prepared by the present invention is distributed mainly in 100nm or so, it is dispersed preferable, meet the requirement of nanometer formulation.The method of the present invention is simple and practicable, it is of low cost, be easy to be prepared on a large scale.Medicine technology is passed using nanometer, improves the dissolubility of saikosaponin-a in water, hemolytic is reduced, so as to reduce the toxic side effect of saikosaponin-a.
Description
Technical field
The invention belongs to biological technical fields, and in particular to carry nano particle of saikosaponin-a and preparation method thereof, especially
It is related to a kind of block copolymer using PCL and PEG as nano particle of load saikosaponin-a of carrier and preparation method thereof.
Background technology
Saikosaponin-a (saikosaponin a, SSa), belongs to pentacyclic triterpene saponin constituent, molecular formula is
C42H68O13, molecular weight 780.98；With anti-epileptic, anticonvulsion, Anti cell adhesion, analgesic, anti-inflammatory, antibacterial, liver protection, shield kidney,
The multiple pharmacological effects such as anticancer, antiviral.In terms of medicine is for characteristic research, SSa presents following feature:Although (l) SSa
There is certain dissolubility, but it is very low；Additionally, since its molecular weight is larger, it is difficult to through biomembrane, therefore, oral bio profit
Expenditure is very low, less than 1%.(2) SSa is made of the aglycon and 2 glycan molecules of three Xue of five rings, after oral medication, easily by
To the effect of intestinal flora, a series of variations such as hydrolysis occur, become secondary glucoside or aglycon.Change administration route, using note
It is the preferred approach for solving the problems, such as that its bioavilability is low to penetrate administration, but SSa, which is simply injected, can cause serious haemolysis anti-
Should, there are great security risks.Therefore, suitable drug delivery system is selected, while its bioavilability is improved, drop
Its low hemolytic toxicity is the key point of research.In terms of preparation process, domestic and international main direction of studying concentrates on radix bupleuri compound
Or total saikosaponins, and it is very few to the research of its active ingredient SSa.The Bupleurum injection listed at present, is to wave radix bupleuri
Hair oil manufactured sterile water solution after Tween 80 solubilising, but Tween-80 has haemocylolysis and cannot be injected intravenously, and radix bupleuri is noted
It is stronger to penetrate the irritation of liquid, patient feels apparent pain.There is scholar once to attempt to change using solid dispersion technology, inclusion technique
The dissolubility of kind SSa can dramatically increase dissolubility but its bioavilability still very little using two base P-CD of hydroxyl inclusions.Therefore,
A kind of dissolubility that can improve dewatering medicament saikosaponin-a is provided, improves its biological safety, while has and biological can drop
The drug delivery system of the advantages that solution, good biocompatibility is required at present.
The content of the invention
The present invention contains saikosaponin-a, and it is an object of the present invention to provide a kind of load SSa by the use of PCL-PEG diblocks as carrier for the first time
Nano particle, so as to improve the water solubility of SSa, reduce its hemolytic, reduce its toxic side effect to human body, improve drug
Stability, effectively extend Half-life in vivo.
It is to provide a kind of nano particle for carrying saikosaponin-a on the purpose of the present invention.
It is to provide a kind of preparation method for the nano particle for carrying saikosaponin-a on the purpose of the present invention.
The technical solution used in the present invention is：
A kind of nano particle for carrying saikosaponin-a, the nano particle contain drug saikosaponin-a and carrier, the carrier
For polycaprolactone and the block copolymer of polyethylene glycol, the mass ratio of the carrier and drug saikosaponin-a is (7~25)：1.
Further, the average molecular weight of polyethylene glycol is 500~8000 in the carrier, the mean molecule of polycaprolactone
It measures as 8000~30000.
A kind of preparation method for the nano particle for carrying saikosaponin-a, comprises the following steps：
1) by PEG-PCL solution and saikosaponin-a solution mixing, A phases are denoted as；Sodium cholate solution is taken, is denoted as B phases, adds in A
Xiang Zhong, after supersound process O/W lotions；
2) sodium cholate solution is added into O/W lotions, stirs curing nano particle；Rotatory vacuum is evaporated in solution
Organic solvent；
3) for the solution after evaporating using filter, ultrafiltration centrifugal concentrating, gained concentrate adds water, repeats ultrafiltration centrifugation
Concentration obtains the solution with blue-opalescent, as carries the nano particle of saikosaponin-a.
Further, in step 1), the concentration of the PEG-PCL solution is 10~120mg/mL.
Further, in step 1), the concentration of saikosaponin-a solution is 5~25mg/mL.
Further, in step 1), the mass ratio of PEG-PCL and saikosaponin-a is (7~25)：1.
Further, in step 1), the concentration of the sodium cholate solution is 0.5~2%w/v.
Further, in step 1), the volume ratio of A phases and B phases is 1~5：1.
Further, in step 2), the concentration of sodium cholate solution is 0.1~0.9%w/v.
Further, in step 2), the volume ratio of O/W lotions and sodium cholate solution is 1：8~25.
The beneficial effects of the invention are as follows：
(1) present invention has following advantages compared with prior art：Medicine technology is passed using nanometer, structure carries the nanometer of SSa
Particle improves the water solubility of SSa, slow release, reduces the problems such as hemolytic, so as to reduce the toxic side effect of saikosaponin-a.The party
Method easy, favorable repeatability convenient and simple for operation, it is of low cost, be easy to be prepared on a large scale.
(2) measure the particle diameter distribution of present invention gained load SSa nano particles with dynamic light scattering (DLS) and show charge,
It and observes the size of nano particle with scanning electron microscope (SEM) and shows pattern, it is seen that diameter of carrier distribution master prepared by the present invention
Will be in 100nm or so, dispersiveness preferably, meets the requirement of nanometer formulation.
Description of the drawings
The PEG-PCL polymer of Fig. 1 after purification1H-NMR is analyzed；
Fig. 2 is the grain size distribution of shown load SSa nano particles；
Fig. 3 is the surface charge figure of shown load SSa nano particles；
Fig. 4 is the scanning electron microscope (SEM) photograph for carrying SSa nano particles.
Fig. 5 is load SSa nano particle release profiles
Specific embodiment
A kind of nano particle for carrying saikosaponin-a, the nano particle contain drug saikosaponin-a and carrier, the carrier
For polycaprolactone and the block copolymer of polyethylene glycol, the mass ratio of the carrier and drug saikosaponin-a is (7~25)：1.
Preferably, the average molecular weight of polyethylene glycol is 500~8000 in the carrier, the average molecular weight of polycaprolactone
For 8000~30000.
A kind of preparation method for the nano particle for carrying saikosaponin-a, comprises the following steps：
1) by PEG-PCL solution and saikosaponin-a solution mixing, A phases are denoted as；Sodium cholate solution is taken, is denoted as B phases, adds in A
Xiang Zhong, after supersound process O/W lotions；
2) sodium cholate solution is added into O/W lotions, stirs curing nano particle；Rotatory vacuum is evaporated in solution
Organic solvent；
3) for the solution after evaporating using filter, ultrafiltration centrifugal concentrating, gained concentrate adds water, repeats ultrafiltration centrifugation
Concentration obtains the solution with blue-opalescent, as carries the nano particle of saikosaponin-a.
Preferably, in step 1), the concentration of the PEG-PCL solution is 10~120mg/mL.
Preferably, in step 1), the solvent of the PEG-PCL solution is selected from least one of dichloromethane, chloroform.
Preferably, in step 1), the concentration of saikosaponin-a solution is 5~25mg/mL.
Preferably, in step 1), the solvent of saikosaponin-a solution is selected from least one of ethyl alcohol, methanol.
Preferably, in step 1), the mass ratio of PEG-PCL and saikosaponin-a is (7~25)：1, more preferably (8~
12)：1.
Preferably, in step 1), the concentration of the sodium cholate solution is 0.5~2%w/v.
Preferably, in step 1), the volume ratio of A phases and B phases is 1~5：1.
Preferably, in step 1), the power of supersound process is 150~250w, and processing time is 0.5~15min.
Preferably, in step 2), the concentration of sodium cholate solution is 0.1~0.9%w/v.
Preferably, in step 2), the volume ratio of O/W lotions and sodium cholate solution is 1：8~25.
Preferably, in step 2), mixing time is 4~6min.
Preferably, in step 3), the filtering is 0.18~0.24 μm of hole membrane filtration using aperture.
Preferably, in step 3), the molecular cut off of the ultrafiltration centrifugation is more than 3500.
Preferably, in step 3), the centrifugal force of ultrafiltration centrifugation is 4500~5500g, centrifugation time for 17~
34min, temperature are 2~6 DEG C.
Preferably, in step 1), the preparation method of the PEG-PCL is：6-caprolactone and Me-PEG are mixed, with octanoic acid
Stannous is catalyst, under nitrogen protection, in 120~140 DEG C be stirred to react 18~26 it is small when, product is dissolved with dichloromethane
Afterwards, add in methanol extraction, will precipitate it is vacuum dried after, obtain the PEG-PCL polymer of purifying.
Preferably, the mass ratio of 6-caprolactone and Me-PEG are 2~10:1.
Preferably, the average molecular weight of polyethylene glycol is 500~8000 in the PEG-PCL polymer, polycaprolactone
Average molecular weight is 8000~30000.
With reference to specific embodiment, the present invention is further illustrated.
Embodiment 1：A kind of preparation method for the nano particle for carrying saikosaponin-a
(1) synthetic vectors PEG-PCL
Carrier synthesis step is as follows：Take 6-caprolactone (ε-CL) 24g, Me-PEG 4g mixing (ε-CL and polyethylene glycol PEG
Mass ratio be 6:1), the stannous octoate of 0.1% overall reaction system quality is as catalyst, and under nitrogen protection, slow machinery stirs
It mixes, when 130 DEG C of reactions 24 are small, obtains brown polymer P EG-PCL.Polymer 1.4g is weighed, adds in the dissolving of 2ml dichloromethane
Afterwards, a large amount of (about 100ml) methanol extractions are added in, remove the epsilon caprolactone homopolymer of unreacted 6-caprolactone and formation, weight
It precipitates 3 times again.Be deposited in 40 DEG C of vacuum drying 48 it is small when after, finally obtain PEG-PCL polymer after purification1H-NMR points
As shown in Figure 1, the average molecular weight of polyethylene glycol is 2000 in the carrier, the average molecular weight of polycaprolactone is 13000 for analysis.Production
Object is yellow-white, dry Cord blood.
(2) nano particle for carrying SSa is prepared
The carrier material PCL-PEG of 90mg is weighed, the methylene chloride of 1mL is added in, it is made fully to dissolve, is added in
The SSa anhydrous alcohol solution 1mL mixings of 10mg/mL, obtain A phases；And then, 1% (w/v) sodium cholate solution (B phases) is taken to be slowly added to
In above-mentioned solution, the volume ratio of wherein A phases and B phases is 2：1；Then it is ultrasonically treated 5 minutes under 200w, it is milky white forms O/W types
Obtained O/W lotions are diluted further to the 0.5%w/v sodium cholate solutions of 15 times of volumes, then stirred at room temperature by color emulsion
5 minutes magnetic stirrers are mixed with curing nano particle.Afterwards, the organic solvent (dichloromethane and absolute ethyl alcohol) of addition passes through rotation
Turn to be evaporated in vacuo.After solution is by 0.22um filtering with microporous membrane, it is dense that ultrafiltration centrifugation is carried out using Millipore ultra-filtration centrifuge tubes
Contracting, 4 DEG C of centrifugation 30min of 5000g, takes concentrate, fills it up with deionization washing, repeat ultrafiltration and centrifuge twice, obtain with blueness
The solution of opalescence as carries SSa nano particles.
The effect of the load SSa nano particles prepared below to the present invention makees further detection.
First, dynamic light scattering experiment (DLS)
The particle diameter distribution of load SSa nano particles prepared by the present invention is measured with dynamic light scattering (DLS) method and shows charge,
Testing result is as shown in Figures 2 and 3.As can be seen from Figure 2 the diameter of carrier distribution that prepared by the present invention is mainly left in 100nm
The right side, dispersiveness preferably, meet the requirement of nanometer formulation.From figure 3, it can be seen that load SSa nano particle tables prepared by the present invention
Face current potential is -25.77mV, and what can relatively be stablized is present in suspension.
2nd, scanning electron microscope detects
Scanning electron microscope (SEM) observes the size and surface topography of nano particle of the present invention.As shown in figure 4, further confirmation
Fig. 2's as a result, nano particle is circle under mirror, and size is homogeneous, good dispersion.
3rd, hemolysis rate detects
Method：Hemolysis in vitro experiment is carried out using sterile de- fiber blood of goats, it is red thin with the sheep of normal saline 2%
Cell lysis liquid carries SSa nano particles when 37 DEG C of incubations 1 are small with the SSa or the present invention of various concentration, 4 DEG C, 800g centrifugation 15min,
Supernatant is collected, is measured with ultraviolet specrophotometer at 540nm and calculates hemolysis rate.
As a result：Testing result is as shown in table 1, there it can be seen that the present invention carries SSa nano particles in 10~100 μ g/ml
Concentration range in show extremely low hemolysis rate, be respectively 0.78 ± 0.13%, 3.26 ± 0.17%.Illustrate energy of the present invention
Improve the water solubility of SSa, reduce its hemolytic, reduce its toxic side effect to human body, improve the stability of drug, effectively extend
Half-life in vivo.
1 present invention of table carries the hemolysis rate testing result of SSa nano particles
4th, release in vitro detects
Method：The release in vitro behavior for carrying SSa nano particles is investigated using dialysis.Dissolution medium is containing 5%Tween-
20 PBS (0.01mol/L, pH7.4), this release test design to ensure that drug release is carried out under sink condition.Take lmL
Drug-carrying nanometer particle solution is added in preswollen bag filter (MWCO=3500Da), tightens sack, is put into and is discharged equipped with 40mL
In the container of medium, in 37 DEG C, 100rpm vibrations carry out release experiment.Respectively at 1,2,4,6,8,10,12,24,48,72,96,
120h samples 1mL, while fills into 37 DEG C of blank dissolution mediums of equivalent, measures the SSa concentration in release sample.Calculate SSa accumulations
Discharge percentage.SSa is as a control group.
As a result：For testing result as shown in figure 5,24 is interior when small, SSa (free SSa) and the present invention carry SSa nano particles
The accumulative release rate of (MePEG-PCL SSa) is respectively 85.0 ± 2.95% and 19.6 ± 1.94%, 120 it is small when after, the present invention
The accumulative release rate for carrying SSa nano particles reaches 75.7 ± 4.8%, illustrates that the present invention carries SSa nano particles and can continue slowly
SSa is discharged, without phenomenon of burst release.
Embodiment 2：A kind of preparation method for the nano particle for carrying saikosaponin-a
(1) synthetic vectors PEG-PCL
Carrier synthesis step is as follows：6-caprolactone (ε-CL) and Me-PEG is taken to mix (the quality of ε-CL and polyethylene glycol PEG
Than for 10:1), the stannous octoate of 0.1% overall reaction system quality is as catalyst, under nitrogen protection, slow mechanical agitation, and 120
DEG C reaction 18 it is small when, obtain brown polymer P EG-PCL.Brown polymer 1.4g is weighed, after adding in the dissolving of 2ml dichloromethane,
A large amount of (about 100ml) methanol extractions are added in, remove the epsilon caprolactone homopolymer of unreacted 6-caprolactone and formation, it is heavy to repeat
It forms sediment 3 times.Be deposited in 40 DEG C of vacuum drying 48 it is small when after, finally obtain PEG-PCL polymer supports after purification, gather in the carrier
The average molecular weight of ethylene glycol is 8000, and the average molecular weight of polycaprolactone is 30000.Product is yellow-white, and dry low temperature is protected
It deposits.
(2) nano particle for carrying SSa is prepared
The carrier material PCL-PEG of 120mg is weighed, the methylene chloride of 1mL is added in, it is made fully to dissolve, is added in
The SSa anhydrous alcohol solution 0.5mL mixings of 25mg/mL, obtain A phases；And then, take 0.5% (w/v) sodium cholate solution (B phases) slow
It adds in above-mentioned solution, the volume ratio of wherein A phases and B phases is 5：1；Then it is ultrasonically treated 15 minutes under 200w, forms O/W types
Obtained O/W lotions are diluted further to the 0.1%w/v sodium cholate solutions of 25 times of volumes, then in room temperature by milky emulsion
4 minutes magnetic stirrers of lower stirring are with curing nano particle.Afterwards, the organic solvent (dichloromethane and absolute ethyl alcohol) of addition is logical
Rotation is crossed to be evaporated in vacuo.After solution is by 0.22um filtering with microporous membrane, using Millipore ultra-filtration centrifuge tubes carry out ultrafiltration from
The heart concentrates (molecular cut off 3500), and 6 DEG C of centrifugation 17min of 5500g take concentrate, fill it up with deionization washing, repeat super
Twice of filter centrifugation, obtains the solution with blue-opalescent, as carries SSa nano particles.
Above-described embodiment is the preferable embodiment of the present invention, but embodiments of the present invention and from above-described embodiment
Limitation, other any Spirit Essences without departing from the present invention with made under principle change, modification, replacement, combine, simplification,
Equivalent substitute mode is should be, is included within protection scope of the present invention.
Embodiment 3：A kind of preparation method for the nano particle for carrying saikosaponin-a
(1) synthetic vectors PEG-PCL
Carrier synthesis step is as follows：6-caprolactone (ε-CL) and Me-PEG is taken to mix (the quality of ε-CL and polyethylene glycol PEG
Than for 2:1), the stannous octoate of 0.1% overall reaction system quality is as catalyst, under nitrogen protection, slow mechanical agitation, and 140
DEG C reaction 26 it is small when, obtain brown polymer P EG-PCL.Brown polymer 1.4g is weighed, after adding in the dissolving of 2ml dichloromethane,
A large amount of (about 100ml) methanol extractions are added in, remove the epsilon caprolactone homopolymer of unreacted 6-caprolactone and formation, it is heavy to repeat
It forms sediment 3 times.Be deposited in 40 DEG C of vacuum drying 48 it is small when after, finally obtain PEG-PCL polymer supports after purification, gather in the carrier
The average molecular weight of ethylene glycol is 500, and the average molecular weight of polycaprolactone is 8000.Product is yellow-white, dry Cord blood.
(2) nano particle for carrying SSa is prepared
The carrier material PCL-PEG of 10mg is weighed, the methylene chloride of 1mL is added in, it is made fully to dissolve, adds in 5mg/
The SSa anhydrous alcohol solution 0.2mL mixings of mL, obtain A phases；And then, 2% (w/v) sodium cholate solution (B phases) is taken to be slowly added to above-mentioned
In solution, the volume ratio of wherein A phases and B phases is 1：1；Then it is ultrasonically treated 0.5 minute under 250w, forms O/W type milkys
Obtained O/W lotions are diluted further to the 0.9%w/v sodium cholate solutions of 8 times of volumes, are then stirred at room temperature 6 by emulsion
Minute, magnetic stirrer was with curing nano particle.Afterwards, the organic solvent (dichloromethane and absolute ethyl alcohol) of addition passes through rotation
It is evaporated in vacuo.After solution is by 0.24um filtering with microporous membrane, ultrafiltration centrifugal concentrating is carried out using Millipore ultra-filtration centrifuge tubes
(molecular cut off 3500), 2 DEG C of centrifugation 34min of 4500g, takes concentrate, fills it up with deionization washing, repeat ultrafiltration centrifugation
Twice, the solution with blue-opalescent is obtained, as carries SSa nano particles.
Above-described embodiment is the preferable embodiment of the present invention, but embodiments of the present invention and from above-described embodiment
Limitation, other any Spirit Essences without departing from the present invention with made under principle change, modification, replacement, combine, simplification,
Equivalent substitute mode is should be, is included within protection scope of the present invention.
Claims (10)
1. a kind of nano particle for carrying saikosaponin-a, which is characterized in that the nano particle contains drug saikosaponin-a and carrier,
The carrier is the block copolymer of polycaprolactone and polyethylene glycol, and the mass ratio of the carrier and drug saikosaponin-a is (7
~25)：1.
2. the nano particle according to claim 1 for carrying saikosaponin-a, which is characterized in that polyethylene glycol in the carrier
Average molecular weight for 500~8000, the average molecular weight of polycaprolactone is 8000~30000.
3. a kind of preparation method for the nano particle for carrying saikosaponin-a, which is characterized in that comprise the following steps：
1) by PEG-PCL solution and saikosaponin-a solution mixing, A phases are denoted as；Sodium cholate solution is taken, is denoted as B phases, adds in A phases
In, O/W lotions are obtained after supersound process；
2) sodium cholate solution is added into O/W lotions, stirs curing nano particle；Rotatory vacuum evaporates organic in solution
Solvent；
3) for the solution after evaporating using filter, ultrafiltration centrifugal concentrating, gained concentrate adds water, and it is dense to repeat ultrafiltration centrifugation
Contracting obtains the solution with blue-opalescent, as carries the nano particle of saikosaponin-a.
4. according to the method described in claim 3, it is characterized in that, in step 1), the concentration of the PEG-PCL solution for 10~
120mg/mL。
5. according to the method described in claim 3, it is characterized in that, in step 1), the concentration of saikosaponin-a solution for 5~
25mg/mL。
6. according to the method described in claim 3, it is characterized in that, in step 1), the mass ratio of PEG-PCL and saikosaponin-a
For (7~25)：1.
7. according to the method described in claim 3, it is characterized in that, in step 1), the concentration of the sodium cholate solution for 0.5~
2%w/v.
8. according to the method described in claim 3, it is characterized in that, in step 1), the volume ratio of A phases and B phases is 1~5：1.
9. according to the method described in claim 3, it is characterized in that, in step 2), the concentration of sodium cholate solution for 0.1~
0.9%w/v.
10. according to the method described in claim 3, it is characterized in that, in step 2), the volume of O/W lotions and sodium cholate solution
Than for 1：8~25.
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| CN117327262A (en) * | 2023-09-06 | 2024-01-02 | 中山大学附属第三医院 | Responsive nano-drug carrier and preparation and application thereof |
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| 张国松: "靶向星形细胞的柴胡皂苷a、柴胡皂苷d复方脂质体制备工艺研究及体内外评价", 《中国博士学位论文全文数据库 医药卫生科技辑》 * |
| 郭曼曼等: "姜黄素PEG-PCL纳米粒的制备及药动学和体外抑瘤作用研究", 《2013抗肿瘤药物研究新进展与肿瘤个性化药物治疗论坛论文集》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN117327262A (en) * | 2023-09-06 | 2024-01-02 | 中山大学附属第三医院 | Responsive nano-drug carrier and preparation and application thereof |
| CN117327262B (en) * | 2023-09-06 | 2024-06-14 | 中山大学附属第三医院 | Responsive nano-drug carrier and preparation and application thereof |
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