CN104398489A - Preparation method for nanocrystalized silybin-hydroxylapatite composite microcapsule - Google Patents
Preparation method for nanocrystalized silybin-hydroxylapatite composite microcapsule Download PDFInfo
- Publication number
- CN104398489A CN104398489A CN201410614631.2A CN201410614631A CN104398489A CN 104398489 A CN104398489 A CN 104398489A CN 201410614631 A CN201410614631 A CN 201410614631A CN 104398489 A CN104398489 A CN 104398489A
- Authority
- CN
- China
- Prior art keywords
- silybin
- silibinin
- preparation
- hydroxyapatite
- nanocrystalized
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 229910052588 hydroxylapatite Inorganic materials 0.000 title claims abstract description 27
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 239000003094 microcapsule Substances 0.000 title claims abstract description 13
- 239000002131 composite material Substances 0.000 title claims abstract description 11
- SEBFKMXJBCUCAI-HKTJVKLFSA-N silibinin Chemical compound C1=C(O)C(OC)=CC([C@@H]2[C@H](OC3=CC=C(C=C3O2)[C@@H]2[C@H](C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 SEBFKMXJBCUCAI-HKTJVKLFSA-N 0.000 claims abstract description 44
- SEBFKMXJBCUCAI-UHFFFAOYSA-N NSC 227190 Natural products C1=C(O)C(OC)=CC(C2C(OC3=CC=C(C=C3O2)C2C(C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 SEBFKMXJBCUCAI-UHFFFAOYSA-N 0.000 claims abstract description 39
- 235000014899 silybin Nutrition 0.000 claims abstract description 36
- 230000003993 interaction Effects 0.000 claims abstract description 3
- 239000000463 material Substances 0.000 claims abstract description 3
- 229950000628 silibinin Drugs 0.000 claims description 31
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 claims description 21
- 230000000975 bioactive effect Effects 0.000 claims description 5
- 150000001875 compounds Chemical class 0.000 claims description 5
- 150000002500 ions Chemical class 0.000 claims description 2
- FDQAOULAVFHKBX-UHFFFAOYSA-N Isosilybin A Natural products C1=C(O)C(OC)=CC(C2C(OC3=CC(=CC=C3O2)C2C(C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 FDQAOULAVFHKBX-UHFFFAOYSA-N 0.000 abstract description 7
- VLGROHBNWZUINI-UHFFFAOYSA-N Silybin Natural products COc1cc(ccc1O)C2OC3C=C(C=CC3OC2CO)C4Oc5cc(O)cc(O)c5C(=O)C4O VLGROHBNWZUINI-UHFFFAOYSA-N 0.000 abstract 5
- 229940043175 silybin Drugs 0.000 abstract 5
- CYGIJEJDYJOUAN-UHFFFAOYSA-N Isosilychristin Natural products C1=C(O)C(OC)=CC(C2C3C=C(C4C(C3=O)(O)OCC42)C2C(C(=O)C3=C(O)C=C(O)C=C3O2)O)=C1 CYGIJEJDYJOUAN-UHFFFAOYSA-N 0.000 description 4
- 239000000047 product Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 230000004071 biological effect Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 235000013376 functional food Nutrition 0.000 description 3
- 210000004185 liver Anatomy 0.000 description 3
- 229960004245 silymarin Drugs 0.000 description 3
- 235000017700 silymarin Nutrition 0.000 description 3
- 239000006228 supernatant Substances 0.000 description 3
- FDQAOULAVFHKBX-KMRPREKFSA-N (+)-Isosilybin A Natural products C1=C(O)C(OC)=CC([C@@H]2[C@H](OC3=CC(=CC=C3O2)[C@@H]2[C@@H](C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 FDQAOULAVFHKBX-KMRPREKFSA-N 0.000 description 2
- FDQAOULAVFHKBX-HKTJVKLFSA-N (2r,3r)-3,5,7-trihydroxy-2-[(2r,3r)-2-(4-hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-6-yl]-2,3-dihydrochromen-4-one Chemical compound C1=C(O)C(OC)=CC([C@@H]2[C@H](OC3=CC(=CC=C3O2)[C@@H]2[C@H](C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 FDQAOULAVFHKBX-HKTJVKLFSA-N 0.000 description 2
- KDMGQPNVTKUNHV-UHFFFAOYSA-N Isosilybin Natural products C1=C(O)C(OC)=CC=C1C1C(CO)OC2=CC=C(C3C(C(=O)C4=C(O)C=C(O)C=C4O3)O)C=C2O1 KDMGQPNVTKUNHV-UHFFFAOYSA-N 0.000 description 2
- RIAZZJBPJQWPIS-UHFFFAOYSA-N Silychristin Natural products COc1cc(ccc1O)C2OC3C(C=C(C=C3O)C4Oc5cc(O)cc(O)c5C(=O)C4O)C2CO RIAZZJBPJQWPIS-UHFFFAOYSA-N 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 230000003078 antioxidant effect Effects 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- BMLIIPOXVWESJG-LMBCONBSSA-N silychristin Chemical compound C1=C(O)C(OC)=CC([C@H]2[C@@H](C3=C(C(=CC(=C3)[C@@H]3[C@H](C(=O)C4=C(O)C=C(O)C=C4O3)O)O)O2)CO)=C1 BMLIIPOXVWESJG-LMBCONBSSA-N 0.000 description 2
- BMLIIPOXVWESJG-UHFFFAOYSA-N silychristin A Natural products C1=C(O)C(OC)=CC(C2C(C3=C(C(=CC(=C3)C3C(C(=O)C4=C(O)C=C(O)C=C4O3)O)O)O2)CO)=C1 BMLIIPOXVWESJG-UHFFFAOYSA-N 0.000 description 2
- CYGIJEJDYJOUAN-JSGXPVSSSA-N silydianin Chemical compound C1=C(O)C(OC)=CC([C@H]2[C@H]3C=C([C@@H]4[C@@](C3=O)(O)OC[C@@H]42)[C@@H]2[C@H](C(=O)C3=C(O)C=C(O)C=C3O2)O)=C1 CYGIJEJDYJOUAN-JSGXPVSSSA-N 0.000 description 2
- 238000001179 sorption measurement Methods 0.000 description 2
- 241000208838 Asteraceae Species 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- MZBGBHVFCYCYLX-UHFFFAOYSA-N Silydianin Natural products COc1cc(ccc1O)C2C3COC4(O)C3C=C(C5Oc6cc(O)cc(O)c6C(=O)C5O)C2C4=O MZBGBHVFCYCYLX-UHFFFAOYSA-N 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 230000003064 anti-oxidating effect Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 231100000481 chemical toxicant Toxicity 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 229960000935 dehydrated alcohol Drugs 0.000 description 1
- 239000008367 deionised water Substances 0.000 description 1
- 229910021641 deionized water Inorganic materials 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 230000002443 hepatoprotective effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 230000008929 regeneration Effects 0.000 description 1
- 238000011069 regeneration method Methods 0.000 description 1
- 229950004304 silidianin Drugs 0.000 description 1
- 239000012086 standard solution Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention provides a preparation method for a nanocrystalized silybin-hydroxylapatite composite microcapsule. Nano-hydroxyapatite (HAP) with good bioavailability and bioactivity is taken as a main material, and is compounded with silybin through ion-charge interaction. The preparation method concretely comprises: preparing a silybin solution with the concentration of 5600 mu g/mL, getting 5 mL of the prepared silybin solution, adding 5 mg of nano-hydroxyapatite (HAP), performing ultrasonic processing for 20 min, uniformly shaking in a shaking table at a rotation speed of 160 r/min at a temperature of 37 DEG C, so as to obtain a maximum loading capacity of silybin after nano-hydroxyapatite is added for 10 min, and further to successfully prepare the nanocrystalized silybin-hydroxylapatite composite microcapsule. The advantages comprise that the silybin structure can be relatively ideally stabilized, the bioactivity of silybin can be relatively ideally given play, and efficient utilization of functional molecules is realized, and the preparation method has extremely important research and practical significance for functional foodstuff, health-care products and biological medicinal application.
Description
Technical field
The present invention relates to the preparation method of microcapsule, particularly relate to a kind of preparation method of silibinin hydroxyapatite composite micro-capsule.
Background technology
Silymarin (Silymarin) refers to a kind of flavanolignan compounds extracting gained from the seed coat of the medicinal plants of Compositae Herba Silybi mariani seed, in yellow powder, and bitter in the mouth.Its molecular formula is as follows:
Main active component has four kinds of isomerss such as silibinin (Silybin), Isosilybin (Isosilybin), Silychristin (Silychristin) and silidianin (Silydianin), and wherein silibinin content is 50%-70%.Silymarin is used for treating the history that liver and gall diseases has more than 2000 year, the damage that silibinin can prevent chemical toxicant, sitotoxin and medicine etc. from causing liver as its main active component, promote hepatocellular regeneration and reparation, be called as " natural hepatoprotective "; As powerful antioxidant, the free radical in human body can be removed, slow down aging.In recent years, due to silibinin demonstrate protect the liver with antioxidation beyond activity and receive much concern, the anticancer and tumor prevention effect that wherein silibinin shows has demonstrated good potentiality to be exploited.It is widely used in the products such as medicine, health product, foods and cosmetics.
Silibinin is the natural activity molecule with antitumor, antioxidant activity, but has poor stability, easily degraded, shortcoming that bioavailability is low, makes it be extremely restricted in the application in the field such as functional food, biomedicine.
How can comparatively ideal stable silibinin structure, play its biological activity, the efficiency utilization of practical function molecule, to functional food, health product and biomedical applications, all there is extremely important research and realistic meaning.
Summary of the invention
Technical problem to be solved of the present invention is the preparation method providing a kind of nanorize silibinin hydroxyapatite composite micro-capsule, can comparatively ideal stable silibinin structure, play its biological activity, the efficiency utilization of practical function molecule.
The present invention solves the problems of the technologies described above by the following technical solutions: a kind of preparation method of nanorize silibinin hydroxyapatite composite micro-capsule, selection has good biocompatibility, bioactive nanometer hydroxyapatite (HAP) is material of main part, carries out compound by ion, charge interaction to silibinin.
Concrete preparation method is: compound concentration is the silibinin of 5600ug/mL, get the silibinin solution 5mL prepared, and add 5mg nanometer hydroxyapatite (HAP), ultrasonic 20 minutes, shake up at the rotating speed of 160r/min, the temperature of 37 DEG C in shaking table, 10min after adding nanometer hydroxyapatite, the useful load of silibinin reaches maximum, and nanorize silibinin hydroxyapatite composite micro-capsule is successfully prepared.
The invention has the advantages that: can comparatively ideal stable silibinin structure, play its biological activity, the efficiency utilization of practical function molecule, to functional food, health product and biomedical applications, all there is extremely important research and realistic meaning.
Accompanying drawing explanation
Fig. 1 is the standard curve of silibinin.
Fig. 2 is the useful load curve of silibinin under variable concentrations.
Fig. 3 is the useful load curve of silibinin under different adsorption time.
Detailed description of the invention
Below in conjunction with accompanying drawing, the present invention is described in detail.
The making of 1 standard curve
Get 0.1mL, 0.2mL, 0.4mL, 0.8mL, 1.0mL silibinin respectively, put into 50mL volumetric flask, then add 19.9mL, 19.8mL, 19.6mL, 19.2mL, 19.0mL 75% dehydrated alcohol respectively.Be configured to the standard solution of 5ug/L, 10ug/L, 20ug/L, 40ug/L, 50ug/L respectively.The correlation coefficient r 2=0.9902 of standard curve, illustrates good relationship.
2, under variable concentrations silibinin molecule with the absorption of nanometer hydroxyapatite
Configure 50ug/mL respectively, 100ug/mL, 200ug/mL, 500ug/mL, 1000ug/mL, 1200ug/mL, 1400ug/mL, 1600ug/mL, 1800ug/mL, 2000ug/mL, 2200ug/mL, 2400ug/mL2600ug/mL, 2800ug/mL, 3000ug/mL, 3200ug/mL, 3400ug/mL, 3600ug/mL, 3800ug/mL, 4000ug/mL, 4200ug/mL, 4400ug/mL, 4600ug/mL, 5000ug/mL, 5200ug/mL, 5400ug/mL, 5600ug/mL, 5800ug/mL, the silibinin molecular solution of 6000ug/mL, therefrom take out 8mL in centrifuge tube, add 5mgHAP respectively, ultrasonic 20 minutes, at 160r/min in shaking table, 37 DEG C shake up 6h, and shake up once every the taking-up of 2h centrifuge tube.After having adsorbed, sample is placed in refrigerator and leaves standstill 12h (or centrifugal), get supernatant and carry out ultraviolet sign, it is stand-by that lower floor is placed on refrigerator.By standard curve, calculate useful load, and make correlation curve.
(1) useful load L (%)=(m1/W1) × 100%
M1: the quality of the bioactive molecule embedded in microcapsule
W1: the gross weight (being say dry state sample in theory) of complex
Useful load (mg/g): (amount of the bioactive molecule in the addition-supernatant of bioactive molecule)/complex weight
(2) from curve, when the concentration of silibinin is 5600ug/mL, useful load is most suitable is 898.78mg/g
2, under different time silibinin molecule with the absorption of nanometer hydroxyapatite
Preparation silibinin concentration is 5600ug/mL, gets solution 5mL, and adds 5mgHAP, ultrasonic 20 minutes, at 160r/min in shaking table, 37 DEG C shake up, respectively after adding HAP 0,10,20,40,60,90,120min, the supernatant 50 μ L is got in 2mL pipe after centrifugal, and add 450 μ L deionized water dilutions to do ultraviolet sign, by standard curve, calculate useful load, make correlation curve, it is stand-by that lower floor is placed on refrigerator.Horizontal survey three groups experiment.
Can find out, for HAP, at about 10min, the useful load of silibinin reaches maximum, and then along with the increase of adsorption time, useful load increased before this, then reduced.
The foregoing is only the preferred embodiment of the invention; not in order to limit the invention; the any amendment done within all spirit in the invention and principle, equivalently to replace and improvement etc., within the protection domain that all should be included in the invention.
Claims (2)
1. the preparation method of a nanorize silibinin hydroxyapatite composite micro-capsule, it is characterized in that: select that there is good biocompatibility, bioactive nanometer hydroxyapatite is material of main part, carries out compound by ion, charge interaction to silibinin.
2. the preparation method of a kind of nanorize silibinin hydroxyapatite composite micro-capsule as claimed in claim 1, it is characterized in that: concrete preparation method is: compound concentration is the silibinin of 5600ug/mL, get the silibinin solution 5mL prepared, and add 5mg nanometer hydroxyapatite (HAP), ultrasonic 20 minutes, shake up at the rotating speed of 160r/min, the temperature of 37 DEG C in shaking table, 10min after adding nanometer hydroxyapatite, the useful load of silibinin reaches maximum, and nanorize silibinin hydroxyapatite composite micro-capsule is successfully prepared.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410614631.2A CN104398489A (en) | 2014-11-04 | 2014-11-04 | Preparation method for nanocrystalized silybin-hydroxylapatite composite microcapsule |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410614631.2A CN104398489A (en) | 2014-11-04 | 2014-11-04 | Preparation method for nanocrystalized silybin-hydroxylapatite composite microcapsule |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104398489A true CN104398489A (en) | 2015-03-11 |
Family
ID=52636201
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410614631.2A Pending CN104398489A (en) | 2014-11-04 | 2014-11-04 | Preparation method for nanocrystalized silybin-hydroxylapatite composite microcapsule |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN104398489A (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007145395A1 (en) * | 2006-06-13 | 2007-12-21 | Han-Bul Cosmetics Co., Ltd. | Method of stabilization of active ingredients that have low solubility, using hollow type multi-layered microcapsule made of hydrophobic polymer/polyhydric alcohols and preparation method thereof, and cosmetic composition containing the microcapsules |
| CN101557720A (en) * | 2006-12-12 | 2009-10-14 | 弗门尼舍有限公司 | Active ingredient delivery system with an amorphous metal salt as carrier |
| CN102657598A (en) * | 2012-05-09 | 2012-09-12 | 上海交通大学 | Porous inorganic material based oral preparation of secondary-dispersion insoluble drug and preparation method thereof |
-
2014
- 2014-11-04 CN CN201410614631.2A patent/CN104398489A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007145395A1 (en) * | 2006-06-13 | 2007-12-21 | Han-Bul Cosmetics Co., Ltd. | Method of stabilization of active ingredients that have low solubility, using hollow type multi-layered microcapsule made of hydrophobic polymer/polyhydric alcohols and preparation method thereof, and cosmetic composition containing the microcapsules |
| CN101557720A (en) * | 2006-12-12 | 2009-10-14 | 弗门尼舍有限公司 | Active ingredient delivery system with an amorphous metal salt as carrier |
| CN102657598A (en) * | 2012-05-09 | 2012-09-12 | 上海交通大学 | Porous inorganic material based oral preparation of secondary-dispersion insoluble drug and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 廖工铁 等: "《靶向给药制剂》", 31 August 1997 * |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Obluchinskaya et al. | Efficacy of natural deep eutectic solvents for extraction of hydrophilic and lipophilic compounds from Fucus vesiculosus | |
| Minzanova et al. | Biological activity and pharmacological application of pectic polysaccharides: A review | |
| Munin et al. | Encapsulation of natural polyphenolic compounds; a review | |
| Ahmad et al. | A critical review on the synthesis of natural sodium alginate based composite materials: An innovative biological polymer for biomedical delivery applications | |
| Chan et al. | Encapsulation of herbal aqueous extract through absorption with ca-alginate hydrogel beads | |
| Kurek et al. | Antioxidants and bioactive compounds in food: critical review of issues and prospects | |
| Nam et al. | Application of bioactive quercetin in oncotherapy: from nutrition to nanomedicine | |
| Jayachandran et al. | Green synthesized silver nanoparticle-loaded liposome-based nanoarchitectonics for cancer management: in vitro drug release analysis | |
| Luo et al. | Particle-stabilizing effects of flavonoids at the oil− water interface | |
| El Asbahani et al. | Essential oils: From extraction to encapsulation | |
| Fraguela-Meissimilly et al. | New trends in supercritical fluid technology and pressurized liquids for the extraction and recovery of bioactive compounds from agro-industrial and marine food waste | |
| Ion et al. | An up-to-date review of natural nanoparticles for cancer management | |
| Zafar et al. | Recent developments in the reduction of oxidative stress through antioxidant polymeric formulations | |
| RU2017101992A (en) | PURIFIED THERAPEUTIC NANOPARTICLES AND METHODS FOR PRODUCING THEM | |
| Jia et al. | Nano-based drug delivery of polyphenolic compounds for cancer treatment: Progress, opportunities, and challenges | |
| AbouAitah et al. | Nanomedicine as an emerging technology to foster application of essential oils to fight cancer | |
| Ferreira et al. | Flavonoids-based delivery systems towards cancer therapies | |
| Imran et al. | Exploring the remarkable chemotherapeutic potential of polyphenolic antioxidants in battling various forms of cancer | |
| Zhou et al. | The commonly used stabilizers for phytochemical-based nanoparticles: stabilization effects, mechanisms, and applications | |
| EP2942061A3 (en) | Ige ch3 peptide vaccine | |
| Coiai et al. | Rosmarinic acid and Ulvan from terrestrial and marine sources in anti-microbial bionanosystems and biomaterials | |
| Pecorini et al. | Polymeric systems for the controlled release of flavonoids | |
| Sanghi et al. | Herbal drugs an emerging tool for novel drug delivery systems | |
| Li et al. | The application of natural carotenoids in multiple fields and their encapsulation technology: A review | |
| Alfei et al. | Nanotechnological manipulation of nutraceuticals and phytochemicals for healthy purposes: Established advantages vs. still undefined risks |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20150311 |