CN103169665A - Oxaliplatin chitosan nanoparticle and application thereof - Google Patents
Oxaliplatin chitosan nanoparticle and application thereof Download PDFInfo
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- CN103169665A CN103169665A CN2012104854295A CN201210485429A CN103169665A CN 103169665 A CN103169665 A CN 103169665A CN 2012104854295 A CN2012104854295 A CN 2012104854295A CN 201210485429 A CN201210485429 A CN 201210485429A CN 103169665 A CN103169665 A CN 103169665A
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Abstract
The invention discloses an oxaliplatin chitosan nanoparticle and an application thereof. The preparation materials of the oxaliplatin chitosan nanoparticle comprise oxaliplatin, chitosan, sodium tripolyphosphate and an acetic acid aqueous solution. The oxaliplatin chitosan nanoparticle disclosed by the invention can be applied to preparing a drug for treating gastrointestinal tumors. Compared with the prior art, the oxaliplatin chitosan nanoparticle disclosed by the invention is small in grain size, high in encapsulation efficiency, low in material price and simpler in process.
Description
(1) technical field
The present invention relates to the medicament nano granule field, relate in particular to a kind of oxaliplatin chitosan nanoparticle and application thereof.
(2) background technology
Oxaliplatin is third generation platinum-containing anticancer drug.FDA in 2004 approval Oxaliplatin for Injection and 5-fluorouracil and folinic acid are united the first-line treatment for progressive stage colon rectal cancer.The oxaliplatin formulations that has now gone on the market has aqueous injection and freeze-dried powder.Oxaliplatin centering advanced colorectal cancer is evident in efficacy, also can treat other digestive tract tumor such as gastric cancer.But along with oxaliplatin extensive application clinically, its untoward reaction is also constantly found and is reported.Neurotoxicity, gastrointestinal reaction, bone marrow depression are its common untoward reaction.
Nanoparticle is a kind of drug-supplying system of good biocompatibility, as the delivery vehicles of antitumor drug, can improve the tumor-targeting of medicine, reduces drug toxicity, therefore receives people's concern.Oxaliplatin is made nanoparticle be delivered in body, medicine better can be delivered to tumor locus, improve the antitumor action of medicine, reduce its toxic reaction.Chitosan is the copolymer that contains β-(Isosorbide-5-Nitrae)-2-acetamido-D-glucose unit and β-(Isosorbide-5-Nitrae)-2 amino-D-glucose unit, is generated after strong lye is freed acetate by chitin, and outward appearance is white or faint yellow translucent chip solid.Chitosan is a kind of reproducible, pharmaceutic adjuvant with good biocompatibility, and the effect that itself has anti-tumor activity and enhancing human body immunity function.As pharmaceutical carrier, the targeting preparation of chitosan preparation has the effect of slow release, controlled release, targeting drug release, also can increase drug absorption and improve its bioavailability, reduces the characteristics such as toxic and side effects.The report and the patent that there is no at present oxaliplatin chitosan nanoparticle.
Therefore, this area in the urgent need to provide a kind of inexpensive, technique is simple, the method for preparing oxaliplatin chitosan nanoparticle of the large production of suitability for industrialized, and requires that the chitosan nano particle diameter obtain is little, envelop rate is high.
(3) summary of the invention
The object of the invention is to provide a kind of oxaliplatin chitosan nanoparticle, to improve the envelop rate of oxaliplatin, reduces particle diameter, slowly discharges, and technique is simple, is suitable for industrialized great production.
For achieving the above object, the present invention adopts following technical scheme:
A kind of oxaliplatin chitosan nanoparticle, raw materials comprise oxaliplatin, chitosan, sodium tripolyphosphate (TPP) and aqueous acetic acid.
The concrete recommend adoption ionic cross-linking of the present invention prepares oxaliplatin chitosan nanoparticle.
The molecular weight of chitosan of the present invention is 5 * 10
3～5 * 10
6, be preferably 5 * 10
3～1 * 10
5, most preferably be 1 * 10
4
In each raw material components of the present invention, the mass ratio of oxaliplatin and chitosan is 1:1～6, is preferably 1:4.The mass ratio of chitosan and sodium tripolyphosphate is 3～9:1, is preferably 7:1.
Concrete, the preparation of described oxaliplatin chitosan nanoparticle comprises the steps:
Chitosan is dissolved in aqueous acetic acid, takes sodium tripolyphosphate (TPP) soluble in water, then will slowly join in chitosan solution after TPP solution and oxaliplatin aqueous solution, and stirring at room gets chitosan nano colloid solution.The water standardize solution carries out ultrafiltration with slipstream film bag, and water repeats ultrafiltration as replacement fluid, adjusts suspension volume and namely gets oxaliplatin chitosan nanoparticle.Ultrafilter membrane bag molecular weight is 3K～50K.
The preferred described oxaliplatin chitosan nanoparticle of the present invention prepares in accordance with the following steps:
Proportioning raw materials is: preferred proportion is that the mass ratio of oxaliplatin and chitosan is 4:1, the mass ratio 7:1 of chitosan and sodium tripolyphosphate.The water standardize solution carries out ultrafiltration with slipstream film bag, and water repeats ultrafiltration as replacement fluid, adjusts suspension volume and namely gets oxaliplatin chitosan nanoparticle.Ultrafilter membrane bag molecular weight is 3K～50K, is preferably 10K.
The oxaliplatin chitosan nanoparticle that the present invention makes can be applicable to prepare the application for the treatment of in digestive tract tumor's medicine, and for example the form with ejection preparation is used for the treatment of digestive tract tumor.
Compared with prior art, the oxaliplatin chitosan nanoparticle particle diameter that the present invention obtains is little, envelop rate is high, and raw material is inexpensive, and technique is simpler, the large production of suitability for industrialized.
(4) description of drawings
Fig. 1 is the particle size distribution figure of embodiment 1 gained oxaliplatin chitosan nanoparticle.
(5) specific embodiment
Below in conjunction with specific embodiment, further set forth the present invention.Should be understood that these embodiment only to be used for explanation the present invention and be not used in and limit the scope of the invention.The experimental technique of unreceipted actual conditions in the following example is usually according to normal condition or the condition of advising according to manufacturer.Unless otherwise indicated, otherwise all percent, ratio, ratio or umber by weight.Unless otherwise defined, the same meaning that all specialties and scientific words and the one skilled in the art who uses in literary composition is familiar with.
Embodiment 1 oxaliplatin chitosan nanoparticle 1
(molecular weight is 1 * 10 to 40 mg chitosans
4) be dissolved in 13 mL aqueous acetic acids (pH=4.0), weighing 5.7 mg sodium tripolyphosphates (TPP) are dissolved in 5 mL water, 10 mg oxaliplatins are dissolved in 2 mL water, with TPP solution with slowly join in chitosan solution after oxaliplatin solution mixes, room temperature magnetic agitation 30 min get chitosan nano colloid solution.Carry out ultrafiltration with slipstream film bag (molecular weight is 10K), water repeats ultrafiltration as replacement fluid, adjusts suspension volume and namely gets oxaliplatin chitosan nanoparticle.Its mean diameter is 59 nm, and envelop rate is 86.54%.
Embodiment 2 oxaliplatin chitosan nanoparticles 2
(molecular weight is 1 * 10 to 40 mg chitosans
4) be dissolved in 13 mL aqueous acetic acids (pH=4.0), weighing 8 mg sodium tripolyphosphates (TPP) are dissolved in 5 mL water, 10 mg oxaliplatins are dissolved in 2 mL water, with TPP solution with slowly join in chitosan solution after oxaliplatin solution mixes, room temperature magnetic agitation 30 min get chitosan nano colloid solution.Water is settled to 20 mL, carries out ultrafiltration with slipstream film bag (molecular weight is 10K), and water repeats ultrafiltration as replacement fluid, adjusts suspension volume and namely gets oxaliplatin chitosan nanoparticle.Its mean diameter is 88nm, and envelop rate is 82.13%.
Embodiment 3 oxaliplatin chitosan nanoparticles 3
(molecular weight is 1 * 10 to 40 mg chitosans
4) be dissolved in 13 mL aqueous acetic acids (pH=4.0), weighing 13.3 mg sodium tripolyphosphates (TPP) are dissolved in 5 mL water, 10 mg oxaliplatins are dissolved in 2 mL water, with TPP solution with slowly join in chitosan solution after oxaliplatin solution mixes, room temperature magnetic agitation 30 min get chitosan nano colloid solution.Water is settled to 20 mL, carries out ultrafiltration with slipstream film bag (molecular weight is 10K), and water repeats ultrafiltration as replacement fluid, adjusts suspension volume and namely gets oxaliplatin chitosan nanoparticle.Its mean diameter is 116 nm, and envelop rate is 83.37%.
The grain-size graph of embodiment 4 experimental example 1 gained oxaliplatin chitosan nanoparticles
With the appropriate distilled water diluting of chitosan nano solution, then use the laser light scattering Particle Size Analyzer that its particle diameter is measured.The particle size distribution that found that nanoparticle is even, and mean diameter is 59 nm.
Claims (9)
1. an oxaliplatin chitosan nanoparticle, is characterized in that the raw materials of described oxaliplatin chitosan nanoparticle comprises oxaliplatin, chitosan, sodium tripolyphosphate and aqueous acetic acid.
2. oxaliplatin chitosan nanoparticle as claimed in claim 1, the molecular weight of chitosan is 5 * 10
3～5 * 10
6
3. oxaliplatin chitosan nanoparticle as claimed in claim 1, it is characterized in that: the mass ratio of oxaliplatin and chitosan is 1:1～6, the mass ratio of chitosan and sodium tripolyphosphate is 3～9:1.
4. oxaliplatin chitosan nanoparticle as described in one of claim 1 ~ 3, is characterized in that the preparation of described oxaliplatin chitosan nanoparticle comprises the steps:
Chitosan is dissolved in aqueous acetic acid, takes sodium tripolyphosphate soluble in water, then will slowly join in chitosan solution after sodium tripolyphosphate solution and oxaliplatin aqueous solution, and stirring at room gets chitosan nano colloid solution; The water standardize solution carries out ultrafiltration with slipstream film bag, and water repeats ultrafiltration as replacement fluid, adjusts suspension volume and namely gets oxaliplatin chitosan nanoparticle.
5. oxaliplatin chitosan nanoparticle as claimed in claim 4, is characterized in that the pH of aqueous acetic acid is 2.0～6.0.
6. oxaliplatin chitosan nanoparticle as claimed in claim 4, the molecular retention amount that it is characterized in that slipstream film bag is 3K～50K.
7. oxaliplatin chitosan nanoparticle as claimed in claim 4, the molecular retention amount that it is characterized in that slipstream film bag is 10K.
8. oxaliplatin chitosan nanoparticle as claimed in claim 4, the mass ratio that it is characterized in that oxaliplatin and chitosan is 4:1, the mass ratio 7:1 of chitosan and sodium tripolyphosphate.
9. oxaliplatin chitosan nanoparticle as claimed in claim 1 is in the application for preparing in treating digestive tract tumor's medicine.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103550245A (en) * | 2013-10-15 | 2014-02-05 | 海南卫康制药(潜山)有限公司 | Aclarubicin composition freeze-dried powder injection for injection |
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| US20100021551A1 (en) * | 2008-07-24 | 2010-01-28 | Food Industry Research And Development Institute | Process for preparing nanoparticles of chitosan in water phase |
| CN101744771A (en) * | 2008-12-17 | 2010-06-23 | 上海海洋大学 | Method for preparing solid enrofloxacin nano particles |
| CN101991541A (en) * | 2010-10-27 | 2011-03-30 | 广东海洋大学 | Preparation method of acyclovir-chitosan nanoparticles |
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2012
- 2012-11-23 CN CN2012104854295A patent/CN103169665A/en active Pending
Patent Citations (4)
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|---|---|---|---|---|
| WO2008126971A1 (en) * | 2007-04-13 | 2008-10-23 | Korea Research Institute Of Bioscience And Biotechnology | Polymer nano particle containing uv blocking material and method for preparing the same |
| US20100021551A1 (en) * | 2008-07-24 | 2010-01-28 | Food Industry Research And Development Institute | Process for preparing nanoparticles of chitosan in water phase |
| CN101744771A (en) * | 2008-12-17 | 2010-06-23 | 上海海洋大学 | Method for preparing solid enrofloxacin nano particles |
| CN101991541A (en) * | 2010-10-27 | 2011-03-30 | 广东海洋大学 | Preparation method of acyclovir-chitosan nanoparticles |
Non-Patent Citations (3)
| Title |
|---|
| A.JAIN，ET AL: "Design and development of ligand-appended polysaccharidic nanoparticles for the delivery of oxaliplatin in colorectal cancer", 《NANOMEDICINE: NANOTECHNOLOGY, BIOLOGY, AND MEDICINE》 * |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103550245A (en) * | 2013-10-15 | 2014-02-05 | 海南卫康制药(潜山)有限公司 | Aclarubicin composition freeze-dried powder injection for injection |
| CN103550245B (en) * | 2013-10-15 | 2015-08-05 | 海南卫康制药(潜山)有限公司 | Injection aclarubicin composite freeze-dried powder |
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Application publication date: 20130626 |