CN103083249A - Method for preparing berberine chitosan drug-carrying microsphere by salting-out process - Google Patents
Method for preparing berberine chitosan drug-carrying microsphere by salting-out process Download PDFInfo
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- CN103083249A CN103083249A CN2011103431975A CN201110343197A CN103083249A CN 103083249 A CN103083249 A CN 103083249A CN 2011103431975 A CN2011103431975 A CN 2011103431975A CN 201110343197 A CN201110343197 A CN 201110343197A CN 103083249 A CN103083249 A CN 103083249A
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- berberine
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Abstract
The invention discloses a method for preparing a berberine chitosan drug-carrying microsphere by a salting-out process. With berberine as a model drug, the method disclosed in the invention adopts the salting-out process, takes unmodified chitosan as a packing material, and employs sodium tripolyphosphate as a cross-linking agent to prepare the berberine chitosan drug-carrying nanoparticle successfully. The invention has the advantages that: no modification on chitosan is needed in advance, the berberine is packed through the salting-out process, the operation is simple, the repeatability is strong, and no toxic or side effect exist. Due to the special properties of chitosan, modification and grafting of other molecules on its surface are easy, thus making targeted transport and metabolic study of packed drugs possible.
Description
Technical field
The invention belongs to the method for utilizing salting out method to prepare berberine chitosan drug-loading microsphere.
Background technology
Along with the development of nanobiology and the propelling of the modernization of Chinese medicine, Nano microsphere receives much concern at drug design with aspect utilizing.Berberine is a kind of broad spectrum antibiotic of commonly using clinically, is mainly used in the bacterial infections such as bacillary dysentery, gastroenteritis, carbuncle, studies have shown that berberine also has the effects such as antitumor, anti-arrhythmia, blood pressure lowering, blood sugar lowering.Chitosan has good biocompatibility and biological degradability, and catabolite generally has no side effect to human body, do not put aside in vivo, and non-immunogenicity, thereby at biomedical sector, extremely wide application prospect is arranged.
Effective ingredient can be stablized or protect to chitosan and derivant thereof as pharmaceutical carrier, promote the absorption of medicine, delay or control drug release, help medicine to send to the target organs tissue and the unique effect of performance.
Summary of the invention
The object of the present invention is to provide a kind of method of utilizing salting out method to prepare nanoscale berberine chitosan drug-loading microsphere.
The present invention adopts salting out method take berberine as raw material, and take unmodified chitosan as lapping, sodium tripolyphosphate is cross-linking agent, has successfully prepared the berberine chitosan nano drug-carrying microsphere.Due to the special nature of chitosan, its surface is modification and other molecules of grafting easily, thereby make the medicine of parcel possess probability aspect targeted, metabolism research.
A kind of method of utilizing salting out method to prepare berberine chitosan drug-loading microsphere, it is characterized in that the method by followingly saltout, crosslinked parcel, vacuum drying process is realized:
In A, berberine aqueous solution, add sodium chloride particle, saltouing obtains the berberine granule that granularity is 400-500nm;
B, chitosan are dissolved in acetic acid solution, obtain 2.5mg/ml chitosan acetic acid solution;
C, the berberine aqueous solution is slowly added in the chitosan acetic acid solution, add equably 1.5mg/ml sodium tripolyphosphate cross-linking agent, be stirred to solution and floccule occurs;
D, the free berberine of dialysis, lyophilisation obtains berberine chitosan drug-loading Nano microsphere.
The invention has the advantages that does not need first chitosan to be carried out modification, by salting out method, berberine is wrapped up, simple to operate, repeatable strong, has no side effect.Due to the special nature of chitosan, its surface is modification and other molecules of grafting easily, thereby make the medicine of parcel that wide Research Prospects arranged aspect pharmacological research.This technology production technology is simple, and production cost is low, is easy to large-scale production.
Description of drawings
Fig. 1 is that berberine is saltoutd effect according to figure.A, berberine be dissolving fully in the liquid phase water environment, does not demonstrate particle characteristic.B, the particle size distribution of the rear berberine granule of saltouing mainly concentrates in the 300-400nm scope.
Fig. 2 is berberine chitosan nano drug-carrying microsphere Electronic Speculum picture.
Fig. 3 is berberine (Fig. 3 a), chitosan (Fig. 3 b), chitosan parcel empty ball (Fig. 3 c), berberine chitosan drug-loading Nano microsphere (Fig. 3 d) IR spectrum scanning figure.
As can be seen from Figure 1, a, berberine be dissolving fully in the liquid phase water environment, does not demonstrate particle characteristic.B, the particle size distribution of the rear berberine granule of saltouing mainly concentrates in the 400-500nm scope.The demonstration of grain size analysis results of comparison, berberine is water-soluble, does not show any particle properties to add sodium chloride in the berberine aqueous solution in water environment, makes comparatively separating out of homogeneous of berberine.
As can be seen from Figure 2, the medicine carrying microballoons diameter about the 500nm left and right, is uniformly dispersed in liquid-phase system greatly, has formed typical nucleocapsid structure, and berberine serves as nuclear structure, and chitosan molecule is externally served as shell structure, wraps up respond well.
As can be seen from Figure 3, the IR spectrum scanning result shows: berberine is at 3408.35cm
-1The place is N
+OH
-Middle O-H stretching vibration peak, 3050.7cm
-1It is the stretching vibration peak of C-H on phenyl ring.1505.95cm
-1, 1599.45cm
-1Near be the skeletal vibration peak of phenyl ring, 1398.41cm
-1Near be the C-N stretching vibration peak, 1036.61cm
-1-1231.47cm
-1The C-O-C stretching vibration peak, 827.72cm
-1Near peak is C-H out-of-plane bending vibration peak on phenyl ring.Chitosan is at 3347.60cm
-1The stretching vibration absworption peak of O-H, overlapping with N-H stretching vibration absworption peak.1650.90cm
-1, 1598.12cm
-1It is the symmetric curvature vibration peak of N-H.1422.38cm
-1, 1381.45cm
-1It is C-N stretching vibration absworption peak.1091.96cm
-1It is the stretching vibration of C-O-C.1156.00cm
-1It is the stretching vibration of the upper C-O of ring.1260.65cm
-1Be-CH
2C-O stretching vibration peak on OH.The empty ball of chitosan parcel is at 3441.99cm
-1The stretching vibration peak of N-H, 3284.74cm
-1It is the stretching vibration peak of O-H.-NH
2Middle N-H peak is by 1650cm
-1Move on to 1575cm
-1The place illustrates-NH
2React, cross-linking reaction occurs in chitosan and TPP.The berberine chitosan nano drug-carrying microsphere is at 3416.13cm
-1The place is N-H, the stretching vibration stack peak of O-H, 1637.68cm
-1, 1541.87cm
-1The place is phenyl ring C=C skeletal vibration peak, 801.31cm
-1The place is C-H out-of-plane bending vibration peak on phenyl ring.Compare with blank microsphere, occurred obvious phenyl ring infrared absorption peak in the nanosphere that has wrapped up, namely the benzene ring structure in the berberine molecule, contain berberine in the Nano microsphere that has as seen wrapped up.
We have also carried out the mensuration of envelop rate, and berberine chitosan drug-loading Nano microsphere is dialysed in liquid phase environment, after free berberine is dialysed fully, measure free berberine concentration (table 1).Recording the average envelop rate of berberine chitosan drug-loading Nano microsphere is 71.35%.
The specific embodiment
Take chitosan 25mg and be dissolved in acetic acid solution, the standing bubble of removing.Accurately take the 2mg berberine and be dissolved in water, add sodium chloride particle to berberine and saltout.The berberine aqueous solution is slowly added in the chitosan acetic acid solution, stir, then add equably 1.5mg/ml sodium tripolyphosphate 4ml, continue to be stirred to solution and floccule occurs.After stirring is completed, the free berberine of dialysis, lyophilisation obtains the berberine chitosan nano drug-carrying microsphere.
Embodiment 2
Take chitosan 50mg and be dissolved in acetic acid solution, the standing bubble of removing.Accurately take the 4mg berberine and be dissolved in water, add sodium chloride particle to berberine and saltout.The berberine aqueous solution is slowly added in the chitosan acetic acid solution, stir, then add equably 1.5mg/ml sodium tripolyphosphate 8ml, continue to be stirred to solution and floccule occurs.After stirring is completed, the free berberine of dialysis, lyophilisation obtains the berberine chitosan nano drug-carrying microsphere.
Embodiment 3
Take chitosan 100mg and be dissolved in acetic acid solution, the standing bubble of removing.Accurately take the 8mg berberine and be dissolved in water, add sodium chloride particle to berberine and saltout.The berberine aqueous solution is slowly added in the chitosan acetic acid solution, stir, then add equably 1.5mg/ml sodium tripolyphosphate 16ml, continue to be stirred to solution and floccule occurs.After stirring is completed, the free berberine of dialysis, lyophilisation obtains the berberine chitosan nano drug-carrying microsphere.
Claims (1)
1. method of utilizing salting out method to prepare berberine chitosan drug-loading microsphere, it is characterized in that the method by followingly saltout, crosslinked parcel, vacuum drying process is realized:
In A, berberine aqueous solution, add sodium chloride particle, saltouing obtains the berberine granule that granularity is 400-500nm;
B, chitosan are dissolved in acetic acid solution, obtain 2.5mg/1 chitosan acetic acid solution;
C, the berberine aqueous solution is slowly added in the chitosan acetic acid solution, add equably 1.5mg/ml sodium tripolyphosphate cross-linking agent, be stirred to solution and floccule occurs;
D, the free berberine of dialysis, lyophilisation obtains berberine chitosan drug-loading Nano microsphere.
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| CN2011103431975A CN103083249A (en) | 2011-11-03 | 2011-11-03 | Method for preparing berberine chitosan drug-carrying microsphere by salting-out process |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106491560A (en) * | 2016-10-20 | 2017-03-15 | 潍坊医学院 | A kind of Berberine hydrochloride targeted nano preparation and its preparation method and application |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1698901A (en) * | 2005-06-15 | 2005-11-23 | 蒋斯扬 | Chitosan or its derivative as drug carrier for carrying red sage root extract |
| CN1813684A (en) * | 2005-11-15 | 2006-08-09 | 暨南大学 | Method for preparing 5-fluorouracil/chitosan nano drug-carrying microsphere |
-
2011
- 2011-11-03 CN CN2011103431975A patent/CN103083249A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1698901A (en) * | 2005-06-15 | 2005-11-23 | 蒋斯扬 | Chitosan or its derivative as drug carrier for carrying red sage root extract |
| CN1813684A (en) * | 2005-11-15 | 2006-08-09 | 暨南大学 | Method for preparing 5-fluorouracil/chitosan nano drug-carrying microsphere |
Non-Patent Citations (1)
| Title |
|---|
| 王道武等: "黄连中小檗碱盐析法提取研究", 《广东化工》, vol. 37, no. 11, 2010, pages 34 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106491560A (en) * | 2016-10-20 | 2017-03-15 | 潍坊医学院 | A kind of Berberine hydrochloride targeted nano preparation and its preparation method and application |
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Application publication date: 20130508 |