CN1621093A - Construction of 5-fluorouracil chitosan minipill for filling to inside of the bladder to treat bladder cancer - Google Patents
Construction of 5-fluorouracil chitosan minipill for filling to inside of the bladder to treat bladder cancer Download PDFInfo
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- CN1621093A CN1621093A CN 200310115263 CN200310115263A CN1621093A CN 1621093 A CN1621093 A CN 1621093A CN 200310115263 CN200310115263 CN 200310115263 CN 200310115263 A CN200310115263 A CN 200310115263A CN 1621093 A CN1621093 A CN 1621093A
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- chitosan
- bladder
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- microballoon
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Abstract
The present invention relates to one kind of microballoon of chitosan carrying anticancer medicine 5-fluoroplex. During preparing the medicine carrying microballoon, chitosan, which characterizes dissolving only in acid environment rather than in neutralized and alkali environment, is immobilized with alkali solution in ion neutralizing process. During the immobilizing process, sodium hydroxide and other matter is used to replace immobilizing agent glutaraldehyde and formaldehyde, and this facilitates the further purification of the microballoon. The medicine carrying microballoon of the present invention may be adhered to bladder wall vian intravesical perfusion, and the medicine is released slowly in the tumor position to reach the aim of treating bladder tumor.
Description
Technical field
The present invention is material with the chitosan, is model drug with 5-fluorouracil (5-Fu), adopts w/o type Emulsion technology of preparing and ionomer solidification method, has prepared the chitosan sustained-release microsphere that is loaded with 5-Fu.
The present invention has the advantage of two uniquenesses, at first, during microsphere, has utilized the physicochemical property of material in preparation dexterously, has replaced present widely used formaldehyde and glutaraldehyde cross-linking solidification method with ionic cross-linking, for the refining purification of medicine carrying microballoons provides convenience; Secondly, utilize the slow release characteristics of medicine carrying microballoons and the bioadhesive of chitosan, make microsphere stick to the bladder inwall by intravesical perfusion administration, slowly the medicine that discharges produces persistent lethal effect to tumor tissues, thereby reaches the effect of treatment tumor of bladder.
Background technology
Tumor of bladder belongs to more common clinically tumor, and for this tumor treatment, Chang Yong method is excision and fulgerizes the most.But because some are special, the bladder cancer patients inconvenience that the has excision that undergos surgery is even if for the patient of excision, for after treatment, also often need by chemotherapy as auxiliary treatment means.
The chemotherapeutics of using clinically all is the cell toxicant material, and its effect is a whole body, and traditional vein or oral administration mode also produce intensive toxicity to normal tissue except tumor is had the lethal effect, particularly vital tissues such as cardiac muscle and bone marrow.The solution of intravesical perfusion cancer therapy drug, though on administering mode, realized topical, but the diffusion of intravesical medicine, not only can make medicine enter its hetero-organization and organ and produce unnecessary toxicity thus, and the drug level of therapentic part also can reduce rapidly, is difficult to reach effective therapeutic effect.
What the present invention prepared is the sustained-release micro-spheres with adhesive attraction, after the intravesical perfusion, can adhere to the bladder inwall, thereby its hetero-organization and organ have been avoided entering, in addition, the slow release of medicine around cancerous tissue can produce persistent fragmentation effect to tumor tissues, and it is needed that these two characteristics are treated tumor of bladder just.The above characteristics that adhere to sustained-release micro-spheres can realize site-specific delivery of drugs, therefore, not only improved curative effect and reduced toxicity, and dosage also can reduce.
Description of the invention
It is material that the present invention adopts chitosan, is model drug with 5-Fu, prepares microsphere by the emulsifying ionic cross-linking.The used material chitosan of the present invention is soluble in acid medium, does not dissolve in neutral and alkaline medium.Because this dissolving is reversible, therefore can utilize its this specific character, be cured by the neutral method of ion.At first, adopt the method for preparing Emulsion, oil phase, water and surfactant are added same container, under agitation prepare w/o type Emulsion, then, adding alkaline solution makes the pH value of interior water reach alkalescence, thereby make chitosan recover its solid state, by centrifugal microsphere is separated and purification again, last, medicine carrying microballoons is prepared into suspension, arrives intravesical by catheter perfusion.
Description of drawings
Sketch 1: at first, oil phase (cyclohexane extraction, dichloromethane, liquid paraffin) mixes with surfactant Span-80, under high-speed stirred, add water (chitosan with 5-fluorouracil aqueous solution), form w/o type Emulsion, the dropping sodium aqueous solution makes the chitosan of aqueous phase be solidified into microsphere.Centrifugal microsphere is separated, use absolute ethanol washing, dry must microsphere.
Embodiment
1. a cyclohexane extraction adds 3% (W/W) Span-80, with 0.2 part of 2% (W/W) chitosan dilute hydrochloric acid (10-1000) solution (wherein, the ratio of chitosan and medicine is 3: 1 w/w), be prepared into W/O Emulsion, under agitation drip 20% sodium hydroxide solution to pH value 7.5.Stir 30min, 3000rpm is centrifugal, and supernatant discarded night, the lower sediment thing is centrifugal again after with absolute ethanol washing, discards ethanol, and drying under reduced pressure obtains medicine carrying microballoons.
2. a liquid paraffin adds 3% (W/W) Span-80, with 0.3 part of 2% (W/W) chitosan dilute hydrochloric acid (10-1000) solution (ratio of chitosan and medicine is 3: 1 w/w), be prepared into W/O Emulsion, under agitation drip 20% sodium hydroxide solution to pH value 7.5.Stir 30min, 3000rpm is centrifugal, and supernatant discarded night, the lower sediment thing is centrifugal again after with absolute ethanol washing, discards ethanol, and drying under reduced pressure obtains medicine carrying microballoons.
3. a dichloromethane adds 3% (W/W) Span-80, with 0.2 part of 2% (W/W) chitosan dilute hydrochloric acid (10-1000) solution (ratio of chitosan and medicine is 3: 1 w/w), be prepared into W/O Emulsion, under agitation drip 20% sodium hydroxide solution to pH value 7.5.Stir 30min, 3000rpm is centrifugal, and supernatant discarded night, the lower sediment thing is centrifugal again after with absolute ethanol washing, discards ethanol, and drying under reduced pressure obtains medicine carrying microballoons.
4. a chloroform adds 3% (W/W) Span-80, with 0.2 part of 2% (W/W) chitosan dilute hydrochloric acid (10-1000) solution (ratio of chitosan and medicine is 3: 1 w/w), be prepared into W/O Emulsion, under agitation drip 20% potassium hydroxide solution to pH value 7.5.Stir 30min, 3000rpm is centrifugal, and supernatant discarded night, the lower sediment thing is centrifugal again after with absolute ethanol washing, discards ethanol, and drying under reduced pressure obtains medicine carrying microballoons.
Claims (4)
1. one kind is the microsphere that is loaded with cancer therapy drug of material preparation by chitosan, and the particle diameter of microsphere is between the 1-100 micron.This medicine carrying microballoons has bioadhesive.
2. according to claim 1, the medicine that medicine carrying microballoons comprised is the 5-fluorouracil (5-Fu) to the tumor of bladder sensitivity, and used material is deacetylation＞80% chitosan, and the ratio of medicine and chitosan is 0.05～0.3: 1 (w/w).
3. according to claims 2, the method for preparing microsphere is the emulsifying solidification method.The oil phase of preparation w/o type Emulsion is cyclohexane extraction, dichloromethane, chloroform, vegetable oil; Emulsifying agent is Span-80, Span-60, cholesterol; Water is 2% chitosan aqueous solution.Used firming agent is the sodium hydroxide of concentration 1-30%.
4. according to above all authority requirement, the microsphere that is loaded with cancer therapy drug of the present invention's preparation, adheres to the slow release in back by medicine carrying microballoons at the bladder inwall and treats bladder cancer through irrigation of bladder with the suspension dosage form after separating.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200310115263 CN1621093A (en) | 2003-11-27 | 2003-11-27 | Construction of 5-fluorouracil chitosan minipill for filling to inside of the bladder to treat bladder cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200310115263 CN1621093A (en) | 2003-11-27 | 2003-11-27 | Construction of 5-fluorouracil chitosan minipill for filling to inside of the bladder to treat bladder cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1621093A true CN1621093A (en) | 2005-06-01 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200310115263 Pending CN1621093A (en) | 2003-11-27 | 2003-11-27 | Construction of 5-fluorouracil chitosan minipill for filling to inside of the bladder to treat bladder cancer |
Country Status (1)
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| CN (1) | CN1621093A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110772478A (en) * | 2019-11-14 | 2020-02-11 | 湖南师范大学 | High-molecular composite hydrogel for treating bladder tumor, preparation method and application |
| CN115737589A (en) * | 2022-10-14 | 2023-03-07 | 中山大学 | Adhesive drug microsphere, preparation method thereof and application thereof in bladder perfusion treatment |
-
2003
- 2003-11-27 CN CN 200310115263 patent/CN1621093A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110772478A (en) * | 2019-11-14 | 2020-02-11 | 湖南师范大学 | High-molecular composite hydrogel for treating bladder tumor, preparation method and application |
| CN115737589A (en) * | 2022-10-14 | 2023-03-07 | 中山大学 | Adhesive drug microsphere, preparation method thereof and application thereof in bladder perfusion treatment |
| CN115737589B (en) * | 2022-10-14 | 2024-06-04 | 中山大学 | Adhesive medicinal microsphere, preparation method thereof and application thereof in bladder perfusion treatment |
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