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Preparation method of 5-fluorouracil-wrapped biodegradable polylactic acid/nano-hydroxyapatite compound microspheres

A nano-hydroxyapatite, biodegradable technology, applied in the direction of drug combination, antineoplastic drugs, bulk delivery, etc., can solve the problems of PLA/nHA that have not been reported, and achieve long-acting and sustained release, drug release Long-term, significant effects

Inactive Publication Date: 2012-08-08
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few reports on PLA and HA as a carrier together, but PLA / nHA as a 5-Fu carrier and made into composite microspheres has not been reported at home and abroad.

Method used

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  • Preparation method of 5-fluorouracil-wrapped biodegradable polylactic acid/nano-hydroxyapatite compound microspheres
  • Preparation method of 5-fluorouracil-wrapped biodegradable polylactic acid/nano-hydroxyapatite compound microspheres
  • Preparation method of 5-fluorouracil-wrapped biodegradable polylactic acid/nano-hydroxyapatite compound microspheres

Examples

Experimental program
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Effect test

example 1

[0026] Preparation of PLA / nHA-5Fu composite microspheres: ① Preparation of nHA-5-Fu: Add 0.3gnHA and 60mg5-Fu to a certain 0.3mol / l sodium hydroxide aqueous solution, first 80kHz ultrasonic mixing, and then magnetic stirring for 24h, Freeze-dried to obtain white freeze-dried powder nHA-5-Fu. ②Preparation of microspheres: Add nHA-5-Fu freeze-dried powder into 10ml dichloromethane solution dissolved with 1g PLA, stir at 10000rpm for 1min at a high speed, after fully mixing and dispersing, an S / O emulsion is formed, and then the above suspension is rapidly Pour into 200ml of 0.4% (w / v, g / ml) deionized aqueous solution of emulsifier methyl cellulose to obtain an S / O / W emulsion, and stir it magnetically at 400rpm for 4h until the dichloromethane is completely volatilized; After standing for 4 hours, it was centrifuged at a speed of 10000 rpm to separate the precipitate, washed three times with deionized water, and then freeze-dried, and the obtained microsphere particles were store...

example 2

[0033] Preparation of PLA / nHA-5Fu composite microspheres: ① Preparation of nHA-5-Fu: Add 0.3gnHA and 30mg5-Fu to 3mol / l potassium hydroxide aqueous solution, first 100kHz ultrasonic mixing, then magnetic stirring for 24h, freeze-drying , to obtain white lyophilized powder nHA-5-Fu. ②Preparation of microspheres: Add nHA-5-Fu freeze-dried powder into 10ml dichloromethane solution dissolved with 1g PLA, stir at 5000rpm at high speed for 1min, after fully mixing and dispersing, an S / O emulsion is formed, and then the above suspension is rapidly Pour into 500ml of 0.1% (w / v, g / ml) deionized aqueous solution of emulsifier methylcellulose to obtain an S / O / W emulsion, stir it magnetically at 600rpm for 4h, and make dichloromethane until it volatilizes completely; After standing for 4 hours, it was centrifuged at a speed of 10000 rpm to separate the precipitate, washed three times with deionized water, and then freeze-dried, and the obtained microsphere particles were stored in a dry s...

example 3

[0035] Preparation of PLA / nHA-5Fu composite microspheres: ① Preparation of nHA-5-Fu: Add 0.1gnHA and 60mg5-Fu to 0.1mol / l sodium hydroxide aqueous solution, first 40kHz ultrasonic mixing, then magnetic stirring for 24h, freeze dry to obtain white lyophilized powder nHA-5-Fu. ②Preparation of microspheres: Add nHA-5-Fu freeze-dried powder into 10ml dichloromethane solution dissolved with 1g PLA, stir at 1000rpm at high speed for 1min, after fully mixing and dispersing, an S / O emulsion is formed, and then the above suspension is rapidly Pour into 100ml of 3.0% (w / v, g / ml) deionized aqueous solution of emulsifier methyl cellulose to obtain an S / O / W emulsion, and stir it magnetically at 1000rpm for 4h until the dichloromethane is completely volatilized; After standing for 4 hours, it was centrifuged at a speed of 10000 rpm to separate the precipitate, washed three times with deionized water, and then freeze-dried, and the obtained microsphere particles were stored in a dry state. ...

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Abstract

The invention provides a preparation method of 5-fluorouracil-wrapped biodegradable polylactic acid / nano-hydroxyapatite compound microspheres, wherein biodegradable high molecular polylactic acid and biological inorganic material nano-hydroxyapatite are jointly adopted as carriers, a single emulsified solvent evaporation method (S / O / W, short for solid in oil in water) is adopted for preparing the5-fluorouracil-wrapped biodegradable polylactic acid / nano-hydroxyapatite compound microspheres, and different mass ratios of NHA / 5-Fu and different stirring speeds are adopted for preparing the compound microspheres. The prepared microspheres have ordered sphere, porous surface, uniformly dispersed sizes, controllability, drug-loading rate of above 3.0 percent, entrapment rate of above 70 percent, long drug release time up to more than 27 days and obvious long-acting and slow-releasing effect, overcomes the defects of short slow-release time or low entrapment rate of a 5-Fu preparation and isexpected to be used for treating cancers.

Description

technical field [0001] The invention relates to a preparation method of biodegradable polylactic acid / nanometer hydroxyapatite composite microspheres wrapping 5-fluorouracil. Background technique [0002] 5-Fluorouracil (5-Fu) can inhibit thymidine nucleotide synthase, block the conversion of deoxypyrimidine nucleotide into thymidine nucleus, interfere with DNA synthesis, and play an anti-cancer role; and it can also be mixed with pseudo metabolites into RNA to inhibit the proliferation of tumor cells. It is the most commonly used anticancer drug in clinical practice for more than 30 years. , bladder cancer, etc. have good curative effect, even so far, it is still an irreplaceable one of the most effective antitumor drugs. Generally, it is administered by intravenous injection or infusion, but the selectivity to tumor cells is poor, the toxic and side effects are large, the metabolism is fast, and the half-life is short, which limits the dosage and cycle of use. Polymer d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/34A61K31/513A61P35/00
Inventor 魏坤李像
Owner SOUTH CHINA UNIV OF TECH