Slow-releasing micro-balls of demethyl cantharidine, and its prepn. method

A technology of demethylcantharidin and slow-release microspheres, which is applied in the field of nanomaterials and biomedicine to achieve high encapsulation efficiency, simple preparation and operation, and improved hydrophilicity

Inactive Publication Date: 2006-01-25
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Foreign research on norcantharidin is mainly aimed at p...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The polymer adopts poly(lactic acid-ethylene glycol), wherein the molecular weight of polyethylene glycol is 4000, the copolymerization ratio of lactic acid and ethylene glycol is 5 / 1, and the polymer charging amount is 0.1505g, which is dissolved in 60ml of dichloromethane to form oil Phase; 40mg norcantharidin is dissolved in 12ml water, add surfactant Tween 80, its addition is 0.8g, forms water phase; Oil phase is mixed with water phase, temperature is controlled at 28 ℃, high-speed stirring 7000 rev / After 18 minutes of stirring time, colostrum is formed; add 120ml of 0.3g / ml PVA aqueous solution to colostrum, stir to form double emulsion, and then place the double emulsion in a dialysis bag for dialysis to remove unencapsulated drugs, and finally dissolve it Freeze-dried into powder and sealed for storage; the obtained norcantharidin sustained-release microspheres have a particle size of 96.9±91nm, an encapsulation rate of 30%, and a stable release of up to 72 hours...

Embodiment 2

[0031] The polymer adopts poly(lactic acid-ethylene glycol), wherein the molecular weight of ethylene glycol is 6000, the copolymerization ratio of lactic acid and ethylene glycol is 5 / 1, and the polymer charging amount is 0.4020g, which is dissolved in 60ml of dichloromethane to form an oil phase ; 80mg norcantharidin was dissolved in 12ml water, adding surfactant Span 80, the addition amount was 0.4g, to form a water phase; the oil phase was mixed with the water phase, the temperature was controlled at 5°C, and the high-speed stirring was performed at 25000 rpm , stirring for 3 minutes to form colostrum; add 150ml of 1g / ml PVA aqueous solution to colostrum, stir to form double emulsion, then place the double emulsion in a dialysis bag for dialysis, remove unencapsulated drugs, and finally freeze-dry it Powdered, sealed and stored; the obtained norcantharidin sustained-release microspheres have a particle size of 61.6±1 nm and an encapsulation efficiency of 23.5%.

Embodiment 3

[0033] When the water-oil ratio of colostrum is 1:10, other conditions are the same as in Example 1, the obtained microsphere particle size is 94.2 ± 52nm, the encapsulation rate of norcantharidin is 27.6%, and the stable release reaches more than 70 hours.

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PUM

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Abstract

A biodegradable slow-release micro-sphere of norcantharidin is prepared from a biodegradable polymer as carrier and norcantharidin as active component through mixing the solution of said polymer in dichloromethane or ethyl acetate with the aqueous solution of norcantharidin containing surfactant, stirring, adding it to the aqueous solution containing polyvinyl alcohol, stirring or evaporation, dialysis and freeze drying.

Description

technical field [0001] The invention belongs to the technical field of nanomaterials and biomedicine, and in particular relates to a norcantharidin sustained-release microsphere and a preparation method thereof. Background technique [0002] Norcantharidin is a new type of anti-tumor drug first synthesized in my country. It also has the functions of increasing white blood cells, protecting liver cells, and regulating immunity, so it has been paid more and more attention. It is believed that with the development of molecular biology techniques, the molecular mechanism of its anticancer effect will be gradually elucidated. However, because norcantharidin still has certain organ toxicity, its clinical dose is limited, which affects the anticancer effect; Cantharidin is an effective way to further popularize and use. A large number of data show that high encapsulation rate and small particle size are necessary conditions for reducing toxicity and improving curative effect. At ...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K9/16A61P35/00
Inventor 任杰郁晓任天斌袁华
Owner TONGJI UNIV
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