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Biodegradable fluorourcacil polyester medicine-carried nanospheres and its preparation method

A fluorouracil and drug-loaded nanotechnology, which is applied in the field of biodegradable polyester-coated fluorouracil drug-loaded nanospheres and its preparation, can solve the problems of high preparation conditions and low drug loading of microspheres, and achieve significant sustained release Effect, uniform diameter distribution, effect of reducing particle size

Inactive Publication Date: 2007-10-17
JILIN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its disadvantage is that the drug loading of microspheres prepared by O / O and O / W emulsification and evaporation methods is low, while the spray drying method requires high preparation conditions.

Method used

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  • Biodegradable fluorourcacil polyester medicine-carried nanospheres and its preparation method
  • Biodegradable fluorourcacil polyester medicine-carried nanospheres and its preparation method
  • Biodegradable fluorourcacil polyester medicine-carried nanospheres and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: 0.1 g of PLA (40000 g / mol) was dissolved in 5 ml of dichloromethane to obtain a polymer solution. Inject 0.5ml, 100mg / ml fluorouracil NaOH solution into the polymer solution, and disperse evenly under the action of ultrasound to obtain a W / O initial emulsion; under high-speed stirring, inject the initial emulsion into 10ml of fluorouracil saturated with 5wt% PVA In the aqueous solution, emulsify for 30 minutes to form a W / O / W double emulsion, and then stir for 3 hours to volatilize the dichloromethane and solidify the microspheres. The obtained suspension was centrifuged, the microspheres were collected, washed several times with distilled water, and then freeze-dried to obtain fluorouracil nanospheres. According to Fig. 1 and Fig. 2, according to measurement and calculation, in the prepared drug-loaded nanospheres, the drug content accounts for 14.1% of the mass of the microspheres, and the average particle diameter of the microspheres is 381.7nm. The relea...

Embodiment 2

[0047] Embodiment 2: This example is basically the same as Example 1, except that the molecular weight of the PLA used is (100000g / mol), and in the prepared drug-loaded nanospheres, the drug content accounts for 20.5% of the microsphere mass, and the average particle size The diameter is 916.1nm. The release time was 76 days (accompanying drawing 4).

Embodiment 3

[0048] Embodiment 3: This example is basically the same as Example 1, except that the polymer used is PLGA, and the molecular weight is (20000-20000g / mol). In the prepared drug-loaded nanospheres, the drug content accounts for 12.7%, and the average particle size is 212.3nm. The release time was 19 days (accompanying drawing 5).

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Abstract

The invention relates to biodegradable fluorouracil(Fu) polyester drug-bearing manoparticles with a coating material of polylactic acid, polylactic acid-glycolic acid, polylactic acid-polyethylene glycol block copolymer or polylactic acid-glycolic acid-polyethylene glycol block copolymer and the producing method including: firstly, fully dissolving the copolymer in the dichloromethane, under the ultrasonic shock, injecting the fluorouracil NaOH solution in the dichloromethane solution, dispersing uniformly, forming W / O primary latex, and beating up the primary latex and injecting into the fluorouracil saturated water solution containing 5 wt% of polyvinylalcohol (PVA), and storing in the refrigeratory after freeze-dry. The drug-bearing manoparticle has a drug content which is 10-25% of the microparticle mass, and has a smooth surface, an even diameter distribution, a remarkable slow release function and not adhesive. The micropartical size is 100-1000nm.

Description

technical field [0001] The invention relates to a fluorouracil drug-loaded nanosphere and a preparation method thereof, in particular to a biodegradable polyester-wrapped fluorouracil drug-loaded nanosphere and a preparation method thereof. Background technique [0002] Fluorouracil is a pyrimidine anti-metabolite, which mainly inhibits the formation of thymine nucleotides and DNA biosynthesis through enzyme competition, thereby inhibiting tumor growth. It has a wide anti-cancer spectrum and is effective against colon cancer, rectal cancer, gastric cancer and breast cancer, and is the drug of choice for the treatment of solid tumors. Although the curative effect of fluorouracil is good, it is also highly toxic, and can cause side effects such as severe gastrointestinal reactions and bone marrow suppression, and it disappears from the plasma soon after intravenous injection. 1 / 2 About 10 to 20 minutes. In order to reduce the toxic and side effects of fluorouracil and improv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/50A61K47/34A61K31/513A61P35/00
Inventor 汤钧林航王锡山汤庆超王策李唯王丽萍
Owner JILIN UNIV
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