Poly-L-lactic acid and polyethyleneglycol block copolymer (PLLA-PEG) supported 5-fluorouracil nanoparticles and preparation method thereof

A technology of fluorouracil and nanoparticles, applied in the field of nanoparticle preparations, can solve problems such as difficult to avoid impurities, difficult to volatilize organic solvents, wide particle size distribution, etc., and achieve the effects of reducing drug toxicity, mild operating temperature, and uniform particle size

Inactive Publication Date: 2012-07-04
SHANGHAI HI TECH UNITED BIO TECHCAL RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Since the invention uses the traditional double emulsion-volatility method to prepare microparticles, the disadvantage is that,
[0005] A. The organic solvent is difficult to volatilize between the two layers of water phase, and the residual amount of the organic solvent is large in the obtained preparation;
[0006] B. The drug loading is not high: due to the slow volatilization rate of the 5-FU aqueous solution, it is difficult to form a high enrichment of 5-FU;
[0007] C. The particle size of the particles prepared by the double emulsion-volatility method is between 1 μm and 100 μm, and it is difficult to prepare nanos...

Method used

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  • Poly-L-lactic acid and polyethyleneglycol block copolymer (PLLA-PEG) supported 5-fluorouracil nanoparticles and preparation method thereof
  • Poly-L-lactic acid and polyethyleneglycol block copolymer (PLLA-PEG) supported 5-fluorouracil nanoparticles and preparation method thereof
  • Poly-L-lactic acid and polyethyleneglycol block copolymer (PLLA-PEG) supported 5-fluorouracil nanoparticles and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Example 1 Preparation of PLLA-PEG loaded 5-FU microparticles

[0044] Polyethylene glycol L-polylactic acid block copolymer (PEG5000-PLLA50000) 200mg is dissolved in 20ml dichloromethane acetone mixed solution, add 2ml 2% 5-fluorouracil (5-FU) 1% polyvinyl alcohol (PVA) aqueous solution and stir into an emulsion. SC-CO 2 The pressure is 16MPa, the temperature is 35°C, and the flow rate is 40g / min. After the temperature and pressure became constant, the emulsion was added at a flow rate of 1ml / min. Pass CO after sample loading 2 20min. Microspheres were collected under reduced pressure. The average particle size of the microspheres was detected by a scanning electron microscope (SEM) to be 229 nm. (attached figure 2 )

Embodiment 2

[0045] Example 2 Preparation of PLLA-PEG loaded 5-FU microparticles

[0046]Polyethylene glycol L-polylactic acid block copolymer (PEG5000-PLLA25000) 200mg is dissolved in 20ml dichloromethane acetone mixed solution, add 2ml2% 5-fluorouracil (5-FU) 1% polyethylene glycol (PEG4000) aqueous solution and stir Make into emulsion. SC-CO 2 The pressure is 12MPa, the temperature is 37°C, and the flow rate is 38g / min. After the temperature and pressure became constant, the emulsion was added at a flow rate of 0.8ml / min. Pass CO after sample loading 2 20min. Microspheres were collected under reduced pressure. The average particle size of the microspheres was detected by a scanning electron microscope (SEM) to be 270 nm. (attached image 3 )

Embodiment 3

[0047] Example 3 Preparation of 5-FU microparticles loaded with PLLA-PEG

[0048] Polyethylene glycol L-polylactic acid block copolymer (PEG5000-PLLA100000) 200mg is dissolved in 20ml dichloromethane acetone mixed solution, add 2ml2% 5-fluorouracil (5-FU) 1% polyethylene glycol (PEG4000) aqueous solution and stir Make into emulsion. SC-CO 2 The pressure is 16MPa, the temperature is 32°C, and the flow rate is 38g / min. After the temperature and pressure became constant, the emulsion was added at a flow rate of 1.2ml / min. Pass CO after sample loading 2 20min. Microspheres were collected under reduced pressure. The average particle size of the microspheres was detected by a scanning electron microscope (SEM) to be 194nm. (attached Figure 4 )

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Abstract

The invention relates to the field of medicinal preparations, in particular to poly-L-lactic acid and polyethyleneglycol block copolymer (PLLA-PEG) supported 5-fluorouracil (5-FU) nanoparticles and a preparation method thereof. The preparation comprises the following components in percentage by weight: 50 to 80 percent of PLLA-PEG, 5 to 20 percent of 5-FU, 1 to 5 percent of beta-cyclodextrin (Beta-CD), 5 to 15 percent of polyvinyl alcohol (PVA) and 5 to 25 percent of PEG. The PLLA-PEG supported 5-FU nanoparticles have the advantages of small average particle size, narrow particle size distribution, high medicine-loading capacity, low toxicity, good targeting performance and the like.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a nanoparticle preparation loaded with 5-fluorouracil (5-FU) on poly(L-lactic acid-polyethylene glycol) block copolymer (PLLA-PEG). Background technique [0002] 5-Fluorouracil (5-FU) is a thymidylate synthase inhibitor, a derivative in which the hydrogen at the 5-position of uracil is replaced by fluorine. 5-FU is converted into 5-fluorouracil deoxynucleotide (5F-dUMP) in the cell, and inhibits deoxythymidylate synthase, preventing the methylation of deoxyuridine (dUMP) from deoxythymidylate (dTMP) , thereby affecting DNA synthesis. In addition, 5-FU can be converted into 5-fluorouridine in vivo, and incorporated into RNA in the form of pseudo-metabolites to interfere with protein synthesis, so it also has effects on cells in other stages. [0003] At present, there are many inventions containing 5-FU particles in China. Such as Chinese patent CN 1686086 "Biodegrada...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/513A61K47/40A61P35/00
Inventor 张赪蒋司嘉黄青山
Owner SHANGHAI HI TECH UNITED BIO TECHCAL RES
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