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

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...

AI Technical Summary

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 nanospheres with a particle size of less than 1 μm. The preparation prepared by this method cannot be used as an injection form;

[0008] D. The particle size of the particles prepared by this method is greater than 500nm, and the tumor ERP effect cannot be utilized, and the preparation has no targeting effect

[0009] Including the preparation method described in Chinese patent CN 1686086, the traditional particle preparation technology still has the following disadvantages, the particle size distribution is wide, it is difficult to avoid impurities, easy to agglomerate, the biological activity is reduced, and the operation safety is poor

Images