1)、PVA濃度(X2)和藥物濃度(X3)作為考察因素,以載藥納米粒的粒徑大?。╕1)和包封率(Y2)作為評價指標(biāo),應(yīng)用中心復(fù)合設(shè)計-效應(yīng)面法優(yōu)化葫蘆素B-PLGA載藥納米粒處方;測定了納米粒的粒徑分布和Zeta電位值,通過透射電鏡觀察其微觀形態(tài),并考察了葫蘆素B-PLGA載藥納米粒的體外藥物釋放特性;比較了葫蘆素B與葫蘆素B-PLGA載藥納米粒對HepG2肝癌細胞的抑制效果。結(jié)果 葫蘆素B-PLGA載藥納米粒的最優(yōu)處方組成為:PLGA濃度為9.0%,PVA濃度為2.0%,藥物濃度為4.5%,制備的納米粒粒徑為(145.4±15.8) nm,Zeta電位值為(-7.6±0.8) mV;透射電鏡下可觀察到納米粒表面光滑,分布均勻;葫蘆素B-PLGA載藥納米粒釋藥前期出現(xiàn)突釋,后期平緩,48 h藥物釋放達到86%;葫蘆素B-PLGA載藥納米粒對HepG2肝癌細胞的抑制作用顯著高于葫蘆素B。結(jié)論 葫蘆素B-PLGA載藥納米??裳泳徦幬镝尫牛岣邔epG2肝癌細胞的抑制活性,為進一步臨床研究奠定實驗基礎(chǔ)。;Objective To prepare cucurbitacin B-loaded PLGA nanoparticles by using PLGA as carrier material, and to investigate its inhibitory effect on HepG2 liver cancer cells.Methods The cucurbitacin B-loaded PLGA nanoparticles were prepared by emulsion solvent evaporation method. Taking PLGA concentration (X1), PVA concentration (X2) and drug concentration (X3) as the investigation factors, the particle size (Y1) and encapsulation efficiency (Y2) of cucurbitacin B-loaded PLGA nanoparticles were used as evaluation indexes. The central composite design-response surface methodology (CCD-RSM) was applied to optimize the formulation of cucurbitacin B-loaded PLGA nanoparticles. The particle size distribution and Zeta potential value were determined. The microscopic morphology was observed by transmission electron microscopy. The in vitro drug release characteristics of cucurbitacin B-loaded PLGA nanoparticles were investigated. The inhibitory effects of cucurbitacin B and cucurbitacin B-loaded PLGA nanoparticles on HepG2 liver cancer cells were compared.Results The optimal formulation of cucurbitacin B-loaded PLGA nanoparticles was:PLGA concentration of 9.0%, PVA concentration of 2.0%, drug concentration of 4.5%. The particle size of (145.4±15.8) nm, and zeta potential of (-7.6±0.8) mV. Transmission electron microscopy showed that the nanoparticles were smooth and uniform in size. The release of cucurbitacin B-loaded PLGA nanoparticles was fast in the early stage, and the late release was slow. Finally, the drug release was 86% within 48 hours. The inhibitory effect of cucurbitacin B-loaded PLGA nanoparticles on HepG2 liver cancer cells was significantly higher than that of cucurbitacin B.Conclusion The cucurbitacin B-loaded PLGA nanoparticles could delay drug release and increase the inhibitory activity of HepG2 liver cancer cells, which lays the experimental foundation for further clinical research."/>

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首頁 > 過刊瀏覽>2019年第42卷第8期 >2019,42(8):1557-1562. DOI:10.7501/j.issn.1674-6376.2019.08.012
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葫蘆素B-聚乳酸-羥基乙酸共聚物載藥納米粒的構(gòu)建與藥效學(xué)評價

Construction and pharmacodynamic evaluation of cucurbitacin B-loaded PLGA nanoparticles

發(fā)布日期:2019-09-07
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