AIM:To evaluate the effect of auraptene(AUR)treatment in forms of free and encapsulated in niosome nanoparticles by investigating the mRNA expression level of vascular endothelium growth factor(VEGF)-A and platelet-de...AIM:To evaluate the effect of auraptene(AUR)treatment in forms of free and encapsulated in niosome nanoparticles by investigating the mRNA expression level of vascular endothelium growth factor(VEGF)-A and platelet-derived growth factors(PDGFs)in human retinal pigment epithelium(RPE)cell line.METHODS:Niosome nanocarriers were produced using two surfactants Span 60 and Tween 80.RPE cell line was treated with both free AUR and niosome-encapsulated.Optimum dosage of treatments was calculated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT)assay.Expression of VEGF-A and PDGF-A,PDGF-B,PDGF-C,PDGF-D genes was measured after total RNA extraction and cDNA synthesis,using real-time polymerase chain reaction(RT-PCR).RESULTS:The highest entrapment efficiency(EE)was achieved by Span 60:cholesterol(1:1)with 64.3%.The half maximal inhibitory concentration(IC50)of free and niosome-encapsulated AUR were 38.5 and 27.78µg/mL,respectively.Release study revealed that niosomal AUR had more gradual delivery to the cells.RT-PCR results showed reduced expression levels of VEGF-A,PDGF-A,PDGF-B,PDGF-C,and PDGF-D after treatment with both free and niosomal AUR.CONCLUSION:Niosomal formulation of Span 60:cholesterol(1:1)is an effective drug delivery approach to transfer AUR to RPE cells.VEGF-A,PDGF-A,PDGF-B,PDGF-C,and PDGF-D are four angiogenic factors,inhibiting which by niosomal AUR may be effective in age-related macular degeneration.展开更多
目的测定水不溶弱碱性药物葡萄内酯的解离常数(pKb)。方法采用Benet法和Chtten and Harris法。利用葡萄内酯易溶于丙酮的性质,选用不同比例丙酮-水混合物为溶剂进行滴定,然后利用Benet法进行pKb的计算。结果葡萄内酯pKb为9.7527,为弱碱...目的测定水不溶弱碱性药物葡萄内酯的解离常数(pKb)。方法采用Benet法和Chtten and Harris法。利用葡萄内酯易溶于丙酮的性质,选用不同比例丙酮-水混合物为溶剂进行滴定,然后利用Benet法进行pKb的计算。结果葡萄内酯pKb为9.7527,为弱碱性药物。结论 Benet法和Chtten and Harris法可有效测定难溶于水的弱碱性药物的pKb。展开更多
基金Supported by Golestan University of Medical Sciences(No.111294).
文摘AIM:To evaluate the effect of auraptene(AUR)treatment in forms of free and encapsulated in niosome nanoparticles by investigating the mRNA expression level of vascular endothelium growth factor(VEGF)-A and platelet-derived growth factors(PDGFs)in human retinal pigment epithelium(RPE)cell line.METHODS:Niosome nanocarriers were produced using two surfactants Span 60 and Tween 80.RPE cell line was treated with both free AUR and niosome-encapsulated.Optimum dosage of treatments was calculated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT)assay.Expression of VEGF-A and PDGF-A,PDGF-B,PDGF-C,PDGF-D genes was measured after total RNA extraction and cDNA synthesis,using real-time polymerase chain reaction(RT-PCR).RESULTS:The highest entrapment efficiency(EE)was achieved by Span 60:cholesterol(1:1)with 64.3%.The half maximal inhibitory concentration(IC50)of free and niosome-encapsulated AUR were 38.5 and 27.78µg/mL,respectively.Release study revealed that niosomal AUR had more gradual delivery to the cells.RT-PCR results showed reduced expression levels of VEGF-A,PDGF-A,PDGF-B,PDGF-C,and PDGF-D after treatment with both free and niosomal AUR.CONCLUSION:Niosomal formulation of Span 60:cholesterol(1:1)is an effective drug delivery approach to transfer AUR to RPE cells.VEGF-A,PDGF-A,PDGF-B,PDGF-C,and PDGF-D are four angiogenic factors,inhibiting which by niosomal AUR may be effective in age-related macular degeneration.
文摘目的测定水不溶弱碱性药物葡萄内酯的解离常数(pKb)。方法采用Benet法和Chtten and Harris法。利用葡萄内酯易溶于丙酮的性质,选用不同比例丙酮-水混合物为溶剂进行滴定,然后利用Benet法进行pKb的计算。结果葡萄内酯pKb为9.7527,为弱碱性药物。结论 Benet法和Chtten and Harris法可有效测定难溶于水的弱碱性药物的pKb。
