Docetaxel (DTX), as a member of taxoid family, has been widely used in the treatment of cancers. The present study prepared pH-sensitive DTX-loaded liposomes (DTX-Lips) by thin-film dispersion method and various physi...Docetaxel (DTX), as a member of taxoid family, has been widely used in the treatment of cancers. The present study prepared pH-sensitive DTX-loaded liposomes (DTX-Lips) by thin-film dispersion method and various physico-chemical and morphological properties were examined. The pH sensitivity of in vitro DTX release and the in vivo pharmacokinetics and tissue distribution using Kunming mice were also investigated. The mean particle size and zetapotential of DTX liposomes were (277±2) nm and (-32.60±0.26) mV, respectively. Additionally, in vitro drug release study showed that the cumulative release rate was 1.3 times more at pH 5.0 than at pH 7.4, suggesting a pH-dependent releaseability of DTX-Lips. Pharmacokinetic and pharmaceutical studies in comparison with Duopafei showed that the half-timeperiod (t1/2) and area under the curve (AUC) of DTX-Lips in mouse plasma were 1.8 times longer and 2.6 times higher,respectively, and that DTX-Lips selectively accumulated in macrophage-rich organs such as liver and spleen. The seresults together suggest that the DTX-Lips could be a promising formulation for the clinical administration of DTX.展开更多
The metabolic activity of organisms can be measured by recording the heat output using microcalorimetry. In this paper, the total alkaloids in the traditional Chinese medicine Radix Aconiti Lateralis were extracted an...The metabolic activity of organisms can be measured by recording the heat output using microcalorimetry. In this paper, the total alkaloids in the traditional Chinese medicine Radix Aconiti Lateralis were extracted and applied to Eschenchia coil and Staphylococcus aureus. The effect of alkaloids on bacteda growth was studied by microcalorimetry. The power-time curves were plotted with a thermal activity monitor （TAM） air isothermal microcalorimeter and pa- rameters such as growth rate constant （p）, peak-time （Trn）, inhibitory ratio （I）, and enhancement ratio （E） were cal- culated. The relationships between the concentration of Aconitum alkaloids and p of E. coil or S. aureus were discussed. The results showed that Aconitum alkaloids had little effect on E. coil and had a potentially inhibitory effect on the growth of S. aureus.展开更多
基金Project supported by the Independent Innovation Foundation of Shandong University, China (No. 2010TS041)the Shandong Provincial Special Funds for Postdoctoral Innovative Projects, China(No. 201003069)
文摘Docetaxel (DTX), as a member of taxoid family, has been widely used in the treatment of cancers. The present study prepared pH-sensitive DTX-loaded liposomes (DTX-Lips) by thin-film dispersion method and various physico-chemical and morphological properties were examined. The pH sensitivity of in vitro DTX release and the in vivo pharmacokinetics and tissue distribution using Kunming mice were also investigated. The mean particle size and zetapotential of DTX liposomes were (277±2) nm and (-32.60±0.26) mV, respectively. Additionally, in vitro drug release study showed that the cumulative release rate was 1.3 times more at pH 5.0 than at pH 7.4, suggesting a pH-dependent releaseability of DTX-Lips. Pharmacokinetic and pharmaceutical studies in comparison with Duopafei showed that the half-timeperiod (t1/2) and area under the curve (AUC) of DTX-Lips in mouse plasma were 1.8 times longer and 2.6 times higher,respectively, and that DTX-Lips selectively accumulated in macrophage-rich organs such as liver and spleen. The seresults together suggest that the DTX-Lips could be a promising formulation for the clinical administration of DTX.
基金supported by the National Natural Science Foundation of China(No.21203112)the Natural Science Foundation of Shandong Province(No.ZR2012BQ002),China
文摘The metabolic activity of organisms can be measured by recording the heat output using microcalorimetry. In this paper, the total alkaloids in the traditional Chinese medicine Radix Aconiti Lateralis were extracted and applied to Eschenchia coil and Staphylococcus aureus. The effect of alkaloids on bacteda growth was studied by microcalorimetry. The power-time curves were plotted with a thermal activity monitor （TAM） air isothermal microcalorimeter and pa- rameters such as growth rate constant （p）, peak-time （Trn）, inhibitory ratio （I）, and enhancement ratio （E） were cal- culated. The relationships between the concentration of Aconitum alkaloids and p of E. coil or S. aureus were discussed. The results showed that Aconitum alkaloids had little effect on E. coil and had a potentially inhibitory effect on the growth of S. aureus.
