The siRNA-loaded lipid nanoparticles have attracted much attention due to its significant gene silencing effect and successful marketization.However,the in vivo distribution and release of siRNA still cannot be effect...The siRNA-loaded lipid nanoparticles have attracted much attention due to its significant gene silencing effect and successful marketization.However,the in vivo distribution and release of siRNA still cannot be effectively monitored.In this study,based on the fluorescence resonance energy transfer(FRET)principle,a fluorescence dye Cy5-modified survivin siRNA was conjugated to nanogolds(Au-DR-siRNA),which were then wrapped with lipid nanoparticles(LNPs)for monitoring the release behaviour of siRNA in vivo.The results showed that once Au-DR-siRNA was released from the LNPs and cleaved by the Dicer enzyme to produce free siRNA in cells,the fluorescence of Cy5 would change from quenched state to activated state,showing the location and time of siRNA release.Besides,the LNPs showed a significant antitumor effect by silencing the survivin gene and a CT imaging function superior to iohexol by nanogolds.Therefore,this work provided not only an effective method for monitoring the pharmacokinetic behaviour of LNP-based siRNA,but also a siRNA delivery system for treating and diagnosing tumors.展开更多
The in vivo release rate of levonorgestrel-containing silicon capsule (in vitro releasing rate: 6 μg/d) placed in rabbits was determined.The results showed that the average release per year was 8. 32 μg with r being...The in vivo release rate of levonorgestrel-containing silicon capsule (in vitro releasing rate: 6 μg/d) placed in rabbits was determined.The results showed that the average release per year was 8. 32 μg with r being 0.96000.The release pattern of the levonorgestrel-containing silicon capsule system was proved to be zero-order release. Our study provided some experimental data for clinical use of the system for birth control.展开更多
Summary： To study the bioequivalence of a kind of progesterone sustained release suppository, a randomized cross over study was conducted in 12 rabbits. A single rectal dose of 2.75 mg/kg progesterone sustained relea...Summary： To study the bioequivalence of a kind of progesterone sustained release suppository, a randomized cross over study was conducted in 12 rabbits. A single rectal dose of 2.75 mg/kg progesterone sustained released suppository （tested formulation, T） and progesterone suppository （reference formulation, R） was administered; a muhiple dose of 2.75 mg/kg was given up to seven times with an interval of 8 h. Concentrations in serum were determined by a competitive enzyme immunoassay. The main parameters of T were： for single and multiple doses, C was 48.8±11.8 ng/mL and 43.5±9.4 ng/mL. Tmax was 0.5±0.3 h and 0. 4±0.3 h, AUC〈（0-21h） was 362. 4±143 ng·h·mL^-1 and 310.6±70. 3 ng·h·mL^-1 , respectively. The relative bioavailability of T to R were （104.2±13.4） % and （111.4±19. 1） %, respectively. Statistical analysis showed that the two formulations were bioequivalent and T had sustained released feature.展开更多
Dopamine is a neurotransmitter crucial for movement, mood, drug addiction and many neural degeneration diseases including Parkinson’s disease. Micro electrochemical carbon
基金by the National Natural Science Foundation of China(81872812,82073800)the China Postdoctoral Science Fundation(2021TQ0111,2021M691040).
文摘The siRNA-loaded lipid nanoparticles have attracted much attention due to its significant gene silencing effect and successful marketization.However,the in vivo distribution and release of siRNA still cannot be effectively monitored.In this study,based on the fluorescence resonance energy transfer(FRET)principle,a fluorescence dye Cy5-modified survivin siRNA was conjugated to nanogolds(Au-DR-siRNA),which were then wrapped with lipid nanoparticles(LNPs)for monitoring the release behaviour of siRNA in vivo.The results showed that once Au-DR-siRNA was released from the LNPs and cleaved by the Dicer enzyme to produce free siRNA in cells,the fluorescence of Cy5 would change from quenched state to activated state,showing the location and time of siRNA release.Besides,the LNPs showed a significant antitumor effect by silencing the survivin gene and a CT imaging function superior to iohexol by nanogolds.Therefore,this work provided not only an effective method for monitoring the pharmacokinetic behaviour of LNP-based siRNA,but also a siRNA delivery system for treating and diagnosing tumors.
文摘The in vivo release rate of levonorgestrel-containing silicon capsule (in vitro releasing rate: 6 μg/d) placed in rabbits was determined.The results showed that the average release per year was 8. 32 μg with r being 0.96000.The release pattern of the levonorgestrel-containing silicon capsule system was proved to be zero-order release. Our study provided some experimental data for clinical use of the system for birth control.
文摘Summary： To study the bioequivalence of a kind of progesterone sustained release suppository, a randomized cross over study was conducted in 12 rabbits. A single rectal dose of 2.75 mg/kg progesterone sustained released suppository （tested formulation, T） and progesterone suppository （reference formulation, R） was administered; a muhiple dose of 2.75 mg/kg was given up to seven times with an interval of 8 h. Concentrations in serum were determined by a competitive enzyme immunoassay. The main parameters of T were： for single and multiple doses, C was 48.8±11.8 ng/mL and 43.5±9.4 ng/mL. Tmax was 0.5±0.3 h and 0. 4±0.3 h, AUC〈（0-21h） was 362. 4±143 ng·h·mL^-1 and 310.6±70. 3 ng·h·mL^-1 , respectively. The relative bioavailability of T to R were （104.2±13.4） % and （111.4±19. 1） %, respectively. Statistical analysis showed that the two formulations were bioequivalent and T had sustained released feature.
基金Supported by grant from Chinese NSFC "973" program
文摘Dopamine is a neurotransmitter crucial for movement, mood, drug addiction and many neural degeneration diseases including Parkinson’s disease. Micro electrochemical carbon
