OBJECTIVE Nanotechnology provides a novel strategy for the delivery of anticancer drugs.METHODS Titanium dioxide coated gold nanostructures(Au/TiO2)was used as the drug carrier for the natural anticancer drug gambogic...OBJECTIVE Nanotechnology provides a novel strategy for the delivery of anticancer drugs.METHODS Titanium dioxide coated gold nanostructures(Au/TiO2)was used as the drug carrier for the natural anticancer drug gambogic acid in order to improve its anticancer effect.Biocompatibility and cellular uptake of Au/TiO2 was studied in human glio⁃blastoma U-87 MG cells.Cell viability was evaluated by ATP assay and calcein AM staining.LysoSensor Green DND-189 and Hoechst 33342 were used to analyze the intracellular location of Au/TiO2.The anticancer effect of gambogic acid loaded nanoparticles was compared with free drug.RESULTS Au/TiO2 was biocompatible,and they were localized at the intracellular acidic compartments of endosomes and lysosomes.The intracellular drug content delivered via Au/TiO2 was 6-fold higher than the free form,thus dramatically enhancing the anticancer effect of gambogic acid.Furthermore,mild photothermal therapy also showed synergistic effect with the drug.CONCLUSION Au/TiO2 is a promising anticancer drug carrier.展开更多
The traditional Chinese medicine tripterygium glycosides(TPG)is used clinically to treat some Rheumatism,Eczema,immunosuppression and tumor,with the activities of hypnosis,antipyretic,analgesic,antiinflammatory,allerg...The traditional Chinese medicine tripterygium glycosides(TPG)is used clinically to treat some Rheumatism,Eczema,immunosuppression and tumor,with the activities of hypnosis,antipyretic,analgesic,antiinflammatory,allergy and antitumor.However TPG has low water solubility and low skin permeability,so its clinical use is limited.Transdermal delivery systems can provide a controlled drug release rate that can keep constant concentrations of drug in the plasma for up to multiple days,improved patient compliance,and the possibility ofreducing the rate and severity of side effects.In this study,a fast and sensitive technique skin-blood two sites synchronous microdialysis coupled with LC-MS was used to study the pharmacokinetic parameter of three different formulations(TPG nanoemulsion,TPG nanoemulsion based gels and TPG gel).Creating a multilayer model,use the model to simulate the three formulations dynamics in transdermal-drug delivery system.The experiment results showed that the TPG nanoemulsion,TPG nanoemulsion based gels can significantly raise the drug concentrations in skin more than that of TPG gels.The numerical simulation results indicating that TPG gel and TPG nanoemulsion are close to practical measurements,only in the concentration increase phase the numerical simulation result has some difference with the experimental results.TPG nanoemulsion based gels have significant difference with the experimental results,both in concentration increase stage and concentration decreasing stage,but its trend was same.The study shows that the skin-blood synchronous microdialysis technique provided a new method for the pharmacokinetics study of nanocarriers transdermal delivery systems.In addition,the microdialysis technique combined with mathematical modeling provides a very good platform for the further study of transdermal delivery system.展开更多
Many drug candidates identified from natural products are poorly water-soluble.The surfactants used to disperse the hydrophobic anticancer drugs in water may cause a serious of acute hypersensitivity reactions.Nanotec...Many drug candidates identified from natural products are poorly water-soluble.The surfactants used to disperse the hydrophobic anticancer drugs in water may cause a serious of acute hypersensitivity reactions.Nanotechnology provides an alternative strategy for delivery of anticancer drugs.Drugs can be encapsulated or attached to the nanomaterials such as lipids,polymers and solid-core nanoparticles.In the present study,porous inorganic nanoparticles have been utilized for delivery of water-insoluble anticancer drugs.The synthesized nanoparticles were functionalized with different organic polymers.The porous nanoparticles were readily internalized by human glioblastoma U-87 MG cells,and didn′t display cytotoxicity.The internalized nanoparticles were mainly localized in endosomes/lysosomes in cells.With the hydrophobic curcumin and carfilzomib as model drugs,intracellular delivery of hydrophobic anticancer drugs by the porous inorganic nanoparticles was studied.The porous nanoparticle-based encapsulation of hydrophobic drug provides the aqueous dispersion of the drugs.In endosomes/lysosomes mimicking buffers with a pH of 4.5-5.5,pH-dependent drug release was observed from drug loaded nanoparticles.The intracellular drug content and cytotoxicity were significantly higher for drug loaded nanoparticles than free drug.These results suggested porous inorganic nanoparticles might be a promising intracellular carrier for hydrophobic anticancer drugs.展开更多
OBJECTIVE To improve the anticancer drug gambogic acid’s effect by using titanium dioxide coated gold nanorods(GNR/Ti O2)as a drug carrier.METHODS Biocompatibility and cellular uptake of GNR/Ti O2was studied in human...OBJECTIVE To improve the anticancer drug gambogic acid’s effect by using titanium dioxide coated gold nanorods(GNR/Ti O2)as a drug carrier.METHODS Biocompatibility and cellular uptake of GNR/Ti O2was studied in human glioblastoma U-87 MG cells.Cel viability was evaluated by ATP assay and calcein AM staining.Lyso SensorTMGreen DND-189 and Hoechst 33342 were used to analyze the intracellular location of GNR/Ti O2.The in vitro anticancer effect of gambogic acid loaded nanoparticles was compared with free drug.RESULTS The results showed that GNR/Ti O2is biocompatible,andthey are localized at the intracellular acidic compartments of endosomes and lysosomes.The intracellular drug content delivered via GNR/Ti O2was 6 fold higher than the free form,thus dramatically enhancing the anticancer effect of gambogic acid.Furthermore,mild photothermal therapy also showed synergistic effect with the drug.CONCLUSION Our study suggested that GNR/Ti O2is a promising anticancer drug carrier。展开更多
OBJECTIVE Nanotechnology provides a novel strategy for the delivery of anticancer drugs.In this study,titanium dioxide coated gold nanorod(GNR/TiO_2) nanostructures were used as the drug carrier for gambogic acid in o...OBJECTIVE Nanotechnology provides a novel strategy for the delivery of anticancer drugs.In this study,titanium dioxide coated gold nanorod(GNR/TiO_2) nanostructures were used as the drug carrier for gambogic acid in order to improve its anticancer effect.METHODS Biocompatibility and cellular uptake of GNR/TiO_2 nanostructures were studied in human glioblastoma U-87 MG cells.Cell viability was evaluated by ATP assay and calcein AM staining.Lyso Sensor Green DND-189 and Hoechst 33342 were used to analyze the intracellular location of GNR/TiO_2 nanostructures.The in vitro anti-cancer effect of gambogic acid loaded nanoparticles was compared with free drug.RESULTS The results showed that GNR/TiO_2 nanostructures are biocompatible,and they are localized at the intracellular acidic compartments of endosomes and lysosomes.The intracellular drug content delivered via GNR/TiO_2 nanostructures was 6 fold higher than the free form,thus dramatically enhancing the anticancer effect of gambogic acid.Furthermore,mild photothermal therapy also showed synergistic effect with the drug.CONCLUSION Our study suggested that GNR/TiO_2 nanostructures can be considered as a promising anticancer drug carrier.展开更多
Alum has an excellent safety record and is the only licensed inorganic adjuvant for human vaccines.However,the exploration of alum nanosheets as chemotherapy drug delivery system,especially the clarification about the...Alum has an excellent safety record and is the only licensed inorganic adjuvant for human vaccines.However,the exploration of alum nanosheets as chemotherapy drug delivery system,especially the clarification about the relationship between structures and drug loading properties,is totally insufficient.Herein,aluminum hydroxides(AlOOH)nanosheets with tunable specific surface area and pore size were synthesized by adjusting the synthesis time in the presence of triblock copolymers.The obtained materials exhibited the highest surface area about 470 m2/g.The structure-dependent chemotherapy drug loading capability for AlOOH nanosheets was observed:the higher specific surface area and pore size are,the higher amount of chemotherapy drug is loaded.AlOOH nanosheets loaded with doxorubicin showed a pH-dependent sustained release behavior with quick release in low pH about 5 and slow release in pH around 7.4.Doxorubicin-loaded AlOOH nanosheets exhibited much higher cancer cellular uptake efficiency than that in free form by flow cytometry.Moreover,doxorubicin-loaded AlOOH nanosheets with high specific surface area showed an increased cellular uptake efficiency and enhanced ratios of apoptosis and necrosis,compared with those showing low specific surface area.Therefore,AlOOH nanosheets are promising materials as chemotherapy drug delivery system.展开更多
基金Macao Science and Technology Development Fund(FDCT)(014/2014/A1)
文摘OBJECTIVE Nanotechnology provides a novel strategy for the delivery of anticancer drugs.METHODS Titanium dioxide coated gold nanostructures(Au/TiO2)was used as the drug carrier for the natural anticancer drug gambogic acid in order to improve its anticancer effect.Biocompatibility and cellular uptake of Au/TiO2 was studied in human glio⁃blastoma U-87 MG cells.Cell viability was evaluated by ATP assay and calcein AM staining.LysoSensor Green DND-189 and Hoechst 33342 were used to analyze the intracellular location of Au/TiO2.The anticancer effect of gambogic acid loaded nanoparticles was compared with free drug.RESULTS Au/TiO2 was biocompatible,and they were localized at the intracellular acidic compartments of endosomes and lysosomes.The intracellular drug content delivered via Au/TiO2 was 6-fold higher than the free form,thus dramatically enhancing the anticancer effect of gambogic acid.Furthermore,mild photothermal therapy also showed synergistic effect with the drug.CONCLUSION Au/TiO2 is a promising anticancer drug carrier.
基金The project supported by National Natural Science Foundation of China(81573613,81373896)the Major Program for the Fundamental Research of Shanghai Committee of Science and Technology(14JC1491300)Open Fund of State Key Laboratory of Natural Medicines(SKLNMKF201612)
文摘The traditional Chinese medicine tripterygium glycosides(TPG)is used clinically to treat some Rheumatism,Eczema,immunosuppression and tumor,with the activities of hypnosis,antipyretic,analgesic,antiinflammatory,allergy and antitumor.However TPG has low water solubility and low skin permeability,so its clinical use is limited.Transdermal delivery systems can provide a controlled drug release rate that can keep constant concentrations of drug in the plasma for up to multiple days,improved patient compliance,and the possibility ofreducing the rate and severity of side effects.In this study,a fast and sensitive technique skin-blood two sites synchronous microdialysis coupled with LC-MS was used to study the pharmacokinetic parameter of three different formulations(TPG nanoemulsion,TPG nanoemulsion based gels and TPG gel).Creating a multilayer model,use the model to simulate the three formulations dynamics in transdermal-drug delivery system.The experiment results showed that the TPG nanoemulsion,TPG nanoemulsion based gels can significantly raise the drug concentrations in skin more than that of TPG gels.The numerical simulation results indicating that TPG gel and TPG nanoemulsion are close to practical measurements,only in the concentration increase phase the numerical simulation result has some difference with the experimental results.TPG nanoemulsion based gels have significant difference with the experimental results,both in concentration increase stage and concentration decreasing stage,but its trend was same.The study shows that the skin-blood synchronous microdialysis technique provided a new method for the pharmacokinetics study of nanocarriers transdermal delivery systems.In addition,the microdialysis technique combined with mathematical modeling provides a very good platform for the further study of transdermal delivery system.
基金Science and Technology Development Fund,Macao SAR(0168/2019/A3)。
文摘Many drug candidates identified from natural products are poorly water-soluble.The surfactants used to disperse the hydrophobic anticancer drugs in water may cause a serious of acute hypersensitivity reactions.Nanotechnology provides an alternative strategy for delivery of anticancer drugs.Drugs can be encapsulated or attached to the nanomaterials such as lipids,polymers and solid-core nanoparticles.In the present study,porous inorganic nanoparticles have been utilized for delivery of water-insoluble anticancer drugs.The synthesized nanoparticles were functionalized with different organic polymers.The porous nanoparticles were readily internalized by human glioblastoma U-87 MG cells,and didn′t display cytotoxicity.The internalized nanoparticles were mainly localized in endosomes/lysosomes in cells.With the hydrophobic curcumin and carfilzomib as model drugs,intracellular delivery of hydrophobic anticancer drugs by the porous inorganic nanoparticles was studied.The porous nanoparticle-based encapsulation of hydrophobic drug provides the aqueous dispersion of the drugs.In endosomes/lysosomes mimicking buffers with a pH of 4.5-5.5,pH-dependent drug release was observed from drug loaded nanoparticles.The intracellular drug content and cytotoxicity were significantly higher for drug loaded nanoparticles than free drug.These results suggested porous inorganic nanoparticles might be a promising intracellular carrier for hydrophobic anticancer drugs.
基金The project supported by Macao Science and Technology Development Fund(014/2014/A1)
文摘OBJECTIVE To improve the anticancer drug gambogic acid’s effect by using titanium dioxide coated gold nanorods(GNR/Ti O2)as a drug carrier.METHODS Biocompatibility and cellular uptake of GNR/Ti O2was studied in human glioblastoma U-87 MG cells.Cel viability was evaluated by ATP assay and calcein AM staining.Lyso SensorTMGreen DND-189 and Hoechst 33342 were used to analyze the intracellular location of GNR/Ti O2.The in vitro anticancer effect of gambogic acid loaded nanoparticles was compared with free drug.RESULTS The results showed that GNR/Ti O2is biocompatible,andthey are localized at the intracellular acidic compartments of endosomes and lysosomes.The intracellular drug content delivered via GNR/Ti O2was 6 fold higher than the free form,thus dramatically enhancing the anticancer effect of gambogic acid.Furthermore,mild photothermal therapy also showed synergistic effect with the drug.CONCLUSION Our study suggested that GNR/Ti O2is a promising anticancer drug carrier。
基金supported by Macao Science and Technology Development Fund(FDCT)(014/2014/A1)
文摘OBJECTIVE Nanotechnology provides a novel strategy for the delivery of anticancer drugs.In this study,titanium dioxide coated gold nanorod(GNR/TiO_2) nanostructures were used as the drug carrier for gambogic acid in order to improve its anticancer effect.METHODS Biocompatibility and cellular uptake of GNR/TiO_2 nanostructures were studied in human glioblastoma U-87 MG cells.Cell viability was evaluated by ATP assay and calcein AM staining.Lyso Sensor Green DND-189 and Hoechst 33342 were used to analyze the intracellular location of GNR/TiO_2 nanostructures.The in vitro anti-cancer effect of gambogic acid loaded nanoparticles was compared with free drug.RESULTS The results showed that GNR/TiO_2 nanostructures are biocompatible,and they are localized at the intracellular acidic compartments of endosomes and lysosomes.The intracellular drug content delivered via GNR/TiO_2 nanostructures was 6 fold higher than the free form,thus dramatically enhancing the anticancer effect of gambogic acid.Furthermore,mild photothermal therapy also showed synergistic effect with the drug.CONCLUSION Our study suggested that GNR/TiO_2 nanostructures can be considered as a promising anticancer drug carrier.
基金National Institute for Materials Science of Japan
文摘Alum has an excellent safety record and is the only licensed inorganic adjuvant for human vaccines.However,the exploration of alum nanosheets as chemotherapy drug delivery system,especially the clarification about the relationship between structures and drug loading properties,is totally insufficient.Herein,aluminum hydroxides(AlOOH)nanosheets with tunable specific surface area and pore size were synthesized by adjusting the synthesis time in the presence of triblock copolymers.The obtained materials exhibited the highest surface area about 470 m2/g.The structure-dependent chemotherapy drug loading capability for AlOOH nanosheets was observed:the higher specific surface area and pore size are,the higher amount of chemotherapy drug is loaded.AlOOH nanosheets loaded with doxorubicin showed a pH-dependent sustained release behavior with quick release in low pH about 5 and slow release in pH around 7.4.Doxorubicin-loaded AlOOH nanosheets exhibited much higher cancer cellular uptake efficiency than that in free form by flow cytometry.Moreover,doxorubicin-loaded AlOOH nanosheets with high specific surface area showed an increased cellular uptake efficiency and enhanced ratios of apoptosis and necrosis,compared with those showing low specific surface area.Therefore,AlOOH nanosheets are promising materials as chemotherapy drug delivery system.
