To improve the oral absorption of poorly water-soluble drugs by overcoming the intestinal epithelium barrier, calcium carbonate nanoparticles targeting to intestine peptide transporter 1（Pep T1） were fabricated by m...To improve the oral absorption of poorly water-soluble drugs by overcoming the intestinal epithelium barrier, calcium carbonate nanoparticles targeting to intestine peptide transporter 1（Pep T1） were fabricated by modification of the surface of calcium carbonate nanoparticles with Gly-Sar. Gly-Sar-conjugated TPGS was successfully synthesized and characterized, and coumarin 6-loaded Gly-Sar modified calcium carbonate nanoparticles were then prepared and characterized to have a nano-scaled size of about 193 nm in diameter, cracked surface morphology under a scanning electron microscope, and high drug loading efficiency（60.5±5.9）%. Moreover, the Gly-Sar-modified calcium carbonate nanoparticles exhibited better drug loading stability during the process of their transcellular transport, and evidently enhanced intestinal absorption of poorly water-soluble agents. Therefore, the designed intestine Pep T1-targeted calcium carbonate nanoparticles might have a promising potential for oral delivery of poorly water-soluble drugs.展开更多
In the present study,we combined CaCO_(3)NPs and Ce6 to construct CaCO_(3)-Ce6 nanoparticles (NPs).CaCO_(3)-Ce6 NPs were characterized in terms of particle size,zeta potential,UV-Vis absorption spectrum,fluorescence s...In the present study,we combined CaCO_(3)NPs and Ce6 to construct CaCO_(3)-Ce6 nanoparticles (NPs).CaCO_(3)-Ce6 NPs were characterized in terms of particle size,zeta potential,UV-Vis absorption spectrum,fluorescence spectrum,FTIR spectrum,and pH-responsive behavior.The reactive oxygen species (ROS) generation in vitro was measured in 4T1 cells.The results showed that CaCO_(3)-Ce6 NPs were uniform-sized NPs with excellent fluorescence properties and pH-responsive behavior.The ability of ROS generation by CaCO_(3)-Ce6 NPs was stronger compared with Ce6 in 4T1 cells because Ca;could enhance the ROS generation,which could contribute to a stronger anti-tumor effect.展开更多
基金The National Natural Science Foundation of China(Grant No.81673366)the National Key Science Research Program of China(973 Program,Grant No.2015CB932100)
文摘To improve the oral absorption of poorly water-soluble drugs by overcoming the intestinal epithelium barrier, calcium carbonate nanoparticles targeting to intestine peptide transporter 1（Pep T1） were fabricated by modification of the surface of calcium carbonate nanoparticles with Gly-Sar. Gly-Sar-conjugated TPGS was successfully synthesized and characterized, and coumarin 6-loaded Gly-Sar modified calcium carbonate nanoparticles were then prepared and characterized to have a nano-scaled size of about 193 nm in diameter, cracked surface morphology under a scanning electron microscope, and high drug loading efficiency（60.5±5.9）%. Moreover, the Gly-Sar-modified calcium carbonate nanoparticles exhibited better drug loading stability during the process of their transcellular transport, and evidently enhanced intestinal absorption of poorly water-soluble agents. Therefore, the designed intestine Pep T1-targeted calcium carbonate nanoparticles might have a promising potential for oral delivery of poorly water-soluble drugs.
文摘In the present study,we combined CaCO_(3)NPs and Ce6 to construct CaCO_(3)-Ce6 nanoparticles (NPs).CaCO_(3)-Ce6 NPs were characterized in terms of particle size,zeta potential,UV-Vis absorption spectrum,fluorescence spectrum,FTIR spectrum,and pH-responsive behavior.The reactive oxygen species (ROS) generation in vitro was measured in 4T1 cells.The results showed that CaCO_(3)-Ce6 NPs were uniform-sized NPs with excellent fluorescence properties and pH-responsive behavior.The ability of ROS generation by CaCO_(3)-Ce6 NPs was stronger compared with Ce6 in 4T1 cells because Ca;could enhance the ROS generation,which could contribute to a stronger anti-tumor effect.
