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
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.
