title: Noncovalent Surface Locking of Mesoporous Silica Nanoparticles for Exceptionally High Hydrophobic Drug Loading and Enhanced Colloidal Stability.
abstract: Advances in water-insoluble drug delivery systems are limited by selective delivery, loading capacity, and colloidal and encapsulation stability. We have developed a simple and robust hydrophobic-drug delivery platform with different types of hydrophobic chemotherapeutic agents using a noncovalent gatekeeper's technique with mesoporous silica nanoparticles (MSNs). The unmodified pores offer a large volume of drug loading capacity, and the loaded drug is stably encapsulated until it enters the cancer cells owing to the noncovalently bound polymer gatekeeper. In the presence of polymer gatekeepers, the drug-loaded mesoporous silica nanoparticles showed enhanced colloidal stability. The simplicity of drug encapsulation allows any combination of small chemotherapeutics to be coencapsulated and thus produce synergetic therapeutic effects. The disulfide moiety facilitates decoration of the nanoparticles with cysteine containing ligands through thiol-disulfide chemistry under mild conditions. To show the versatility of drug targeting to cancer cells, we decorated the surface of the shell-cross-linked nanoparticles with two types of peptide ligands, SP94 and RGD. The nanocarriers reported here can release encapsulated drugs inside the reducing microenvironment of cancer cells via degradation of the polymer shell, leading to cell death.
authors.affiliation: Department of Chemistry, School of Natural Science, and ‡Department of Chemical Engineering, School of Energy and Chemical Engineering, Ulsan National Institutes of Science and Technology (UNIST) , Ulsan 689-798, Korea.
authors.forename: L
authors.initials: L
authors.lastname: Palanikumar
authors.affiliation: Department of Chemistry, School of Natural Science, and ‡Department of Chemical Engineering, School of Energy and Chemical Engineering, Ulsan National Institutes of Science and Technology (UNIST) , Ulsan 689-798, Korea.
authors.forename: Ho Young
authors.initials: HY
authors.lastname: Kim
authors.affiliation: Department of Chemistry, School of Natural Science, and ‡Department of Chemical Engineering, School of Energy and Chemical Engineering, Ulsan National Institutes of Science and Technology (UNIST) , Ulsan 689-798, Korea.
authors.forename: Joon Yong
authors.initials: JY
authors.lastname: Oh
authors.affiliation: Department of Chemistry, School of Natural Science, and ‡Department of Chemical Engineering, School of Energy and Chemical Engineering, Ulsan National Institutes of Science and Technology (UNIST) , Ulsan 689-798, Korea.
authors.forename: Ajesh P
authors.initials: AP
authors.lastname: Thomas
authors.affiliation: Department of Chemistry, School of Natural Science, and ‡Department of Chemical Engineering, School of Energy and Chemical Engineering, Ulsan National Institutes of Science and Technology (UNIST) , Ulsan 689-798, Korea.
authors.forename: Eun Seong
authors.initials: ES
authors.lastname: Choi
authors.affiliation: Department of Chemistry, School of Natural Science, and ‡Department of Chemical Engineering, School of Energy and Chemical Engineering, Ulsan National Institutes of Science and Technology (UNIST) , Ulsan 689-798, Korea.
authors.forename: M T
authors.initials: MT
authors.lastname: Jeena
authors.affiliation: Department of Chemistry, School of Natural Science, and ‡Department of Chemical Engineering, School of Energy and Chemical Engineering, Ulsan National Institutes of Science and Technology (UNIST) , Ulsan 689-798, Korea.
authors.forename: Sang Hoon
authors.initials: SH
authors.lastname: Joo
authors.affiliation: Department of Chemistry, School of Natural Science, and ‡Department of Chemical Engineering, School of Energy and Chemical Engineering, Ulsan National Institutes of Science and Technology (UNIST) , Ulsan 689-798, Korea.
authors.forename: Ja-Hyoung
authors.initials: JH
authors.lastname: Ryu
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D003102:Colloids; D004337:Drug Carriers / Q000737:chemistry / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007624:KB Cells; D053758:Nanoparticles / Q000737:chemistry*; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology; D016062:Porosity; D012822:Silicon Dioxide / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D003102:Colloids; D004337:Drug Carriers; D009842:Oligopeptides; D012822:Silicon Dioxide; C047981:arginyl-glycyl-aspartic acid