Concept Graphene, a single layer of sp2-hybridized carbon atoms arranged in a honeycomb two-dimensional (2-D) crystal lattice, has evoked enormous interest throughout the scientific community since its first appearance in 2004. Due to its unique structure and geometry, graphene possesses remarkable physical-chemical properties (including large specific surface area and biocompatibility) that enable it to be an ideal material for several applications, ranging from quantum physics, nanoelectronics, energy research, catalysis and engineering of nanocomposites and biomaterials. In the area of nanomedicine, graphene and its derivatives can be exploited for a broad range of applications, including a new generation of biosensors, nanocarriers for drug delivery and probes for cell and biological imaging [1]. In particular, graphene oxide (GO), synthesized by intensive oxidation of crystalline graphite and then turned into a monolayer material by sonication, consists of aromatic planes and polar functional groups which consequently provide it an excellent capability to adsorb aromatic compounds via ?-? stacking and hydrogen bonding. In order to improve its biocompatibility and physiological stability, some biocompatible polymer can be introduced onto GO. Among the commercially available polymers, poly(ethylene glycol) (PEG) is a very useful reagent in biology because of its minimal toxicity, biocompatibility, protein resistance, and good solubility in water or other common solvents [2]. Motivations and Objectives Sorafenib is a small molecule that acting as a multi-kinases inhibitor blocks tumor-cell proliferation and tumor angiogenesis. It increases the rate of apoptosis in a wide range of tumor models and is the first drug that is clinically approved for patients with advanced hepatocellular carcinoma (HCC) [3]. In the present study, we aimed to develop a GO-PEG based carrier for enhanced delivery and controlled release of sorafenib into specific cancer cells. Results and Discussion Herein, we developed a GO-PEG nanocarrier for enhanced delivery and controlled release of sorafenib into specific cancer cells. GO-PEG was first synthesized dispersing GO in bi-distilled water followed by adding PEG2000-NH2. For the preparation of sorafenib loaded GO-PEG a solution of sorafenib in DMSO was added to an aqueous GO-PEG dispersion at pH 8.4, and the obtained solution was kept under magnetic stirring at room temperature overnight. The empty and drug-loaded GO-PEG were characterized in terms of size, zeta potential, polydispersity, morphology and drug loading capacity. The release kinetic studies, carried out in an appropriate medium mimicking the physiological environment, confirmed that this system permits a controlled release of sorafenib.
Synthesis and characterization of PEGylated graphene oxide for sorafenib modified release
Erika Amore;
2015
Abstract
Concept Graphene, a single layer of sp2-hybridized carbon atoms arranged in a honeycomb two-dimensional (2-D) crystal lattice, has evoked enormous interest throughout the scientific community since its first appearance in 2004. Due to its unique structure and geometry, graphene possesses remarkable physical-chemical properties (including large specific surface area and biocompatibility) that enable it to be an ideal material for several applications, ranging from quantum physics, nanoelectronics, energy research, catalysis and engineering of nanocomposites and biomaterials. In the area of nanomedicine, graphene and its derivatives can be exploited for a broad range of applications, including a new generation of biosensors, nanocarriers for drug delivery and probes for cell and biological imaging [1]. In particular, graphene oxide (GO), synthesized by intensive oxidation of crystalline graphite and then turned into a monolayer material by sonication, consists of aromatic planes and polar functional groups which consequently provide it an excellent capability to adsorb aromatic compounds via ?-? stacking and hydrogen bonding. In order to improve its biocompatibility and physiological stability, some biocompatible polymer can be introduced onto GO. Among the commercially available polymers, poly(ethylene glycol) (PEG) is a very useful reagent in biology because of its minimal toxicity, biocompatibility, protein resistance, and good solubility in water or other common solvents [2]. Motivations and Objectives Sorafenib is a small molecule that acting as a multi-kinases inhibitor blocks tumor-cell proliferation and tumor angiogenesis. It increases the rate of apoptosis in a wide range of tumor models and is the first drug that is clinically approved for patients with advanced hepatocellular carcinoma (HCC) [3]. In the present study, we aimed to develop a GO-PEG based carrier for enhanced delivery and controlled release of sorafenib into specific cancer cells. Results and Discussion Herein, we developed a GO-PEG nanocarrier for enhanced delivery and controlled release of sorafenib into specific cancer cells. GO-PEG was first synthesized dispersing GO in bi-distilled water followed by adding PEG2000-NH2. For the preparation of sorafenib loaded GO-PEG a solution of sorafenib in DMSO was added to an aqueous GO-PEG dispersion at pH 8.4, and the obtained solution was kept under magnetic stirring at room temperature overnight. The empty and drug-loaded GO-PEG were characterized in terms of size, zeta potential, polydispersity, morphology and drug loading capacity. The release kinetic studies, carried out in an appropriate medium mimicking the physiological environment, confirmed that this system permits a controlled release of sorafenib.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
