ABSTRACT
Background: Enhancing the therapeutic profile of hydrophobic drugs using the development of biocompatible drug delivery systems is an urgent need. Many types of research have been conducted on graphene derivatives owing to their unique characteristics. Methods: In this survey, quercetin (QUER), a natural medicine, was loaded on carboxylated graphene oxide (GO), and cytotoxicity assay and the uptake of QUER into prostate cancer cells (PC3) were evaluated. Results: The release behavior of QUER was temperature- and pH-sensitive. Although QUER was loaded with high efficiency, the released rate was low (23.25% at pH 5.5 and 42 °C). The toxicity and intensity of fluorescence in the FREE QUER were higher than the loaded form. Conclusion: High-capacity loading and controlled release of GO QUER can be recognized as a proper candidate in treating cancer.
Subject(s)
Antineoplastic Agents , Graphite , Antineoplastic Agents/pharmacology , Drug Delivery Systems , Graphite/chemistry , Humans , Male , Quercetin/pharmacologyABSTRACT
Free polymer graphene aerogel nanoparticles (GA NPs) were synthesized by using reduction/aggregation of graphene oxide (GO) sheets in the presence of vitamin C (as a biocompatible reductant agent) at a low temperature (40⯰C), followed by an effective sonication. Synthesis of GA NPs in doxorubicin hydrochloride (DOX)-containing solution results in the simultaneous synthesis and drug loading with higher performance (than that of the separately synthesized and loaded samples). To investigate the mechanism of loading and the capability of GA NPs in the loading of other drug structures, two groups of ionized (DOX, Amikacin sulfate and, d-glucosamine hydrochloride) and non-ionized (Paclitaxel (PTX)) drugs were examined. Furthermore, the relationship between the bipolar level of DOX solution (contributing to H-bonding of DOX and GO) and the amount of DOX loading was investigated. The DOX showed higher loading (>3 times) than PTX, as anticancer drugs. Since both DOX and PTX possess aromatic structures, the higher loading of DOX was assigned to its positive partial charge and ionized nature. Accordingly, other drugs (having positive partial charge and ionized nature, but no aromatic structure) such as Amikacin sulfate and d-glucosamine hydrochloride presented higher loading than PTX. These results indicated that although the π-π interactions induced by aromatic structures are important in drug loading, the electrostatic interaction of ionized drugs with GO (especially through H-bonding) is the dominant mechanism. DOX-loaded GANPs showed high pH-sensitive release (equivalent to the carrier weight) after 5 days, which can indicate benefits in tumor cell acidic microenvironments in-vivo.
Subject(s)
Antineoplastic Agents/chemistry , Doxorubicin/chemistry , Graphite/chemistry , Nanoparticles/chemistry , Paclitaxel/chemistry , Amikacin/chemistry , Drug Liberation , Gels/chemistry , Glucosamine/chemistry , Hydrogen-Ion Concentration , Particle Size , Surface PropertiesABSTRACT
The effect of graphene oxide (GO) and nanodiamond (ND) is investigated on the spectral properties of doxorubicin (DOX) fluorescence emissions in the form of (DOX+GO) and (DOX+ND) biomaterials. It is shown that carbon nanostructure additives lead to sensible blueshifts, due to their optical properties and surface functionality. The quenching coefficient KND is obtained to be KND=0.043 (µg/ml)-1 and KGO=0.342 (µg/ml)-1 in DOX solutions. In general, Stern-Volmer attests that excited (DOX+GO) strongly quenches with respect to that of (DOX+ND) regarding its privileged bonding affinity.
