Development, in vitro and in vivo evaluation of dexketoprofen trometamol (DT)-loaded nanosized drug delivery system was aimed in this study. DT-loaded solid lipid nanoparticles (SLNs) were prepared using probe sonication. DT release from SLNs prepared and their kinetics were investigated. Structures of SLNs were elucidated by particle size and zeta potential measurements, shape and surface imaging, thermal analysis, X-ray diffraction, FT-IR and 1 H-NMR determinations. DT-loaded particles demonstrated characteristic plaque shapes while in vitro release studies showed extended release of DT. Korsmeyer-Peppas kinetic model was found to fit the best using DDSolver software program. Stability, cytotoxicity and in vivo animal experiments were further performed on DT-loaded SLN showing also prolonged analgesic activity in mice. Depending on the in vitro and in vivo test results, formulation developed in this study seems to prolong DT release and is promising for extending analgesic activity.

We report the synthesis and applications of a novel N-doped graphene quantum dots (GQDs) using hydrothermal reaction between citric acid and p-aminophenol. The synthesized N-doped GQDs have been characterized physico-chemically and evaluated its antioxidant, antimicrobial, DNA binding and cleavage activities. siRNA loading studies were performed and their effects on cells were evaluated. Obtained results indicate that monodisperse solution of N-doped GQDs has been obtained with particles size ca. ∼10.9 ± 1.3 nm. UV–Vis spectroscopy studies of the interactions between the N-doped GQDs and calf thymus DNA (CT-DNA) showed that the compound interact with CT-DNA via both intercalative and electrostatic binding. The DNA cleavage study showed that the N-doped GQDs cleaved DNA without any external agents. The antioxidant activity of N-doped GQDS was very active when compared to BHT. As the concentration of the compound increased, the antioxidant activity also increased. Cell viability assay demonstrated that the Ndoped GQDs showed cell viability (70%) when the concentration reached 200 μg/mL for A549 and also MDA-MB-231, 150 μg/mL for NIH-3T3 cell lines at 24 h incubation. N-doped GQDs were coated with Eudragit RS 100 and EphA2-siRNA was loaded. As a result of the studies on these formulations, it was concluded that there may be significant effects on A549 cells. The microscopy results revealed that N-doped GQDs was quickly internalized into the cell. Our novel N-doped-GQDs with siRNA are candidate for in situ tumor suppression via DNA and mRNA breakage.

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Purpose: To design, formulate and characterize sustained-release formulations of dexketoprofen trometamol (DT) nanoparticles (NPs) Methods: Dexketoprofen trometamol (DT)-loaded poly(lactic-co-glycolic acid) (PLGA) NPs were produced by double emulsion-solvent evaporation method. The NPs were variously characterized for drug loading and release, particle profile, as well as by thermal analysis, x-ray difraction (XRD), Fourier transform infrared spectroscopy (FTIR) and nuclear magnetic resonance analysis (1 H-NMR). Furthermore, the NPs were evaluated for cytotoxicity against NIH-3T3 cells by 3-(4,5-dimethylthiazol-2-Yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results: The DT-loaded NPs demonstrated nanostructural characteristics and extended drug release. Particle size was in the range of 243 and 295 nm which remained unchanged in drug stability testing in simulated gastrointestinal media. Encapsulation efficiency ranged from 49-64 % for all the formulations. Higuchi and Korsmeyer-Peppas were the best-fit release kinetic models for the NPs containing 5 and 10 % DT, respectively. The NPs with 10 % DT presented no significant cytotoxicty at the doses and periods studied. Conclusion: Stable and non-toxic DT NPs with potential for sustained and controlled release of the drug have been successfully developed.

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Ocular allergy is one of the most common disorders of the eye surface. Following diagnosis this condition is typically treated with preparations containing antihistamines. However, anatomy of the eye and its natural protective mechanisms create challenges for ocular drug delivery. Rapid elimination of antihistamine substances due to short residency times following application can lead to insufficient treatment of ocular allergies. With this in mind, the aim of this study was to prepare a controlled ocular delivery system to extend the retention time of olopatadine hydrochloride (OLO) and in doing so to reduce the need for frequent application. We developed extended-release ocular in situ gelling systems for which in vivo retention times were determined in sheep following in vitro characterization and cytotoxicity studies. In vivo results were then compared to commercially available Patanol eye drops. the transparent gels formulated using appropriate amounts of polymers and having longer ocular retention times appear to be a viable alternative to commercially available eye drops.