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.

No abstract

Clarithromycin (CLR) is a member of the macrolide antibiotic group. CLR has low systemic oral bioavailability and is a drug of class II of the Biopharmaceutical Classification System. In many studies, using nanoparticles (NPs) as a drug delivery system has been shown to increase the effectiveness and bioavailability of active drug substances. This study describes the development and evaluation of poly (lactic-co-glycolic acid) (PLGA) NPs and chitosan (CS)-coated PLGA NPs for oral delivery of CLR. NPs were obtained by nanoprecipitation technique and characterized in detail, and the effect of three molecular weights (Mw1: 7.000–17.000, Mw2: 38.000–54.000, Mw3: 50.000–190.000) of PLGA and CS coating on particle size (PS), zeta potential (ZP), entrapment efficiency (EE%), and release properties etc. were elucidated. Gastrointestinal stability and cryoprotectant effect tests were performed on the NPs. The PS of the prepared NPs were in the range of 178 to 578 nm and they were affected by the Mw and CS coating. In surface-modified formulations with CS, the ZP of the NPs increased significantly to positive values. EE% varied from 62% to 85%, depending upon the Mw and CS coating. In vitro release studies of CLR-loaded NPs showed an extended release up to 144 h. Peppas–Sahlin and Weibull kinetic model was found to fit best for CLR release from NPs. By the broth microdilution test method, the antibacterial activity of the formulations was determined on Staphylococcus aureus (ATCC 25923), Listeria monocytogenes (ATCC 1911), and Klebsiella pneumoniae (ATCC 700603). The structures of the formulations were clarified by thermal (DSC), FT-IR, and 1H-NMR analysis. The results showed that PS, ZP, EE%, and dissolution rates of NPs were directly related to the Mw of PLGA and CS coating.