The main challenges in treating cancer using chemotherapeutics are insufficient dose at the target site and the development of drug resistance, while higher doses can induce side effects by damaging nontarget tissues. Combinatorial drug therapy may overcome these limitations by permitting lower doses and more specific targeting, thereby mitigating drug resistance and nontarget side effects. Recent reports indicate that nonsteroidal anti-inflammatory drugs (NSAIDs) have anticancer potential and can be used together with conventional chemotherapeutics to improve efficacy and safety. In the present study, imatinib mesylate and dexketoprofen trometamol were selected as model drugs to develop targeted surface-modified liposome and nanocochleate formulations for fibrosarcoma treatment. The physicochemical properties and in vitro efficacy of various formulations were evaluated by measurement of particle size distribution, polydispersity index, zeta potential, encapsulation efficiency, diffusion through Caco-2 cells, and toxicity in culture. Selected formulations were then evaluated in fibrosarcoma-bearing model mice by histopathological observations and tyrosine kinase receptor inhibition assays.The most effective formulation on the fibrosarcoma model was a PEGylated nanocochleate formulation. These findings provide a foundation for developing more effective formulations and chemotherapeutic strategies for the treatment of fibrosarcoma and other types of cancer.

Wild animals, including wild boars, are suitable for use as bioindicators. The aim of this study was to evaluate the concentrations of selected essential (Co, Cu, Fe, Se, Zn) and non-essential (As, Cd, Pb) potentially toxic trace elements in various tissues (hair and hoof) of wild boars hunted in the vicinity of Antalya province in Turkey, in relation to hunting seasons. Concentrations in mg/kg on dry weight basis were determined as 0.37 ± 0.27 mg/kg for As, 0.05 ± 0.04 mg/kg for Cd, 0.24 ± 0.33 mg/kg for Co, 4.84 ± 2.48 mg/kg for Cu, 289.94 ± 165.26 mg/kg for Fe, 8.71 ± 15.68 mg/kg for Pb, 0.24 ± 0.10 mg/kg for Se, and 28.99 ± 21.41 mg/kg for Zn in the hair samples; and as 0.11 ± 0.04 mg/kg for As, 0.01 ± 0.04 mg/kg for Cd, 0.01 ± 0.01 mg/kg for Co, 1.03 ± 0.25 mg/kg for Cu, 56.88 ± 18.68 mg/kg for Fe, 0.30 ± 0.18 mg/kg for Pb, 0.11 ± 0.05 mg/kg for Se, and 17.91 ± 10.98 mg/kg for Zn in the hoof samples.

Abstract. Liposome (spherical vesicles) and cochleate (multilayer crystalline, spiral structure) formulations containing raloxifene have been developed having dimethyl-β-cyclodextrin (DM-β-CD) or sodium taurocholate (NaTC). Raloxifene was approved initially for the treatment of osteoporosis but it is also effective on breast tissue and endometrial cells. Raloxifene inhibits matrix metalloproteinase-2 (MMP-2) enzyme, which is known to be responsible for tumor invasion and the initiation of angiogenesis during the tumor growth. Therefore, raloxifene was selected as a model drug. A series of raloxifene-loaded liposome and cochleate formulations were prepared. In vitro release studies and in vivo tests were performed. Breast cancer cell lines (MCF-7) were also used to find the most effective formulation. Highest antitumor activity was observed, and MMP-2 enzyme was also found to be inhibited with raloxifene-loaded cochleates containing DM-β-CD. These developed formulations can be helpful for further treatment alternatives and new strategies for cancer therapy.

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