Mohsen Rezaei

Transferrin targeted liposomal 5-fluorouracil induced apoptosis via mitochondria signaling pathway in cancer cells

&NA; The purpose of this study was to prepare transferrin (Tf) targeted liposomal 5‐Fluorouracil (5FU) to improve the safety and efficacy of the drug. Liposomes were prepared using thin layer method. Morphology of liposomes was characterized by transmission electron microscopy (TEM) and their particle size was also determined. The in vitro cytotoxicity was investigated via MTT assay on HT‐29 (as cancer cell) and fibroblast (as normal cell). Moreover, cytotoxicity mechanism of targeted liposomes was determined through the production of reactive oxygen species (ROS), mitochondrial membrane potential (&Dgr;&PSgr;m) and release of cytochrome c. Results showed that encapsulation efficiency (EE%) was 58.66 ± 0.58 and average size of liposomes was 107 nm. Also, nano‐particles were spherical as shown by TEM. MTT assay on HT‐29 cells revealed the higher cytotoxic activity of targeted liposomes in comparison to free drug and non‐targeted liposome. In contrast, comparing with cancer cells, targeted liposomes had no cytotoxic effect on normal cells. In addition, targeted liposomes induced apoptosis through activation of mitochondrial apoptosis pathways, as evidenced by decreased mitochondrial membrane potential and release of cytochrome c. Results of the study indicated that targeted liposomes would provide a potential strategy to treat colon cancer by inducing apoptosis via mitochondria signaling pathway with reducing dose of the drug and resulting fewer side‐effects.

Folic acid-modified liposomal drug delivery strategy for tumor targeting of 5-fluorouracil

Abstract The aim of this study was to develop a liposomal formulation to selectively target cancer cells. Liposomes were prepared using thin layer method and folic acid (FA) was applied for targeted delivery of 5FU to cancer cells. Liposomes prepared were characterized for encapsulation efficiency (EE%), morphology and their particle size. Cellular uptake, cytotoxicity study and ROS production were evaluated using CT26 cell line. Hemolysis test was performed on rat red blood cells (RBCs). Moreover, the efficacy of targeted liposomes were investigated by in vivo antitumor activity and tissue toxicities were studied by histological examination. The EE% and average particle size of liposomes were 67.88 ± 1.84% and 114.00 ± 4.58 nm, respectively. TEM image revealed that liposomes were spherical in shape. Targeted liposomes showed higher cellular uptake, lower IC50 (12.02 &mgr;M compared to 39.81 &mgr;M for liposomal 5FU and 39.81 &mgr;M for free 5FU) and higher ROS production than free drug (62,271.28 vs 2369.55 fluorescence intensity) on cancer cells. Results of hemolysis assay confirmed the blood biocompatibility of the liposomes. Moreover, folate targeted liposomes showed better tumor inhibition than free drug (88.75 mm3 tumor volume vs 210.00 mm3) and no tissue abnormalities were found in histological examination. It can be concluded that folate targeted liposomes provide an effective and safe strategy for colon cancer targeted chemotherapy. Graphical abstract Figure. No caption available.

The chemical evolution of groundwater in the Kerman plain aquifer, Iran

A comprehensive hydrogeochemical study was carried out in the Kerman Plain Aquifer, Iran. Groundwater samples were collected from 58 sites. Groundwater was analysed for major constituents (Na+, K+, Ca2+, Mg2+, Cl–, SO42– HCO3–. Different methods including composite diagrams, saturation indices and multivariate statistical methods were employed in assessing groundwater quality. The results show that the main hydrochemical facies of the aquifer (Na+, K+– Cl– SO42–) represents 73% of the total wells. Calcite, dolomite, and gypsum solubilities were assessed in terms of the saturation index indicating supersaturation with respect to calcite and dolomite and undersaturation with respect to gypsum. Groundwater samples were classified into three distinctive groups using cluster analysis. The results of factor analysis indicate that four factors explain about 88.9% of the total sample variance. The variables underlying the first and the most important factor are mainly controlled by halite dissolution. Dissolution of gypsum is the second important source of salinity.

Effects of coating layer and release medium on release profile from coated capsules with Eudragit FS 30D: an in vitro and in vivo study

Abstract The aim of the present research was to evaluate the impact of coating layers on release profile from enteric coated dosage forms. Capsules were coated with Eudragit FS 30D using dipping method. The drug profile was evaluated in both phosphate buffer and Hank’s solutions. Utilization X-ray imaging, gastrointestinal transmission of enteric coated capsules was traced in rats. According to the results, no release of the drug was found at pH 1.2, and the extent of release drug in pH 6.8 medium was decreased by adding the coating layers. The results indicated single-layer coated capsules in phosphate buffer were significantly higher than that in Hank’s solution. However, no significant difference was observed from capsules with three coating layers in two different dissolution media. X-ray imaging showed that enteric coated capsules were intact in the stomach and in the small intestine, while disintegrated in the colon.