Soluble ocular inserts of chloramphenicol were prepared with the aim of achieving once a day administration. Drug reservoir was prepared using hydrophilic polymer and rate-controlling hydrophobic polymer; Eudragit L100, Eudragit S100, Eudragit RL100. All the formulations indicated no interaction between drug and polymer in FTIR studies. The Inserts were evaluated for the several parameters, viscosity, drug–polymer interaction, in vitro drug release, sterility testing. They were also evaluated for % moisture loss, % moisture uptake,thickness, and tensile strength. Ophthalmic inserts provide that prolonged and sustained drug release. Ocular inserts prepared were smooth and passed all the evaluation tests performed. Mechanical properties and in vitro drug release were dependent on film composition. The release profile of all the formulations showed a steady, controlled drug release. Ocular inserts formulated also passed the test for sterility. In vitro studies demonstrated that P5 insert can ensure a sustained drug release on the ocular surface for a prolonged over 20 hours' time period. Also, reduction in frequency of administration, may improve the patient compliance.

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The Capillary Electrophoresis (CE) is a very useful technique to determine and to quantify pharmaceutical materials. In this work, a capillary electrophoresis method has been developed for the determination of Cefquinome sulfate in aqueous solution and in biological media (urine, milk and plasma). The ion mobility was measured at the various pH values. The detection limit and the relative standard deviation of migration times of the peak area were determined. The influence of the pH on the separation of Cefquinome sulfate in plasma and in urine was investigated. The SDS micellar elecrokinetic chromatography (SDS-MEKC) was used for the determination of Cefquinome sulfate in water, plasma and urine. The solubility and stability of Cefquinome sulfate were considered at the different pH values. The best stability was found at pH 7.4. Also the hydrophilic/lipophilic properties of Cefquinome sulfate (partition coefficient and permeation, in vitro) were investigated. The hydrophilic properties of cefquinome affected the results; the partition coefficient was 0.01 at pH 7.4. In addition, the permeation coefficient was 1.65 at pH 7.4. Acid the dissociation constant of cefquinome was calculated using CZE. The low amount of sample required and the relatively short analyze time were the main advantages of this method.

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Mucoadhesive oral delivery systems have been of interest to researchers because of improving bioavailability and patient compliance by increasing concentration gradient. This study aimed to investigate local delivery of vancomycin using against gram-positive bacteria. Vancomycin is not absorbed from the gastrointestinal tract, so it will be given by injection. Also, slow infusion of vancomycin in blood is so vital to reduce its severe side effects and is excreted through the urine. Controlled dose of vancomycin can reduce drug resistance. Here in, a blend of chitosan and gelatin loaded with vancomycin was electrospun. The obtained nanofibers were characterized by FTIR, UV and SEM. The swelling and stability of the nanofibers were evaluated. In vitro release of the vancomycin was measured over a 72-hours period by total immersion method. The average diameter of drug-loaded nanofiber was 384 nm. The release behavior of the optimum fibrous mat conform Higuchi kinetic model.

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The ample of studies show that Adriamycin caused hepatotoxicity in rat. The present study investigated the effects of Nigella Sativa (N. Sativa) and combination with Curcuma longa (C. longa) extract on Adriamycin-induced hepatotoxicity in rat. Rats were divided into eight experimental groups: Control (CO), Adriamycin (ADR), Vitamin C (Vit C), Adriamycin with Vitamin C (ADR+VitC), N. Sativa with and without Adriamycin (NS +ADR, NS -ADR), Combination extract of C. longa and N. Sativa with and without Adriamycin (NS+CL+ADR, NS+CL-ADR). Malondialdehyde (MDA) and thiol levels and also the activities of catalase (CAT) in liver tissue were evaluated. MDA level in the liver tissue in ADR was increased compared to CO group but in NS+ADR group, ADR+VitC and NS –ADR groups decreased compared to ADR group. Thiol levels in ADR and ADR+VitC groups were decreased compared to CO group. Thiol levels in treatment groups were increased compared to ADR group. The activities of CAT in liver tissue of ADR group were lower than CO group, and increased in treatment groups comparison with ADR group. The results showed that chronic administration of N. sativa hydroalcoholic extract in Adriamycin-induced hepatotoxicity rats could decrease the oxidative stress injuries in liver tissue.

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The physicochemical properties and binding potentials of defatted cake derived from Blighia sapida seeds (BSSC) were studied and compared with maize starch BP in ascorbic acid formulations. Milled seeds of Blighia sapida was macerated with n-hexane for 5 days to separate the oil, the resultant defatted cake was further extracted with a mixture of ethanol and water (4:10). The physicochemical properties of the BSSC were determined using standard procedures. Compatibility of BSSC powder with ascorbic acid was evaluated using Fourier Trans Infra-Red (FTIR) and Differential Scanning Calorimetry (DSC) techniques. Ascorbic acid tablets were formulated using varying concentrations of the BSSC as a binder at the same compression settings. The physical properties of formulated tablets were studied. BSSC had pH of 5.58 and a moisture content of 6.68 %. Its bulk and tapped density were 0.35 ± 0.3 g/mL and 0.45 ± 0.4 g/mL; the powder had fair flow with angle of repose 40 ± 1.5° and Hausner's ratio of 1.29. FITR technique showed that BSSC was compatible with ascorbic acid, however, the DSC thermogram showed that there was a well-defined interaction of the ascorbic acid and BSSC which were evidenced by the shift of the endothermic melting peak. The ascorbic acid tablets formulated using BSSC as binder had low friability; hard tablets with consistent disintegration rates and also similar binding properties to 2 %w/w maize starch BP were obtained. BSSC has similar binding properties compared to maize starch BP and can be a potential source of a low-cost binder.

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The Objective of the study was to prepare and design a stable formulation for self-emulsifying drug delivery system in order to enhance the solubility and oral absorption of a poorly-soluble drug, called griseofulvin. The prepared self-emulsifying systems were evaluated regarding their refractory index, particle size, emulsifying strength, drug release, and rat intestine permeability. The results showed that a mixture of oleic acid (as a fatty acid) with Labrafil-Tween 20 (as a surfactant), Labrafac PG (as a co-surfactant), and Poloxamer and hydroxypropyl methylcellulose (as a polymer) led to prepare stable emulsions with a refractive index higher than acidic medium and water. The particle size of the formulations was obtained between 310 to 834 nm. The particle size of samples was influenced by S/C ratios, so that the mean particle size decreases with an increasing in the S/C ratios. The percentage of drug release after 24 hours for formulations was 22.38 to 46.95. The correlation between the percentages of drug released after 24 hours with S/Oil and S/C ratios was significant. In Ex-vivo intestinal permeability, there was a significant and direct correlation between Q4 and surfactant/oil ratio. The selected formulations showed drug permeability through the rat intestine 3- folds more, compared with the control.

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Previous studies showed that palladacycle complexes with three phenyl phosphine ligands and piperidine or biphosphinic based palladacycle complexes were cytotoxic on K562, HT29, and Hela cell lines. In the present study, in order to evaluate the efficacy of the compound on cisplatin resistant cells, first we made HT-29 cells resistant to cisplatin, and then evaluated the potential cytotoxicity of the mentioned plladacylce complex on them. In addition, it was evaluated whether cytotoxic effect of the compound is mediated via apoptosis or necrosis death mechanisms. In this regard, Annexin V/PI by staining followed by flow cytometric analysis was performed. Results showed that palladacycle complexes were 45 times more cytotoxic than cisplatin (P<0.05) on the resistant HT-29 cells. Flow cytometry results also revealed that apoptosis induction was the major cell death mechanism of these compounds. Therefore, it could be concluded that these compounds might be effectively cytotoxic for cisplatin resistant cells. However, further in vitro and in vivo preclinical studies on evaluation of specific and non-specific cytotoxic characteristics of these complexes are necessary.

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Alzheimer's disease (AD) as form of senile dementia is a cognitive and neurodegenerative disorder as well as behavioral and psychological problems in the geriatric people. The disease is characterized by memory deficit as well as decline in daily activities. The deficiency of the cholinergic system is one the main causes of the disease. Some medications such as donepezil are capable of enhancement of the acetylcholine neurotransmitter via the inhibition of the acetylcholinesterase (AChE) enzyme. According to the positive background of the chalcone derivatives in inhibition of AChE, a new series of chalcone derivatives were synthesized using aldol condensation procedure and their enzyme inhibitory potency were assessed by Ellman's test. Some of the tested derivatives demonstrated superior activity than donepezil (IC₅₀ = 0.41 ± 0.09 μM) especially methoxylated compounds 3h (2-OCH₃, IC₅₀ = 0.1 ± 0.02 μM), 3i (3-OCH₃, IC₅₀ = 0.12 ± 0.03 μM) and 3j (4-OCH₃, IC₅₀ = 0.39 ± 0.04 μM). Compound 3b (3-Cl, IC₅₀ = 0.13 ± 0.03 μM) also possessed higher activity than donepezil. Molecular docking investigation also confirmed an effective hydrogen bonding interaction of 3h with AChE. In conclusion, the synthesized compounds could be suggested as new anti-acetylcholinesterase lead compounds.

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Low number of engrafted cells is the main challenge in stem cell therapy. The cells should overcome with reactive oxygen species, food deprivation and toxicity of the pharmacological agents that patients take during their treatment. As an example, cardiac glycosides such as digoxin can inhibit the cell proliferation and lead to apoptosis. Therefore, in this study, we are trying to know stem cell behavior following digoxin treatment. Mesenchymal Stem Cells were treated with different concentrations of digoxin for 6, 12, 24 and 48 hours. Cell viability was detected with trypan blue. Hoechst staining and tunnel assay were conducted to evaluate nuclear configuration and apoptosis in MSCs. Cell viability decreased after digoxin treatment in all groups during 6, 12, 24 and 48h significantly (P<0.05). After 6 hours, rate of nuclear fragmentation was significantly higher in30 and 40μM digoxin than control group (P< 0.001). Treatment with 20, 30 and 40μM digoxin led to nuclear damage significantly compare to control group after 12h (P< 0.001). Also, after 24 and 48 hours, nuclear damage significantly increased in 15, 20, 30 and 40μM of digoxin (P< 0.001).Digoxin induced apoptosis significantly in all groups in time and dose dependent, so that the highest rate of cell death was found after 48h.It is suggested that digoxin might lead to decline in cell survival and increase cell apoptosis in a dose and time dependent and interfere with stem cell therapy. Therefore, it is recommended to consider application of glycosides in concurrence with stem cell therapy.

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Ethanol induces different side effects on tissues and organs and it is associated with biochemical, physiological, and pathological alterations in the liver. Tragopogon graminifolius (TG) is traditionally used for the treatment of gastrointestinal disorders. The aim of present study was to investigate TG effect against ethanol induced liver enzyme (ALT, AST and ALP) and nitric oxide (NO) secretion in male rat. In this experimental study, 30 male Wistar rats (210 ±10 g) have been randomly divided into the experimental, ethanol and control groups (6/group). The experimental groups were received one of TG hydroalcoholic extract (50, 100 and 150 mg/kg) for 15 days orally. One ml of distilled water was given to ethanol and control group daily. At the day of 15th, ethanol (5 g/kg) was given to all groups orally except control group. After one hour, cardiac blood sample was collected and serum levels of ALT, ALP, AST and NO concentration were measured. Data were analyzed by one way-ANOVA test. Ethanol increased ATL, AST, AP and NO in the serum of male rat. Pretreatment with TG extract prevent increasing the serum level of ALT (p=0.001), ALP (p=0.004) and NO (p=0.000) significantly during ethanol consumption. Moreover, serum AST decreased in experimental groups (p>0.05). TG extract has protective effect on ethanol-induced liver toxicity in rats and also verified claims of traditional medicine about hepatoprotective function of TG.

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