Colon targeted delivery of niclosamide from ß-cyclodextrin inclusion complex incorporated electrospun Eudragit® L100 nanofibers.

Electrospun nanofibers incorporated with inclusion complex (IC) of niclosamide (NIC) and hydroxypropyl-beta-cyclodextrin (HPßCD) (NIC-HPßCD-IC) was produced from pH-responsive polymer (Eudragit® L100, EUD), which disintegrates at pH values higher than 6, (EUD-NIC-HPßCD-IC-NF) for targeted delivery of NIC to the colon. Pristine EUD nanofibers (EUD-NF), only NIC loaded (EUD-NIC-NF) and physical mixture of NIC and HPßCD loaded EUD nanofibers (EUD-NIC-HPßCD-NF) were also produced as reference. SEM images revealed the bead-free and uniform morphology of nanofibers. XRD, TGA, and DSC were also performed for both NIC-HPßCD-IC and electrospun nanofibers and it was seen that there are some NIC molecules, which cannot make IC. Dissolution studies were carried out for 240 min at pH 1.2 and pH 7 simulating stomach and colon, respectively. EUD-NIC-NF released almost 53 % of NIC in 120 min, whereas EUD-NIC-HPßCD-NF (15 %) and EUD-NIC-HPßCD-IC-NF (8 %) released at most 15 % of NIC in 120 min. Then, remained NIC in the nanofibers released into the colon for the next 120 min. The slight difference in the release of NIC into stomach from EUD-NIC-HPßCD-NF and EUD-NIC-HPßCD-IC-NF might be due to the uncomplexed NIC molecules in EUD-NIC-HPßCD-IC-NF. More importantly, EUD-NIC-HPßCD-IC-NF was quite effective for preventing the release of NIC in the stomach in contrast to EUD-NIC-NF, which has already released more than half amount of NIC in 120 min. In conclusion, this study might open new areas for developing targeted delivery systems by the combination of nanofibers and CD-ICs for hydrophobic drugs such as NIC.

Potency and use of chia mucilage coating containing propolis liquid extract for improves shelf-life of sea bass fillets.

BACKGROUND: In this study the effects of the use of chia mucilage - CM coating in combination with propolis liquid extract - PLE on the physico-chemical (total volatile basic nitrogen - TVB-N, peroxide value - PV, thiobarbituric acid - TBA) and bacteriological (total viable count - TVC, psychrophilic bacteria count -PBC) quality properties of sea bass fillets during storage at 2°C, as well as its potency, were investigated. METHODS: The fillets were randomly separated into four lots and subjected to the following treatments by dipping: chia mucilage - CM, chia mucilage + 0.1% PLE, chia mucilage + 0.3% PLE and control (uncoated), then stored at 2°C. RESULTS: The results showed that the chia musilage coating containing PLE was effective on TVC and PCA. While the shelf life of the control group was 8 days, the CM + 0.3% PLE group was 20 days. CONCLUSIONS: According to these results, it can be said that chia mucilage coating preserves the shelf life and quality of chilled seafood and can be used safely as a coating material.

Use of Spectroscopic Techniques to Monitor Changes in Food Quality during Application of Natural Preservatives: A Review.

Consumer demand for food of high quality has driven research for alternative methods of food preservation on the one hand, and the development of new and rapid quality assessment techniques on the other hand. Recently, there has been a growing need and interest in healthier food products, which has led to an increased interest in natural preservatives, such as essential oils, plant extracts, and edible films and coatings. Several studies have shown the potential of using biopreservation, natural antimicrobials, and antioxidant agents in place of other processing and preservation techniques (e.g., thermal and non-thermal treatments, freezing, or synthetic chemicals). Changes in food quality induced by the application of natural preservatives have been commonly evaluated using a range of traditional methods, including microbiology, sensory, and physicochemical measurements. Several spectroscopic techniques have been proposed as promising alternatives to the traditional time-consuming and destructive methods. This review will provide an overview of recent studies and highlight the potential of spectroscopic techniques to evaluate quality changes in food products following the application of natural preservatives.

Development and validation of highly selective method for the determination of imatinib mesylate and dexketoprofen trometamol combination in three different media

Imatinib mesylate is a small molecule used in cancer therapy as a thyrosine kinase inhibitor. Dexketoprofen trometamol is a non-steroidal anti-inflammatory drug that has seen use in cancer therapy in combination with an anticancer drug to minimize tumor size and to reduce pain in patients. In the present study, imatinib mesylate and dexketoprofen trometamol were selected as potential model drugs to be used in combination. A new, simple and selective Ultra Performance Liquid Chromatography method was developed and validated to determine the drug substances in distilled water, in a pH 7.4 phosphate buffer and in Dulbecco's Modified Eagle Medium. The proposed method was developed using a BEH C-18 column with isocratic elution. A mixture of methanol:acetonitrile (80:20, v/v) and pH 9.5, 0.05 M ammonium acetate were (70:30, v/v) used as a mobile phase. Detection was carried out with a flow rate of 0.3 mL/min, a column temperature of 30°C and an injection volume of 20 µL. The method was validated considering linearity, accuracy, precision, specificity, robustness, detection limit and quantitation limit values, and was found to be linear in a range from 0.05 to 20.0 µg/mL for the three different media

Novel water soluble BODIPY compounds: Synthesis, photochemical, DNA interaction, topoisomerases inhibition and photodynamic activity properties.

In this study, BODIPY compounds (2, 3, 5 and 6) bearing 3,4-bis(3-pyridin-3-ylpropoxy)benzyl, 4-(3-pyridin-3-ylpropoxy)benzyl groups were synthesized for the first time and further functionalized in a Knoevenagel condensation reaction with 3,4-bis(3-pyridin-3-ylpropoxy)benzaldehyde and 4-(3-pyridin-3-ylpropoxy)benzaldehyde. The water soluble derivatives of BODIPY compounds (3a and 6a) were synthesized by treating BODIPY compounds 3 and 6 with excess iodomethane in DMF. The photochemical properties and DNA binding modes of 3a and 6a were determined using ct-DNA by UV-Vis spectrophotometer and viscometer. DNA cleavage and topoisomerases inhibition properties were studied DNA using agarose gel electrophoresis. Their topoisomerase inhibition mechanisms were investigated at molecular level and correlations with the in vitro results were searched for using molecular docking method. In addition, cytotoxicity and phototoxicity of both compounds were performed on colorectal cancer cells (HCT-116) using MTT assay for 24 h. Annexin V-FITC/PI test was performed to determine the cell death mechanism of 6a induced by irradiation. Finally, 6a-loaded liposomes (LP6a) and PLGA nanoparticles (NP6a) were prepared and their cytotoxic and phototoxic effects were evaluated by MTT assay. The results claimed that 6a had great potential as photosensitizer agent for colorectal cancer owing to its photochemical, DNA interaction and phototoxic properties.

Efficacy of targeted liposomes and nanocochleates containing imatinib plus dexketoprofen against fibrosarcoma.

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.

Development of Nanocochleates Containing Erlotinib HCl and Dexketoprofen Trometamol and Evaluation of In Vitro Characteristic Properties.

OBJECTIVES: Erlotinib HCI is a tyrosine kinase receptor inhibitor and an anticancer agent that was first approved by the FDA in 2004 for treatment of non-small-cell lung cancer and pancreatic cancer. Dexketoprofen trometamol is a NSAID, but recent studies showed that dexketoprofen trometamol also had an effect in carcinoma due to its inhibitor effects on prostaglandins. The combination of dexketoprofen and anti-cancer agents reduces pain caused by cancer by diminishing the tumors pressure, which causes necrosis; it also lowers the poor prognosis of cancer. Combination therapy will make life easier for patients, considering drug administration and dosing. Nanocochleates are new drug delivery systems that have not been examined as much as liposomes, but they have more advantages than liposomes. MATERIALS AND METHODS: In this study, erlotinib HCl and dexketoprofen trometamol were loaded into nanocochleates with various formulations and particle sizes/distributions, polydispersity indexes, and zeta potential analyses were performed. Transmission electron microscopy imaging was performed with the obtained optimal formulation and drug-release studies using Franz diffusion cells were conducted. RESULTS: As a result, drug carrier systems with a particle size of 196.42-312.33 nm and zeta potential greater than 15 mV were produced. The highest encapsulation efficiency for the main active ingredient, erlotinib HCl, was obtained in the KOH-1B formulation with 86.22±1.45%. CONCLUSION: This study showed that the drugs were successfully loaded into the nanocochleates and the nanocochleates actively released the drugs.

Protective effect of essential oils on the shelf life of smoked and vacuum packed rainbow trout (Oncorhynchus mykiss W.1792) fillets.

This study was investigated the effects of some oils on chemical, microbiological and sensory quality in vacuum packed smoked rainbow trout (Oncorhynchus mykiss W.1792) fillets. Acceptability scores for appearance, taste and odour of untreated and treated smoked trout decreased with storage time. The limit of sensory acceptance was reached after 56 days for the untreated samples, after 84 days for with rosemary and thyme oil-treated samples after 98 days for with sage oil-treated and after 112 days for with clove oil-treated samples. Significant differences were not found between groups as microbiological (p > 0.05). However, significant differences were found both among groups and during the storage in term of TBA (thiobarbituric acid) and PV (peroxide value), FFA (free fatty acid) values (p < 0.05). Essential oils as natural antioxidant can be used in conjunction with vacuum packed to enhance hot smoked fish quality.