Formulization and characterization of guar gum and almond gum based composite coating and their application for shelf-life extension of okra (Hibiscus esculentus).

The current novel study aims was to development and characterization of gum based (guar gum: almond gum) composite formulations with or without addition of oregano essential oils to extend the shelf life of okra at ambient condition. In this study, the optimized composite of guar gum: almond gum (75:25 V/V) prepared with addition of different concentrations (0.05, 0.1 and 0.15 % (V/V) of oregano essential oils to study their physicochemical, rheological, antimicrobial and particle size & zeta potential distribution. In addition, the effects of prepared edible coatings on shelf-life of okra vegetables were also investigated by assessing their postharvest quality attributes at ambient (23 °C) storage up to 7 days storage. The results revealed, increasing concentration of essential oils in composite coating significantly increased in pH, TSS, particle size, antimicrobial (Apergillus. niger, Escherichia coli, Staphylococcus aureus) activity respectively. Furthermore, the increasing EOs improved viscosity (n) and stability of the coatings matrix. In addition, the applications of guar gum (0.25 %): almond gum (0.5 %) composite ratio (75,25) with oregano essential oils exhibited excellent properties and potential to maintain the postharvest characteristics of okra throughout the storage period. The results of this study revealed that the addition of higher concentration (0.15 %) of essential oils in composite formulation of 75 % guar gum +25 % almond gum (03) showed higher value of pH (5.45), antioxidant activity (20.87 %), particle size (899.1 nm), zeta potential (-8.6 mV), polydispersity index (50.6 %) and higher antimicrobial activity against E.coli (19 mm), S. aureus (29 mm) and A. niger (35 mm) as compared to other formulations. Therefore, the lower composite formulation (01) with lower concentration (0.05 %) of oregano essential oil was found most effective formulation to maintain the shelf life of okra for up to 4 days as compared to other treated and control okra samples at ambient temperature by retarded the weight loss (12.74 %), maintained higher firmness (0.998 N), lower respiration rate (484.32 ml Co2/kg/h) respectively on 7 days of storage. The microbial load in the okra samples treated with different guar gum: almond gum composite showed lower microbial load in terms of total plate count and yeast & mold counts as compared to control samples. Samples treated with O3 coating showed lowest TPC (0.1 × 108 cfu/g) and YMC (6.63 × 106 cfu/g) followed by O2 (0.48 × 108 cfu/g, 7.9 × 106 cfu/g) and O1 (0.78 × 108 cfu/g, 9.45 × 106 cfu/g) respectively on 6rd day of storage, overall results indicated that the application of composite coating with different concentrations of oregano essential oils were effective to maintained postharvest shelf life of okra up to 4 days at ambient condition.

Nose-to-brain delivery of octreotide acetate in situ gel for pituitary adenoma: Pharmacological and in vitro cytotoxicity studies.

Octreotide acetate (OA), a potent octapeptide, is used in the treatment of pituitary adenoma. An approach has been made in the present research to formulate an OA-loaded intranasal in situ gel (OA-ISG) to target pituitary adenoma. To achieve the objective of the present work, OA-ISG was fabricated using cold method, and further optimization was done by 32 factorial design. The optimized formulation was evaluated for gelation temperature, mucoadhesive strength, and % drug release (8 h), and the results were found to be 30.01 ± 0.4 °C, 40.12 ± 0.5 g, and 98.54 ± 0.45 %, respectively. Brain availability of OA was determined through gamma scintigraphy, wherein Cmax for technetium (99mTC) labeled intranasal OA-ISG (99mTC-OA-ISG) was found to be 1.041 % RA/g, and the findings for 99mTC-OA-Solution (intranasal) and 99mTC-OA-Solution (intravenous) were 0.395 % and 0.164 % RA/g, respectively. Consequently, a 3-10-fold increase in brain OA concentrations was observed upon intranasal administration (OA-ISG) as compared to others. Additionally, drug targeting index (100.13), targeting efficiency (10013 %), and direct transport percentage (2564.1 %) corroborate brain targeting of OA via intranasal route. Further, the cytotoxic potential of OA-ISG was screened on human pituitary tumor (GH3) cell lines using MTT assay. The IC50 value was found to be 9.5 µg/mL for OA-ISG, whereas it was 20.1 µg/mL for OA-Solution, thereby confirming the superior results of OA-ISG as compared to OA-Solution. Hence, the developed intranasal OA-ISG can be further explored for establishing its potential clinical safety, and as effective platform for targeted drug delivery to the brain in pituitary adenoma.

Facile synthesis of the spiro-pyridoindolone scaffold via a gold-catalysed intramolecular alkynol cyclisation/hydroindolylation.

A simple approach for the synthesis of pyridoindolone scaffolds with a spiroannulated tetrahydrofuran ring is described. The overall process comprises intramolecular sequential gold-catalysed 5-endo-dig alkynol cycloisomerization and subsequent addition of indole C2 to the in situ generated oxocarbenium cation.

An Apparent Umpolung Reactivity of Indole through [Au]-Catalysed Cyclisation and Lewis-Acid-Mediated Allylation.

The sequential functionalization of indole C2 and C3 in an umpolung fashion was executed with a predesigned substrate and choice of reagents. The developed method comprises gold-catalysed alkynol cycloisomerisation/intramolecular addition of C2 of indole and subsequent BF3 ⋅OEt2 -mediated regioselective C3 allylation, resulting in the synthesis of the functionalized indoloisoquinolinone scaffold. The reaction involves 5-endo-alkynol cycloisomerisation and the dearomative addition of indole C2 to the intermediate oxocarbenium cation, which results in two equilibrating fused and spiropentacyclic intermediates, which upon treatment with allyl silane in the presence of BF3 ⋅OEt2 , undergo selective indole C3 allylation. Other nucleophiles, such as hydride, azide and indole, were also found to be compatible with this process.

Withdrawal Notice: Drug Repurposing for Prospective Anti-Cancer Agents Along with the Clinical Status of the Repurposed Drug

The article has been withdrawn by the Editorial office of the journal Anti-Cancer Agents in Medicinal Chemistry because of the lack of clarity and obscurity in the content regarding language. Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused. The Bentham Editorial Policy on Article Withdrawal can be found at https://benthamscience.com/editorial-policiesmain.php Bentham Science Disclaimer: It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneously submitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewhere must be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submitting the article for publication the authors agree that the publishers have the legal right to take appropriate action against the authors, if plagiarism or fabricated information is discovered. By submitting a manuscript, the authors agree that the copyright of their article is transferred to the publishers if and when the article is accepted for publication.

Effect of binary combinations of solvent systems on permeability profiling of pure agomelatine across rat skin: a comparative study with statistically optimized polymeric nanoparticles.

Objective: Agomelatine (AGM), an antidepressant drug has low biological half-life coupled with extensive hepatic first-pass metabolism. For effective treatment of depression, daily medication is required but irregular dose intake occurs due to psychological illness which can be overcome by development of transdermal drug delivery system. But for effective transdermal delivery permeation of AGM through stratum corneum is a crucial step. Thus present study was intended to formulate and optimize polymeric nanoparticles of agomelatine and to compare the effect of binary combinations of solvent system on permeability profiling of pure agomelatine with statistically optimized polymeric nanoparticles.Methods: Polymeric agomelatine nanoparticles (AGM-PNPs) were prepared by nano-precipitation method which was further optimized by experimental design and characterized by FTIR, DSC, XRD and SEM study while ex-vivo study was performed on adult male wistar rats.Results: The optimized formulation has particle size in nano range (107.64 nm) with low PDI (0.209), stable zeta potential (-15 mV) and high entrapment efficiency (81.91%). Ex-vivo analysis of optimized nanoparticles suggests that nanoparticles permeate faster compared to plain AGM, while, permeation profile of AGM was enhanced when combination of solvent systems were used. It was observed that among various solvent system 33% PG-ethanol showed maximum flux (148.48 ± 3.24 µg/cm2/h) and least lag time (4.04 ± 0.12 h). The flux was further enhanced (180.98 ± 2.54 µg/cm2/h) when 5%v/v transcutol-HP was added as penetration enhancer.Conclusion: The above observations concluded that binary combination of 33% PG-ethanol with 5 %v/v transcutol-HP can serve as a solvent system of choice for effective transdermal delivery of agomelatine via nanoparticulate system.

Effect of Silver Nanowire Alignment on Electrical Resistance and Mechanical Reliability.

Given the increasing demands for high portability and large screens, electronic devices are evolving toward flexible electronics. Since the flexible devices will be operated by a current generated by repeated mechanical deformations, high mechanical stability, electrical conductivity, and optical properties of transparent conductive electrodes (TCE) under mechanical deformations are required; hence silver nanowire (AgNW) electrodes are attracting much interest. However, the anisotropic shape of AgNW can result in different electrical properties and mechanical reliability depending on the AgNW alignment. In this study, two kinds of AgNW films were prepared by roll-to-roll screening printing. One film has an isotropic arrangement of AgNW, the other an anisotropic arrangement, along the roll-to-roll machine direction (MD). These samples were cut with different directions from the MD. Whereas the isotropic sample exhibited an identical electrical resistance regardless of sample direction, the anisotropically aligned samples showed low resistance when parallel to the MD and high resistance when perpendicular to the MD. The mechanical reliability during repeated bending fatigue according to the AgNW alignment direction was also evaluated. Depending on the direction of alignment of the AgNW, the fatigue lifetime differed because the mechanical stability at the AgNW junction was different.

N-Bromosuccinimide promoted and base switchable one pot synthesis of α-imido and α-amino ketones from styrenes.

An N-Bromosuccinimide (NBS) promoted one pot strategy for the synthesis of α-amino functionalized aryl ketones starting from commercially available styrenes has been developed. NBS participates in multiple tasks, such as bromonium ion formation, oxidation of bromohydrin and providing a nucleophilic nitrogen source. The reaction can easily be switched between α-imido and α-amino ketones by the choice of base. This one pot strategy was successfully applied for the synthesis of psychoactive drug candidates, amfepramone, mephedrone and 4-MEC.

Gold(I)-catalyzed hydroindolylation of allenyl ethers.

The gold(i)-catalyzed reaction/rearrangement of allenyl ethers has been investigated in the presence of indoles. Either hydroindolylation or alkylation of an indole with the pendant group of allenyl ether has been observed. The reaction outcome seems to be decided mainly by the nature of the pendant group of the allenyl ether. Control experiments are indicative of an inner sphere mechanism for the hydroindolylation reaction.