20 research outputs found

    Facile fabrication of fluorine free zirconium zinc stearate based superhydrophobic and superoleophilic coating on cotton fabric with superior antibacterial property

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    A simple solution technique has been adopted to fabricate in situ generated zirconium zinc stearate based superhydrophobic and superoleophilic fluorine-free coating on cotton fabric with superior antibacterial and excellent photocatalytic properties. The materials properties of the specimen such as crystallinity/crystal phase, chemical bonding, surface morphology, and surface roughness have been characterized systematically. The coated cotton derived from an optimized precursor composition shows the retention of superhydrophobicity with static water contact angle \~163 degrees after several cycles of machine laundering and mechanical abrasion. It is seen that zirconium species may have caused an enhancement in laundering durability and mechanical robustness while hierarchical morphology of zinc stearate is responsible for acquiring superior antibacterial property along with self cleaning ability of the coating to make the coated fabric promising for real life application such as military uniform, biomedical clothing/devices. In addition, the coated cotton is found to be suitable for separation of oil from oil-water mixtures with high efficiency (\~99%) even after 10 cycles of repeated use. Thus, the material can be used for separation of oil from oil-contaminated industrial wastewater/marine water. Moreover, AgBr modified superhydrophobic cotton fabric shows excellent photocatalytic activity towards degradation of organic dye. This facile process can be up-scaled for commercial u

    Formulation Development, Optimization, and Characterization of Cilnidipine-Loaded Self-microemulsifying Drug Delivery System

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    Cilnidipine, a 2, 4-dihydropyridine antihypertensive, is poorly bioavailable and belongs to Biopharmaceutical Classification System Class II. The present study was carried out to develop and evaluate a cilnidipine-loaded self-microemulsifying drug delivery system (SMEDDS) using food grade oil for enhanced pharmacokinetic parameters. The SMEDDS was prepared by low-energy method. A pseudo-ternary phase diagram was developed using triacetin, Tween 20, and Transcutol HP as oil, surfactants, and cosurfactants, respectively. The statistically optimized formulation was obtained and was evaluated for relevant in vitro characterizations. Globule size, zeta potential, and polydispersity index (PDI) of the optimized formulation were found to be 9.045 nm, −2.32 mv and 0.203, respectively, indicating stable and uniformly distributed microemulsion nature of the formulation. Developed SMEDDS of viscosity 31 cps was found to be clear in 500 times dilution in water and phosphate buffer pH 1.2. Selection of the optimized SMEDDS was followed by various formulation characteristics, including goat intestinal membrane permeability. The in vitro dissolution study of optimized SMEDDS exhibited much better result as compared to the marketed tablet of cilnidipine

    Synthesis and Characterization of Furo[3,2-h]Quinoliniums as Potent Non-Detergent Spermicides

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    7-Aryl substituted furo[3,2-h]quinoliniums have been synthesised in two steps from 5-chloro-8-hydroxy-7- iodo-quinoline through a tandem Sonogashira alkynylation-cyclization pathway using aryl acetylenes followed by quaternisation reaction with alkyl halides under microwave irradiation. The compounds have been characterized spectroscopically and assessed for their sperm-immobilizing efficacy in vitro by modified Sander–Cramer test. Most of the derivatives showed potent spermicidal effect with minimum effective concentration (MEC) ranging from 125�g/ml – 1mg/ml. The results were further confirmed by double fluoroprobe staining with syber14/PI (Propidium Iodide). The mode of spermicidal action was assessed by (a) Hypo-osmotic swelling tests and (b) Scanning electron microscopy. The compounds have been found to be nontoxic to lactobacillus in 36 hours of culture whereas mild to moderately effective on common vaginal pathogens. Taken together it can be inferred that the water-soluble salts prepared from facile technique are potential candidates for spermicides and could further be utilized for the preparation of vaginal contraceptives

    Synthesis, Characterization, and Biological Evaluation of 99mTc(CO)3-Labeled Peptides for Potential Use as Tumor Targeted Radiopharmaceuticals

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    During the past decade, several peptides containing Arg-Gly-Asp sequence have been conjugated with different chelating agents for labeling with various radionuclides for the diagnosis of tumor development. In this study, we report the synthesis of two tetrapeptides (Asp-Gly-Arg-His and Asp-Gly-Arg-Cys) and one hexapeptide [Asp-Gly-Arg-D-Tyr-Lys-His] by changing the amino acid sequence of the Arg-Gly-Asp motif. Peptide synthesis was initiated from aspartic acid. Aspartic acid placed at C-terminal end of the peptide chain can be conjugated with different drug molecules facilitating their transport to the site of action. The peptides were synthesized in excellent yield and labeled using freshly prepared [99mTc(CO)3(H2O)3]+ intermediate. A complexation yield of over 97% was achieved under mild conditions even at low ligand concentrations of 10�2 M. Radiolabeled peptides were characterized by HPLC and were found to be substantially stable in saline, in His solution as well as in rat serum and tissue (kidney, liver) homogenates. Internalization studies using Ehrlich ascites carcinoma cell line showed rapid and significant internalization (30–35% at 30 min of incubation attaining maximum value of about 40–60% after 2–4 h incubation). A good percentage of quick internalization was also observed in avb3-receptor-positive B16F10 mouse melanoma cell line (14–16% after 30 min of incubation and 25–30% after 2–4 h incubation). Imaging and biodistribution studies were performed in Swiss albino mice bearing Ehrlich ascites tumor in right thigh. Radiolabeled peptides exhibited fast blood clearance and rapid elimination through the urinary systems. 99mTc(CO)3-tetra-Pep2 exhibited remarkable localization at tumor site (1.15%, 1.17%, and 1.37% ID/g at 2, 4, and 6 h p.i., respectively) which could be due to slow clearance of the radiolabeled peptide from blood in comparison with the other two radiolabeled peptides. However, 99mTc(CO)3-hexa-Pep exhibited the highest tumor to muscle and tumor to blood ratios among the three. The preliminary results with these amino acid–based peptides are encouraging enough to carry out further experiments for targeting tumor

    Beverage-induced enhanced bioavailability of carbamazepine and its consequent effect on antiepileptic activity and toxicity

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    The present study was undertaken to investigate the food–drug interaction of carbamazepine (CBZ). Common fruit juices [grapefruit juice (GFJ), lime juice (LJ)], known to inhibit the enzyme cytochrome P450 3A4 (CYP3A4), and some widely consumed beverages [milk (M), black tea (BT)] were involved in this study in the presence of CBZ, as might happen during clinical therapy. The effects of the beverages on the pharmacokinetics and drug-induced toxicity of CBZ was observed after concomitant administration for a period of 28 days. Accordingly, the influence of altered bioavailability of CBZ on its antiepileptic activity was investigated. A significant shift in the Cmax as well as Tmax of CBZ was observed in the presence of LJ and GFJ. This increase in bioavailability significantly enhanced hepatotoxicity and delayed the onset of tremor and piloerection against pentylene tetrazole (PTZ)-induced seizure in experimental animals. However, increased toxicity of CBZ was found to be absent with BT. Thus, from our observation, LJ or GFJ in the presence of CBZ significantly increased the bioavailability of CBZ, which might lead to increased toxicity and antiepileptic activity of the drug

    Organic Cultivation of Tomato in India with Recycled Slaughterhouse Wastes: Evaluation of Fertilizer and Fruit Safety

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    Environmental and health safety of recycled slaughterhouse wastes-derived fertilizer and the produce obtained through its application is not well understood. Waste bovine blood and rumen digesta were mixed, cooked and sun-dried to obtain bovine-blood-and-rumen-digesta-mixture (BBRDM, NPK 30.36:1:5.75). 1.26 ± 0.18 log CFU mL−1 fecal coliforms were recovered in BBRDM. E. coli O157:H7, Mycobacteria, Clostridium sp., Salmonella sp., Bacillus sp. and Brucella sp. were absent. No re-growth of pathogens was observed after 60 days storage in sealed bags and in the open. However, prions and viruses were not evaluated. Heavy metals (Pb, Cr, Cd, Cu, Zn, As, Ni, Mn) concentrations in BBRDM were within internationally permissible limits. BBRDM was applied for field cultivation of tomato during 2012–2013 and 2013–2014. Lycopene and nitrate contents of BBRDM-grown tomatoes were higher than Diammonium phosphate (DAP) + potash-grown tomatoes because BBRDM supplied 2.5 times more the amount of nitrogen than DAP (NPK 18:46:0) + potash (NPK 0:0:44). Heavy metals and nitrate/nitrite concentrations in tomatoes were within internationally acceptable limits. BBRDM-grown tomatoes showed no mutagenic activity in the Ames test. Sub-acute toxicity tests on Wistar rats fed with BBRDM-grown tomatoes did not show adverse clinical picture. Thus, no immediate environmental or health risks associated with BBRDM and the tomatoes produced were identified

    Quality Related Safety Evaluation of a South African Traditional Formulation (PHELA<sup>®</sup>) as Novel Anti-Biofilm Candidate

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    A South African traditional formulation, PHELA®, is consumed by the traditional people for severe chest problems with coughing, diarrhea, oral ulcers etc. The present study focused on establishing the anti-infective properties of a safe and standardized poly-herbal formulation through a series of criteria and specifications
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