Materials and Methods: The rats were divided into four groups: i) Normoxia treated with sucrose (n=12), ii) Normoxia treated with Tualang honey (n=12), iii) Hypoxia treated with sucrose (n=12), and iv) Hypoxia treated with Tualang honey (n=12). Tualang honey (0.2 g/kg/BW) and sucrose (1 mL of 7.9%) supplementations were administered orally to the rats daily for 14 days. Then the hypoxia groups were exposed to hypoxia (~11%) for 7 days, while the normoxia groups were kept in normal conditions. Following exposure to hypoxia, the rats' memories were analyzed using a novel object recognition task and T-maze test.

Results: The data revealed that rats exposed to hypoxia showed significant impairment in short-term memory (STM), spatial memory (p<0.01), and long-term memory (LTM) when compared to the normoxia group. Hypoxia rats treated with Tualang honey showed significant improvement in STM, LTM, and spatial memory (p<0.05) compared with those treated with sucrose (p<0.05). Tualang honey also reduced neuronal damage in the hippocampus of adult male Sprague Dawley rats exposed to hypoxia.

Materials and Methods: Twenty-four pregnant rats were randomly grouped into a control group (C), a stress group (S), and a stress group treated with TH. Eight male pups from each group were randomly chosen and they were sacrificed at eight or ten weeks of age following the novel object recognition test. Their brains were removed and histological changes and levels of MDA and NMDA receptors in the hippocampus were determined.

Results: The offspring from TH group showed significantly increased preference index (p<0.05) with higher neuronal number compared to S group. A significantly lower level of MDA and NMDA receptors were shown in TH group (P<0.01; P<0.05 respectively) compared to S group. The parameters investigated were not significantly different between C and TH groups.

Materials and Methods: Biodegradable polymeric microneedle arrays were fabricated out of poly lactic-co-glycolic acid (PLGA) using the micromolding technique under aseptic conditions, and the morphology of the microneedles was characterized using light microscopy. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis was used to rule out drug-polymer interactions. Standard procedures were used to analyze the prepared microneedle arrays for in vitro drug release and to perform a microneedle insertion test. Enzyme-linked immunosorbent assay was used to quantify rHuKGF.

Results: The PLGA polymer was safe for use in the fabrication of rHuKGF microneedles as there was no interaction between the drug and the polymer. The fabricated rHuKGF microneedle arrays had fully formed microneedles with a height of 600 µm and a base of 300 µm. The drug from the microneedle patch was released in vitro within 30 minutes. The strength of the microneedles in the patch was good, as they were able to reach a depth of 381±3.56 µm into parafilm without any structural change or fracture.

Materials and Methods: We have developed and validated 2D and 3D QSAR models by using multiple linear regression, partial least square regression, and k-nearest neighbor-molecular field analysis methods.

Results: 2D QSAR models had q2: 0.950 and pred_r2: 0.877 and 3D QSAR models had q2: 0.899 and pred_r2: 0.957. These results showed that the models werere predictive.

Materials and Methods: Twenty gel matrices were prepared with different durations of microwave irradiation, amounts of maize, and concentrations of sodium bicarbonate as suggested by Design Expert (DX®). The percentage drug release, the coefficient of variance (CV) in release, and the mean dissolution time (MDT) were the properties explored in the designed experimentation.

Results: Target responses were dependent on microwave irradiation time, cross-linker amount, and salt concentration. Classical and microwave heating did not demonstrate statistically significant difference in modifying the percentage of drug released from the matrices. However, the CVs of microwave-assisted formulations were lower than those of the gel matrices prepared via classical heating. Thus, microwave heating produced lesser variations in drug release. The optimized gel matrices demonstrated that the observed percentage of drug release, CV, and MDT were within the prediction interval generated by DX®. The release mechanism of the matrix formulations followed the Peppas-Korsmeyer anomalous transport model.

Materials and Methods: The formulation design was based on the independent formulation variables of the concentration of chitosan and sodium tripolyphosphate using a simple factorial design experiment. DEET-loaded microparticles were developed and incorporated into a hydrogel. The size of the microparticles was analyzed using the Zetasizer Nano® particle size analyzer, and the surface morphology, using field emission scanning electron microscopy. Drug release from the microparticles was determined by the dialysis bag method. A rheological evaluation of the formulated gel was performed using a Thermo Haake Rheometer. The in vitro permeation of the formulation was performed using a synthetic Strat-M® membrane.

Results: The size of the microparticles ranged from 0.45 to 8.3 μm, and the encapsulation efficiencies were >50% for all the formulations. The drug-release curves showed no initial burst release from the microparticle formulation. Instead, a slow and controlled drug release was observed over 24 hours that followed Higuchi kinetics. The cumulative amount of DEET permeated (over 24 h) from the DEET solution (control), and the formulation was 211.6±19.5 μg/cm2 and 4.07±0.08 μg/cm2, respectively.

Materials and Methods: The 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide assay was used to determine the cytotoxic effect of MPSE treatment at concentrations ranging from 31.15 to 1000 μg/mL. The NO concentration was determined by Griess assay and IL-1β proinflammatory cytokine concentration by enzyme-linked immunosorbent assay in the supernatant of MPSE-treated LPS-activated J774A.1 cell culture.

Results: The results show that the MPSE was not cytotoxic at 1000 μg/mL but significantly (p<0.001) inhibited NO and IL-1β production by the LPS-activated macrophage J774A.1 cells.

Materials and Methods: The synthesis was accomplished by the reaction of 2,3-dihydro-1,4-benzodioxin-6-amine (1) with 4-methylbenzenesulfonyl chloride (2) using 10% aqueous Na2CO3 to afford N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-methylbenzenesulfonamide (3). Further the parent molecule 3 was reacted with different alkyl/aralkyl halides (4a-e) to achieve N-(alkyl/aralkyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-methylbenzenesulfonamides (5a-e), using polar aprotic solvent; N,N-dimethylformamide (DMF) and catalytic amount of lithium hydride as base. The characterization of synthesized compounds was conducted by contemporary spectral techniques e.g., IR, 1H-NMR and EI-MS. Then these molecules were subjected to screening against various bacterial strains and their inhibitory potential against Lipoxygenase was also ascertained.

Results: The screening results against various Gram-positive and Gram-negative bacterial strains revealed that N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-methylbenzenesulfonamide (3), N-(2-bromoethyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-methylbenzenesulfonamide (5a) and N-(2-phenethyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-methylbenzenesulfonamide (5b) showed good inhibitory activity as compared to standard Ciprofloxacin. Moreover, N-(3-phenylpropyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-methylbenzenesulfonamide (5c) and N-(4-chlorobenzyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-methylbenzenesulfon-amide (5e) displayed decent inhibition against lipoxygenase enzyme relative to standard Baicalein.

MATERIALS AND METHODS: In situ gels containing 0.5% w/v OS extract prepared using cold dispersion method were subjected to physicochemical characterization, including in vitro-release studies. Antimicrobial efficacy was tested against Staphylococcus aureus, Micrococcus luteus, Escherichia coli, and Pseudomonas aeruginosa using agar diffusion method.

RESULTS: Thin layer chromatography and high performance liquid chromatography chromatograms confirmed the presence of rosmarinic acid (RA) and sinensitin in OS extracts with same retention factor (0.26 and 0.49) and retention times (12.2 and 20.7 min) against reference standards. A homogenous brown coloured in situ gel exhibited low viscosity as a solution and increased viscosity in gel form at ocular temperature. The optimized formulations, P7 (21% P407/4% P188), P8 (21% P407/5% P188) and F5 (1.5% chitosan and 45% β-glycerophosphate) exhibited ideal ocular pH (7.27-7.46), phase transition at ocular temperature (33-37°C) and prolonged RA release up to 12 h. Formulation F5 showed an inhibition zone of 4.3 mm against M. luteus.

MATERIALS AND METHODS: As a prerequisite for this, the solubility of the drug was assessed in media of different pH (1.2-7.4), and surfactant concentrations of 0.5-1.5% (w/v) sodium lauryl sulfate (SLS) in water, and pH 7.4 phosphate buffer. The dissolved drug concentration in each medium was quantified by UV analysis at 280 nm wavelength.

RESULTS: The drug solubility was found to be high at a pH of 1.2 and 7.4. The media with surfactant enhanced solubility of the drug by approximately 17-fold and exhibited better sink conditions. The discriminative power of the developed dissolution medium (i.e., 1% w/v SLS in pH 7.4) was determined by performing in vitro dissolution studies of the prepared THC tablets and comparing their release profiles using fit factors (f1 and f2). The results of the fit factor comparisons made between the dissolution profiles of THC tablets proved the discriminative ability of the medium. The validation of the developed dissolution method was performed by international guidelines and the method showed specificity, linearity, accuracy, and precision within the acceptable range.