Prevalence of oral infections in diabetic patients is a health challenge due to persistent hyperglycemia. However, despite great concerns, limited treatment options are available. We therefore aimed to develop nanoemulsion gel (NEG) for oral bacterial infections based on essential oils. Clove and cinnamon essential oils based nanoemulgel were prepared and characterized. Various physicochemical parameters of optimized formulation including viscosity (65311 mPa·S), spreadability (36 g·cm/s), and mucoadhesive strength 42.87 N/cm2) were within prescribed limits. The drug contents of the NEG were 94.38 ± 1.12% (cinnamaldehyde) and 92.96 ± 2.08% (clove oil). A significant concentration of clove (73.9%) and cinnamon essential oil (71.2 %) was released from a polymer matrix of the NEG till 24 h. The ex vivo goat buccal mucosa permeation profile revealed a significant (52.7–54.2%) permeation of major constituents which occurred after 24 h. When subjected to antimicrobial testing, significant inhibition was observed for several clinical strains, namely Staphylococcus aureus (19 mm), Staphylococcus epidermidis (19 mm), and Pseudomonas aeruginosa (4 mm), as well as against Bacillus chungangensis (2 mm), whereas no inhibition was detected for Bacillus paramycoides and Paenibacillus dendritiformis when NEG was utilized. Likewise promising antifungal (Candida albicans) and antiquorum sensing activities were observed. It was therefore concluded that cinnamon and clove oil-based NEG formulation presented significant antibacterial-, antifungal, and antiquorum sensing activities.
The objective was to use caffeine and Soluplus® to improve the dissolution rate and to maintain a concentration of BCS Class II rosuvastatin calcium that exceeds its solubility. Caffeine and Soluplus® together substantially improved the dissolution rate and the extent of rosuvastatin release. Formulations for direct compression tablets included Formulation F1, a control with drug but with neither caffeine nor Soluplus® present; F2 with drug-caffeine complex; F3 with drug and Soluplus® and F4 with drug-caffeine complex and Soluplus®. Each formulation blend provided satisfactory flow properties. Tablets were comparable in mass, hardness and friability. A marked decrease in disintegration time occurred when the hydrotropic or micellar agent was included in the formulation. Assay (98-100%) and content uniformity (99-100%) results met requirements. Release studies in pH 1.2, 6.6, and 6.8 buffers revealed the superiority of F4. At 45 min sampling time, F3 and F4 tablets each provided a cumulative drug release greater than 70% in each medium. F2 tablets exhibited compliance to official standards in pH 6.6 and 6.8 buffers but not in pH 1.2 buffer, whereas tablets based on F1 failed in each medium. Two-factor ANOVA of the release data revealed a statistical difference across the four formulations in each release medium. Pairwise comparison of release profiles demonstrated that, of the four formulations, F4 provided the most effectively enhanced dissolution rate, improvement to the extent of drug release and support of a concentration higher than the solubility of rosuvastatin calcium.
Crude extracts prepared from aerial parts and nut galls of Quercus floribunda Lindl. Ex. A. Camus were evaluated for phytochemical screening, in vitro antioxidant, and in vivo analgesic, anti-inflammatory and antipyretic activities. Various solvents including methanol (M), acetone (A), distilled water (DW), distilled water + methanol (DWM) were used for extraction. Highest total phenolic (66.9 ± 0.05 μg GAE/mgE) and flavonoid content (38.4 ± 0.72 μg QE/mgE) were measured in QFAA extract by colorimetric methods. Cumulative maximum concentrations of polyphenols were quantified in QFMG, QFAA, and QFMA extracts i.e. 19.036, 15. 574 and 11.647 μg/mg of extract by RP-HPLC analysis. From aerial parts extracts, apentacyclic tritepenoid, glutinol was isolated using column chromatography techniques and structure was elucidated using spectroscopic techniques. QFDWMA (205.5 ± 0.56 μg AAE/mg of extract) showed highest total reducing power while highest total antioxidant capacity (207.1 ± 0.49 AAE/mg of extract) and free radical scavenging potential (96.1 ± 0.42%) were observed in QFAA extract. QFAA extract showed significant (p ≤ 0.001) analgesic potential in different pain models i.e. hot plate method, cold plate method, Haffner's tail clip method and acetic acid induced writhing assay having 50.20%, 62.07%, 57.26% and 70.49% analgesia respectively at 300 mg/kg. QFAA extract showed maximum anti-inflammatory activity in croton oil induced edema (68.83%) and in carrageenan induced paw edema models (72.32%) at 300 mg/kg concentration. QFAA extract markedly reduced the rectal temperature at 300 mg/kg concentration, in brewer's yeast induced pyrexia model. Detailed investigations can be executed in future to determine the molecular mechanisms of these pharmacological attributes.