METHODS: Valproic acid-encapsulated nanoemulsions were formulated and physically characterised (osmolarity, viscosity, drug content, drug encapsulation efficiency). Further investigations were also conducted to estimate the drug release, cytotoxic profile, in-vitro blood-brain barrier (BBB) permeability, pharmacokinetic parameter and the concentration of VPA and VANE in blood and brain.
KEY FINDINGS: Physical characterisation confirmed that VANE was suitable for parenteral administration. Formulating VPA into nanoemulsion significantly reduced the cytotoxicity of VPA. In-vitro drug permeation suggested that VANEs crossed the BBB as freely as VPA. Pharmacokinetic parameters of VANE-treated rats in plasma and brain showed F3 VANE had a remarkable improvement in AUC, prolongation of half-life and reduction in clearance compared to VPA. Given the same extent of in-vitro BBB permeation of VPA and VANE, the higher bioavailability of VANE in brain was believed to have due to higher concentration of VANE in blood. The brain bioavailability of VPA was improved by prolonging the half-life of VPA by encapsulating it within the nanoemulsion-T80.
CONCLUSIONS: Nanoemulsion containing VPA has alleviated the cytotoxic effect of VPA and improved the plasma and brain bioavailability for parenteral delivery of VPA.
METHODS: 1.5% (w/v) chitosan films with Chrysanthemum morifolium essential oil (0% to 6% (v/v)) were produced through homogenization, the casting of a film solution in a petri dish and convection drying. The edible film was evaluated in terms of its physical (color, thickness, water vapor permeability), mechanical (puncture strength, tensile strength, elongation at break) and chemical properties (antioxidant assay, Fourier Transform Infrared Spectroscopy (FTIR)).
RESULTS: With an increasing concentration of Chrysanthemum morifolium in the chitosan film, the test values of physical properties such as tensile strength, puncture force, and elongation at break declined significantly. However, the thickness, water permeability, and color profile (L*, a*, b*) values of the chitosan film increased. Similarly, the scavenging effect of antioxidant assay increased (from 4.97% to 18.63%) with a rise in Chrysanthemum morifolium concentration. 2%, 3%, and 4% of Chrysanthemum morifolium in the chitosan film showed a significant inhibition zone ranging from 2.67 mm to 3.82 mm against Staphylococcus aureus, a spoilage bacterium that is commonly found in chicken and beef products. The storage and pH tests showed that 4% of Chrysanthemum morifolium in the film maintained pH level (safe to consume), and the shelf life was extended from 3 days to 5 days of meat storage.
CONCLUSIONS: This study demonstrated that the incorporation of 4% (v/v) Chrysanthemum morifolium extract into 1.5% (w/v) chitosan film extends the storage duration of raw meat products noticeably by reducing Staphylococcus aureus activity. Therefore, it increases the quality of the edible film as an environmentally friendly food packaging material so that it can act as a substitute for the use of plastic bags. Future studies will be conducted on improving the tensile strength of the edible film to increase the feasibility of using it in the food industry. In addition, the microstructure and surface morphology of the edible film can be further determined.
METHODS: We investigated the ocular permeation of topical tazocin after single drop application in normal rabbit eyes by estimating piperacillin and tazobactam concentrations in cornea, aqueous, and vitreous using a validated LC-MS/MS method. Furthermore, we determined the efficacy of repeated dose administration of tazocin against experimentally induced P. aeruginosa keratitis in rabbits in comparison to moxifloxacin. To determine the efficacy, clinical examination, histopathological examination, and estimation of bacterial load and inflammatory cytokines in cornea were done.
RESULTS: Significant corneal concentration of piperacillin and tazobactam was detected in normal rabbit corneas after single dose treatment with tazocin. In rabbits with Pseudomonas-induced keratitis, topical tazocin caused significant clinical and histopathological improvement. This improvement was associated with reduction in corneal bacterial load and inflammatory cytokines. Compared to moxifloxacin 0.5%, tazocin treated group showed greater clinical response which was associated with higher interleukin (IL)-1β, lower tumor necrosis factor (TNF)-α, a comparable level of IL-8, greater reduction in corneal bacterial load, and lesser inflammatory cell infiltration.
CONCLUSION: Tazocin showed good ocular penetration and was effective in treatment of Pseudomonas induced keratitis in rabbits.