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EN
The active ingredients in the Elderflower liquid extract are responsible for the antibacterial, antioxidant and anti-inflammatory effects of the plant. The aim of the study was to design semisolid formulations with liquid Elderflower extract and evaluate the quality of them using a biopharmaceutical research method in vitro. The quality of the Elderflower (Sambucus nigra L.) extracts were evaluated spectrophotometrically by determining the total polyphenols and flavonoids content. Antiradical activity was determined by employing the spectrophotometrically DPPH free radical scavening method. Antibacterial activity was determined in vitro using the agar diffusion method. The biopharmaceutical experiment in vitro of the semisolid pharmaceutical formulations was performed by using modified Franz type diffusion cells. The results revealed that the highest amount of active compounds were found in the extracts when 70% (v/v) ethanol was used for the extraction of the raw material. The extracts obtained have antiradical activity and antimicrobial effects against S. aureus and B. cereus. Released amount of active compounds decreased when oleogel concentration in the formulation increased. The in vitro results of a biopharmaceutical semisolid formulation study showed that the base and the amount of excipients affected the release kinetics of the active compounds from the formulations. The results of the study showed that, as the lipophilicity and viscosity of the base increase, the formulation is characterized by a prolonged action: the release of the flavonoids, with the increase in the amount of oleogel, slow down. The best carrier of ederflower liquid extract was confirmed the hydrophilic base.
EN
Abstract: The purpose of this study was to develop and characterize novel gel formulations of oleogels and oleo-hydrogels (bigels) as topical drug delivery systems for ketoconazole (KET). Oleogels were prepared using paraffin oil, rapeseed oil or castor oil as a solvent and Aerosil® 200 as organogelator with addition of surfactant Tween 80. Bigels were prepared by mixing castor oil oleogels with sodium alginate hydrogel. The received formulations were analyzed microscopically, for pH, viscosity and the texture profile analysis was also conducted to examine the mechanical parameters. In addition, the in vitro release of KET was evaluated and ex vivo bioadhesive properties of obtained oleogels and bigels on the rat skin model were estimated. It was found that obtained formulations were non-Newtonian systems, showing a shear-thinning behavior and thixotropic properties, with proper textural features such as firmness, compressibility, adhesiveness. Moreover, they were characterized by beneficial bioadhesive properties. Prepared oleogels and bigels were considered as better formulations in terms of drug release compared to commercially available ketoconazole cream.
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