The growing interest in high-energy emulsification is a result of its scalability, which is important from an industrial perspective and allows for a more reproducible and efficient production of pharmaceutical formulations. The aim of this study was to evaluate the effect of composition, mainly a fixed surfactant/cosurfactant (Smix) ratio, their concentration, and the parameters of high-pressure homogenization (HPH) processing on the quality and stability of ophthalmic fluconazole-loaded nanoemulsions. After a physicochemical analysis of nanoemulsions containing 20% w/w of oil, as optimal conditions for the HPH process, three cycles at a pressure of 1000 bar were established, obtaining formulations with an average droplet diameter size in the range of 80.63–129.68 nm and PDI values below 0.25. While it was expected that an increasing cosurfactant concentration decreased the droplet size, in the case of formulations containing Tween 20 and 10% w/w of cosurfactants, “over-processing” was observed, identified by the droplet size and polydispersity index increase. Consecutively, the selected formulations were evaluated for in vitro drug release in Franz’s cell, antifungal activity, and 30-day stability using NMR spectroscopy. An antifungal activity test showed no significant difference in the antifungal activity between optimal fluconazole-loaded nanoemulsions and a 0.3% aqueous drug solution, but previously, research showed that prepared formulations were characterized by a higher viscosity and satisfactory prolonged release compared to a control. In a 30-day stability study, it was observed that higher HLB values of the used surfactants decreased the stability of the formulations in the following order: Kolliphor EL, Tween 80, Tween 20. The NMR spectra confirmed that Kolliphor EL-based formulations ensured the higher stability of the nanoemulsion composition in comparison to Tween 80 and a better stabilizing effect of propylene glycol as a cosurfactant in comparison to PEG 200. Therefore, the optimization of HPH technology should be focused on the selection of Smix and the Smix:oil ratio in order to prepare stable formulations of high quality.
This study aimed to develop and optimize polyvinyl alcohol (PVA)-based polymeric films containing resveratrol (RSV) and to evaluate their applicability as oral mucosal wound dressings. Given the dynamic and complex nature of the oral environment, physicochemical parameters such as elasticity, mucoadhesive strength, and the release profile of the RSV were systematically investigated. The therapeutic performance of pure resveratrol was compared with that of an extract derived from Reynoutria japonica. Films were fabricated using a solvent casting method and characterized in terms of thickness uniformity, weight, color consistency, and flexibility, all of which met the required pharmaceutical criteria. Two tested formulations, FR2 (RSV/PVA/PVP/MCA15C/NaCMC/W/PGE), FE2 (extract/PVA/PVP/MCA15C/NaCMC/W/PGE), showed the best mucoadhesive properties (261.11 ± 0.5 g for FR2 and 299.43 ± 0.38 g for FE2) and a favorable release profile both in water (72.42% for FR2, 77.23% for FE2) and in saliva (49.74% for FR2, 49.70% for FE2). Moreover, the optimized films are characterized by hydrophilicity (contact angle < 90°) and the pH value of the extract after their blurring is close to physiological, which promotes better tolerance and reduces the risk of irritation. Obtained results for polymeric films with resveratrol and R. japonica extract confirmed their great potential for use in dentistry as modern, mucoadhesive dressings, improving the effectiveness of local therapies.
The combination of statins and fibrates in the treatment of lipid abnormalities effectively regulates individual lipid fraction levels. In this study, the screening and assessment of the physicochemical properties of simvastatin-fenofibrate solid dispersions were performed. Fenofibrate and simvastatin were processed using the kneading method in different weight ratios, and the resulting solid dispersions were assessed using differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), contact angle, as well as dissolution tests. The obtained results confirmed the formation of a simple eutectic phase diagram, with a eutectic point containing 79 wt% fenofibrate and 21 wt% simvastatin, lack of chemical interactions between the ingredients, and simvastatin impact on improving fenofibrate dissolution profile, due to the formation of crystalline solid dispersions by the kneading method.
Background/Objectives: The development of novel formulations that could have beneficial properties combined with dermatological procedures such as microneedling remains a challenge. The group of patients that could benefit from such a novel protocol is large and includes patients with acne scars. Both topical retinyl palmitate and the microneedling procedure have strong fibroblast-stimulating properties. Methods: In the study 5% w/w retinyl palmitate-loaded nanoemulsions and oleogel were prepared and examined to obtain formulations that meet criteria eligible for formulations combined with microneedling. All formulations were designed for aseptic preparation. Multiple nanoemulsion compositions were tested to select the optimal one. The selected 5% w/w retinyl palmitate-loaded nanoemulsion and oleogel were tested. Results: While retinyl palmitate-loaded oleogel met proper pharmacopeial norms for drug content and stability, the retinyl palmitate-loaded nanoemulsion, even though it demonstrated adequate physical parameters, maintained active substance losses during the manufacturing process above required limits. Conclusions: The retinyl palmitate-loaded nanoemulsion and oleogel remain promising formulations that could potentially be combined with microneedling. Considering its high sensitivity to manufacturing conditions, preparation of the retinyl palmitate-loaded nanoemulsion still remains a challenge.