Elwira Lasoń

The aim of the study was to obtain stable systems of lipid-based nanocarriers (SLN, NLC, HA-NLC, liposomes) with a selected berry polyphenol – quercetin as an active ingredient. Lipid-based nanosystems were obtained using ultrasonification technique. The stability was assessed by macro- and microscopic observation and viscosity measurements. The physicochemical properties of both incorporated and nonincorporated carriers were examined with dynamic light scattering technique (DLS). In vitro release studies of quercetin were performed using cellulose membrane and the mixture of PBS/ethanol as an acceptor solution. The lowest average particle size was achieved for the traditional NLC formulation and ranged between 126:5 ± 1:6 nm for unloaded and 138:7 ± 1:0 nm for NLC with quercetin. Release study of the active ingredient from optimal lipid-based nanocarriers indicated its prolonged and controlled release profile. On this basis, a mathematical model that best describes the kinetics of the active substance release from the tested carriers was fitted. According to the results, the best fit of quercetin release from examined nanocarriers was obtained for the Higuchi model. The conducted research gave promising results allowing to conclude that the obtained lipid-based nanosystems may be potential carriers for quercetin which possess a therapeutic effect in the treatment of skin disorders.

Psoriasis, a prevalent inflammatory skin disorder affecting a significant percentage of the global population, poses challenges in its management, necessitating the exploration of novel cost-effective and widely accessible therapeutic options. This study investigates the potential of ursolic acid (UA), a triterpenoid known for its anti-inflammatory and pro-apoptotic properties, in addressing psoriasis-related inflammation and keratinocyte hyperproliferation. The research involved in vitro models employing skin and immune cells to assess the effects of UA on psoriasis-associated inflammation. The presented research demonstrates the limiting effects of UA on IL-6 and IL-8 production in response to the inflammatory stimuli and limiting effects on the expression of psoriatic biomarkers S100A7, S100A8, and S100A9. Further, the study reveals promising outcomes, demonstrating UA’s ability to mitigate inflammatory responses and hyperproliferation of keratinocytes by the induction of non-inflammatory apoptosis, as well as a lack of the negative influence on other cell types, including immune cells. Considering the limitations of UA’s poor solubility, hybrid systems were designed to enhance its bioavailability and developed as hybrid nano-emulsion and bi-gel topical systems to enhance bioavailability and effectiveness of UA. One of them in particular–bi-gel–demonstrated high effectiveness in limiting the pathological response of keratinocytes to pro-psoriatic stimulation; this was even more prominent than with ursolic acid alone. Our results indicate that topical formulations of ursolic acid exhibit desirable anti-inflammatory activity in vitro and may be further employed for topical psoriasis treatment.

Psoriasis is a chronic disorder that causes a rash with itchy, scaly patches. It affects nearly 2–5% of the worldwide population and has a negative effect on patient quality of life. A variety of therapeutic approaches, e.g., glucocorticoid topical therapy, have shown limited efficacy with systemic adverse reactions. Therefore, novel therapeutic agents and physicochemical formulations are in constant need and should be obtained and tested in terms of effectiveness and minimization of side effects. For that reason, the aim of our study was to design and obtain various hybrid systems, nanoemulgel–macroemulsion and nanoemulgel–oleogel (bigel), as vehicles for ursolic acid (UA) and to verify their potential as topical formulations used in psoriasis treatment. Obtained topical formulations were characterized by conducting morphological, rheological, texture, and stability analysis. To determine the safety and effectiveness of the prepared ursolic acid carriers, in vitro studies on human keratinocyte cell-like HaCaT cells were performed with cytotoxicity analysis for individual components and each formulation. Moreover, a kinetic study of ursolic acid release from the obtained systems was conducted. All of the studied UA-loaded systems were well tolerated by keratinocyte cells and had suitable pH values and stability over time. The obtained formulations exhibit an apparent viscosity, ensuring the appropriate time of contact with the skin, ease of spreading, soft consistency, and adherence to the skin, which was confirmed by texture tests. The release of ursolic acid from each of the formulations is followed by a slow, controlled release according to the Korsmeyer–Peppas and Higuchi models. The elaborated systems could be considered suitable vehicles to deliver triterpene to psoriatic skin.

Terpenes are a group of phytocompounds that have been used in medicine for decades owing to their significant role in human health. So far, they have been examined for therapeutic purposes as antibacterial, anti-inflammatory, antitumoral agents, and the clinical potential of this class of compounds has been increasing continuously as a source of pharmacologically interesting agents also in relation to topical administration. Major difficulties in achieving sustained delivery of terpenes to the skin are connected with their low solubility and stability, as well as poor cell penetration. In order to overcome these disadvantages, new delivery technologies based on nanostructures are proposed to improve bioavailability and allow controlled release. This review highlights the potential properties of terpenes loaded in several types of lipid-based nanocarriers (liposomes, solid lipid nanoparticles, and nanostructured lipid carriers) used to overcome free terpenes’ form limitations and potentiate their therapeutic properties for topical administration.

The application of nanoemulsions as a novel delivery system for lipophilic materials, such as essential oils, flavors, and fragrances is one of the growing technologies used in cosmetic, pharmaceutical, and food industries. Their characteristic properties, like small droplet size with high interfacial area, transparent or semi-transparent appearance, low viscosity, and high kinetic stability, make them a perfect vehicle for fragrances, in the perfume industry. They could be a great alternative to water-based perfumes, without alcohol, and solve problems related to the oxidation and low bioavailability of fragrances with other non-alcoholic vehicles of perfumes like pomades or gels. The aim of our study was to develop stable Oil-in-Water (O/W) nanoemulsions that are compatible with selected fragrance compositions, without ethanol, polyols, and ionic surfactants, and to study their physicochemical, microbiological, and dermatological properties. The nano-perfume systems were obtained with a low-energy (Phase Inversion Composition; PIC) and with a high-energy (ultrasound, US) method, taking into account the possibility of moving from the laboratory scale to an industrial scale. The optimized nano-perfume formulations, prepared with different methods, yielded the same physicochemical properties (stability, medium droplet size of the inner phase, polydispersity, viscosity, surface tension, pH, density). Stable systems were obtained with a fragrance composition concentration within 6–15% range. These formulations had a low viscosity and a pH suitable for the skin. Moreover, the obtained results confirmed the protective role of nanoemulsions. The peroxide number measurement (POV) showed that the tested fragrance compositions had a high chemical stability. The results of the microbiological tests confirmed that the obtained products were free of microbiological contamination and were appropriately preserved. The dermatological test results confirmed the safety of the developed preparations.

Alcohol-based perfumes, e.g., eau de parfum, eau de toilette, eau de cologne or au fraiche, are the most common type of fragrance products available on the market. There are also alcohol-free fragrance products, mainly in the form of solid or oil perfume. From the consumers’ point of view, such perfumery products are of interest; therefore, looking for new solutions is still interesting. Nanoemulsions are liquid, kinetically stable colloidal dispersions, consisting of an aqueous phase, an oil phase and a surfactant, with or without a co-surfactant. They are transparent, not greasy, easy to spray and spread. Additionally, they show capacity to protect fragrances from oxidation. The development of a water-based perfumes in the form of stable nanoemulsions containing fragrance compositions (in the range of 5–15%), stabilized by nonionic surfactants, allows to create safe products for a wider group of consumers, including children, adolescents and people with sensitive skin. In this article, an application of nanoemulsions as a potential form of perfumery products were described.

NLC (nanostructured lipid carriers), composed with substances of GRAS (generally recognized as safe) status, were obtained by using the hot high pressure homogenization technique (HPH). The influence of number of homogenization cycles and concentration of a surfactant (decyl glucoside) on NLC properties were studied. The systems stability was assessed by macroscopic observation, light backscattering and zeta potential measurements. NLC particle size was measured by means of dynamic light scattering (DLS). The kinetically stable formulations were loaded with forskolin and selected for in vitro drug permeation study (Franz cell method). The concentration of forskolin in the receptor solution (i.e. Ethanol/PBS mixture) was analyzed by high performance liquid chromatography (HPLC) with UV detection. The obtained results have shown that NLC formulations could be used as effective carriers for forskolin permeation through the skin.

Two O/W forskolin-loaded nano-emulsions (0.075% wt.) based on medium chain triglycerides (MCT) and stabilized by a nonionic surfactant (Polysorbate 80 or Polysorbate 40) were studied as forskolin delivery systems. The nano-emulsions were prepared by the PIC method. The mean droplet size of the nano-emulsions with Polysorbate 80 and Polysorbate 40 with oil/surfactant (O/S) ratios of 20/80 and 80% water concentration, measured by Dynamic Light Scattering (DLS), was of 118 nm and 111 nm, respectively. Stability of the formulations, as assessed by light backscattering for 24 h, showed that both nano-emulsions were stable at 25°C. Studies of forskolin in vitro skin permeation from the nano-emulsions and from a triglyceride solution were carried out at 32°C, using Franz-type diffusion cells. A mixture of PBS/ethanol (60/40 v/v) was used as a receptor solution. The highest flux and permeability coefficient was obtained for the system stabilized with Polysorbate 80 (6.91±0.75 µg · cm-2·h-1 and 9.21 · 10-3±1.00 · 10-3 cm · h-1, respectively) but no significant differences were observed with the flux and permeability coefficient value of forskolin dissolved in oil. The obtained results showed that the nano-emulsions developed in this study could be used as effective carriers for topical administration of forskolin.