Search Results (6)

The present study aimed to formulate and characterize a hesperetin formulation to achieve adequate deposition and retention of hesperetin in the epidermis as a target for some cosmetic/dermatological actions. To derive the final emulgel, various formulations incorporating different proportions of Polysorbate 80 and hyaluronic acid underwent testing through a Box–Behnken experimental design. Nine formulations were created until the targeted emulgel properties were achieved. This systematic approach, following the principles of a design of experiment (DoE) methodology, adheres to a quality-by-design (QbD) paradigm, ensuring a robust and purposeful formulation and highlighting the commitment to a quality-driven design approach. The emulsions were developed using the phase inversion method, optimizing the emulgel with the incorporation of hyaluronic acid. Physically stable optimized emulgels were evaluated for their globule size, surface charge, viscosity, pH, electrical conductivity, and hesperetin content. These assays, along with the temperature swing test, were used to select the optimal formulation. It was characterized by a droplet size, d[4,3], of 4.02 μm, a Z-potential of −27.8 mV, an O/W sign, a pH of 5.2, and a creamy texture and proved to be stable for at least 2 months at room temperature. Additionally, in vitro release kinetics from the selected emulgel exhibited a sustained release profile of hesperetin. Skin assays revealed adequate retention of hesperetin in the human epidermis with minimum permeation. Altogether, these results corroborate the promising future of the proposed emulgel in cosmetic or dermatological use on healthy or diseased skin. Full article

Emulgels are biphasic emulsified systems in which the continuous phase is structured with a specific gelling agent. In this work, a rheological and microscopic investigation of O/W emulgels prepared by structuring the aqueous (continuous) phase with citrus fiber was carried out with the aim of designing their macroscopic properties for food uses and predicting their characteristics with a rheological model. According to previous investigations, fiber suspensions behave as “particle gels” and, consequently, the derived emulgels’ properties are strongly dependent on the fiber concentration and on process conditions adopted to produce them. Therefore, a rotor–stator system was used to prepare emulgels with increasing fiber content and with different levels of energy and power used for mixing delivered to the materials. An investigation of particle gels was then carried out, fixing the operating process conditions according to emulgel results. Furthermore, the effect of the dispersed (oil) phase volume fraction was varied and a modified semi-empirical Palierne model was proposed with the aim of optimizing a correlation between rheological properties and formulation parameters, fixing the process conditions. Full article

W/O/W emulsions can be used to encapsulate both hydrophobic and hydrophilic bioactive as nutritional products. However, studies on protein stabilized gel-like W/O/W emulsions have rarely been reported, compared to the liquid state multiple emulsions. The purpose of this study was to investigate the effect of different oil–water ratios on the stability of W/O/W emulgels fabricated with salt-soluble proteins (SSPs) of Sipunculus nudus. The physical stability, structural characteristics, rheological properties, and encapsulation stability of vitamin C and β-carotene of double emulgels were investigated. The addition of W/O primary emulsion was determined to be 10% after the characterization of the morphology of double emulsion. The results of microstructure and rheological properties showed that the stability of W/O/W emulgels increased with the increasing concentration of SSPs. Additionally, the encapsulation efficiency of vitamin C and β-carotene were more than 87%, and 99%, respectively, and still could maintain around 50% retention of the antioxidant capacity after storage for 28 days at 4 °C. The aforementioned findings demonstrate that stable W/O/W emulgels are a viable option for active ingredients with an improvement in shelf stability and protection of functional activity. Full article

Dry (D.E.) and liquid (L.E.) extracts were prepared from flaxseeds and their application in health field was evaluated. The chemical analysis showed that D.E. is rich in the lignan secoisolariciresinol diglucoside and L.E. in unsaturated triglycerides containing linolenic acid. Mainly, D.E. showed reducing (15.73 μmol Fe²⁺/g) and radical scavenging capacities (5.25 mg TE/g) and ability to down-regulate the expression of the pro-inflammatory cytokines NO (IC₅₀ = 0.136 ± 0.009 mg/mL) and IL-6 (IC₅₀ = 0.308 ± 0.103 mg/mL), suggesting its use in wound treatment. D.E. and L.E. were active against S. pyogenes and D.E. also against S. aureus. The two extracts were combined in a novel O/W emulgel in which the water phase was viscosized using a low molecular weight and highly deacetylated chitosan (1% wt./v). The presence of this polymer in the emulgel decreased the MIC values of the extracts. In fact, MIC shifted from 0.59 mg/mL to 0.052 mg/mL for D.E. and from 0.22 mg/mL to 0.036 mg/mL for L.E., concentrations safe both for keratinocytes and macrophages. Moreover, the emulgel demonstrated to inhibit S. aureus, P. aeruginosa, S. pyogenes, E. coli, and K. pneumoniae growth (inhibition halos 24–36 mm), strains often responsible for diabetic foot ulcer infection. Full article

The oral administration of dapsone (DAP) for the treatment of cutaneous leishmaniasis (CL) is effective, although serious hematological side effects limit its use. In this study, we evaluated this drug for the topical treatment of CL. As efficacy depends on potency and skin penetration, we first determined its antileishmanial activity (IC₅₀ = 100 μM) and selectivity index in vitro against Leishmania major-infected macrophages. In order to evaluate the skin penetration ex vivo, we compared an O/W cream containing DAP that had been micronized with a pluronic lecithin emulgel, in which the drug was solubilized with diethylene glycol monoethyl ether. For both formulations we obtained similar low flux values that increased when the stratum corneum and the epidermis were removed. In vivo efficacy studies performed on L. major-infected BALB/c mice revealed that treatment not only failed to cure the lesions but made their evolution and appearance worse. High plasma drug levels were detected and were concomitant with anemia and iron accumulation in the spleen. This side effect was correlated with a reduction of parasite burden in this organ. Our results evidenced that DAP in these formulations does not have an adequate safety index for use in the topical therapy of CL. Full article

The choice of formulation is often of crucial importance in order to obtain a pharmaceutical product for the administration of poorly soluble drugs. Recently, a new water-soluble microparticulate powder form (MTE-mp) for the oral administration of a high functionality/low solubility silymarin rich milk thistle extract (MTE) has been developed. Findings showed that extract-loaded microparticles by spray-drying were produced with high and reproducible yields and encapsulation efficiency. The in vitro dissolution and permeation rates of silymarin were dramatically improved with respect to the raw material, and also enhanced the silymarin anti-inflammatory abilities. Given these successful results, the new MTE-mp delivery system has been proposed as an active ingredient for dermal applications. The aim of this research was the design and development of two topical formulations, hydrogel and emulgel (O/W emulsion), containing the MTE-mp delivery system or MTE raw extract. All the formulations were compared to each other in terms of handling and incorporation amount of the active ingredient during the productive process. Moreover, the addition to the emulgel of lecithin (L) as enhancer of permeation was tested. The MTE-mp ingredient that resulted was stable and more-easily incorporated both in hydrogel and emulgel than raw MTE extract, obtaining the best permeation profile for MTE-mp from emulgel with the addition of L. The obtained results confirm that the MTE-mp system could be used as a stable, water-soluble, and easy-handling functional ingredient, giving the opportunity to develop new strategies for MTE delivery in health products. Full article