Benzo[k,l]xanthene Lignan-Loaded Solid Lipid Nanoparticles for Topical Application: A Preliminary Study

Abstract

Skin is the first human barrier that is daily exposed to a broad spectrum of physical and chemical agents, which can increase reactive oxygen species (ROS) and lead to the formation of topical disorders. Antioxidant molecules, such as benzo[k,l]xanthene lignans (BXL), are ideal candidates to eliminate or minimize the effects of ROS. Herein, we aimed to formulate BXL-loaded solid lipid nanoparticles (SLN-BXL) to improve the bioavailability and interaction with the skin, and also to investigate the protective impact against intracellular ROS generation in HFF-1 in comparison with the drug-free situation. SLN-BXL were formulated using the PIT/ultrasonication method, and then were subjected to physicochemical characterizations, i.e., average size, zeta potential (ZP), polydispersity index (PDI), encapsulation efficiency (%EE), thermotropic behavior, and interaction with a biomembrane model. The results show a mean size around 200 nm, PDI of 0.2, and zeta potential of about −28 mV, with values almost unchanged over a period of three months, while the EE% is ≈70%. Moreover, SLN-BXL are able to deeply interact with the biomembrane model, and to achieve a double-action release in mildly hydrophobic matrices; the results of the in vitro experiments confirm that SLN-BXL are cell-safe and capable of attenuating the IL-2-induced high ROS levels. In conclusion, based on our findings, the formulation can be proposed as a candidate for a preventive remedy against skin disorders induced by increased levels of ROS.

Ethyl Protocatechuate Encapsulation in Solid Lipid Nanoparticles: Assessment of Pharmacotechnical Parameters and Preliminary In Vitro Evaluation for Colorectal Cancer Treatment

“…The methodology, previously developed [ 28 ] on the basis of Sephadex-LH20 column chromatography followed by HPLC identification and quantification method, was adapted for the determination of the entrapment efficiency (EE%) of PCAEE in SLN and SLN containing Tween 80 (SLN-T). The EE% was obtained indirectly (Equation 1) by quantification of free PCAEE eluted with ethanol from gel permeation chromatography.…”

“…Differential scanning calorimetry is a powerful technique to study the thermotropic behavior of SLN [ 28 , 37 ]. Calorimetric curves are shown in Figure 3 .…”

“…The formulations’ names and their composition are reported in Table 1 . The preparation of SLN is based on the phase inversion temperature–ultrasonication combined method, described elsewhere [ 28 ]. Briefly, 500 mg of PrecirolATO 888 (T m = 55 °C) and 200 mg of Gelucire 50/13 were transferred in a beaker and successively placed in a water bath onto a hotplate magnetic stirrer.…”

“…SLN-PCAEE and SLN-T-PCAEE formulations (0.4 mL) were loaded onto a column (1.0 × 10 cm) packed with Sephadex LH20 and eluted with 15 mL of water, 10 mL of EtOH, and finally 10 mL of acetone [ 28 ]. The fractions were analyzed by HPLC-UV equipped with a Luna C-18 column (Phenomenex; 250 mm × 4.60 mm, 5 µM), employing the following elution program made up of H 2 O+ 1%CH 2 O (solvent A) and CH 3 CN+ 1%CH 2 O: t0 = 0% B, t 10 = 50% B, t 15 = 100% B, t 25 = 0% B.…”

Development of Solid Lipid Nanoparticles as Dry Powder: Characterization and Formulation Considerations

“…The sensitivity was automatically chosen as the maximum possible by the calorimetric system. Aluminum crucibles of 40 µL for dried SLNs and 160 µL for nanoparticle suspensions were used [ 49 , 50 ].…”