Natural-Origin Betaine Surfactants as Promising Components for the Stabilization of Lipid Carriers.

In the present work, we demonstrate studies involving the influence of the formulation composition on the physicochemical properties of nanocarriers: solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). Novel lipid-origin platforms were prepared using two "green" betaine-based surfactants, cocamidopropyl betaine (ROKAmina K30) and coco betaine (ROKAmina K30B), in combination with three different solid lipids, cetyl palmitate (CRODAMOL CP), trimyristin (Dynasan 114), and tristearin (Dynasan 118). Extensive optimization studies included the selection of the most appropriate lipid and surfactant concentration for effective SLN and NLC stabilization. The control parameters involving the hydrodynamic diameters of the obtained nanocarriers along with the size distribution (polydispersity index) were determined by dynamic light scattering (DLS), while shape and morphology were evaluated by atomic force microscopy (AFM) and transmission electron microscopy (TEM). Electrophoretic light scattering (ELS) and turbidimetric method (backscattering profiles) were used to assess colloidal stability. The studied results revealed that both betaine-stabilized SLN and NLC formulations containing CRODAMOL CP as lipid matrix are the most monodisperse and colloidally stable regardless of the other components and their concentrations used, indicating them as the most promising candidates for drug delivery nanosystems with a diverse range of potential uses.

Self-assembled bilosomes with stimuli-responsive properties as bioinspired dual-tunable nanoplatform for pH/temperature-triggered release of hybrid cargo.

The rapid development of colloid chemistry has raised the possibility of using nanocarriers for the targeted delivery and the controlled drug release at predictable locations to reduce side effects and enhance therapeutic efficacy. In the present work, we focused on the influence of temperature and pH upon in vitro controlled phytochemical/dye-release from a modified bilosome. Drug molecules can affect the properties of nanocarriers, so the effect of encapsulated bioactive compounds on nanoparticle structure has been investigated. The self-assembly process of bioinspired components (i.e., phospholipids, bile salts, and cholesterol), and biocompatible polymeric triblock materials, made it possible to receive structures with a size below 100 nm, demonstrated good capacity for active cargo encapsulation. Differential scanning calorimetry studies showed the possibility of the payloads' interaction with the bilosomes structure. A highly lipophilic compound, such as curcumin, can weaken hydrophobic interactions between the acyl chains of phospholipids, leading to a more flexible membrane. The in vitro release profiles have proved that both solubilities of the therapeutic substances and various environmental conditions affect the release rate of the hybrid cargo. Overall, the obtained double-loaded bilosomes represent a promising bioinspired nanoplatform for oral, intravenous, and topical drug delivery in future biomedical applications.

Novel Surface-Modified Bilosomes as Functional and Biocompatible Nanocarriers of Hybrid Compounds.

In the present contribution, we demonstrate a new approach for functionalization of colloidal nanomaterial consisting of phosphatidylcholine/cholesterol-based vesicular systems modified by FDA-approved biocompatible components, i.e., sodium cholate hydrate acting as a biosurfactant and Pluronic P123-a symmetric triblock copolymer comprising poly(ethylene oxide) (PEO) and poly(propylene oxide) (PPO) blocks Eight novel bilosome formulations were prepared using the thin-film hydration method followed by sonication and extrusion in combination with homogenization technique. The optimization studies involving the influence of the preparation technique on the nanocarrier size (dynamic light scattering), charge (electrophoretic light scattering), morphology (transmission electron microscopy) and kinetic stability (backscattering profiles) revealed the most promising candidate for the co-loading of model active compounds of various solubility; namely, hydrophilic methylene blue and hydrophobic curcumin. The studies of the hybrid cargo encapsulation efficiency (UV-Vis spectroscopy) exhibited significant potential of the formulated bilosomes in further biomedical and pharmaceutical applications, including drug delivery, anticancer treatment or diagnostics.