Characterization of entrapment behavior of polyphenols in nanostructured lipid carriers and its effect on their antioxidative activity.

Polyphenols are widely used as antioxidant agents to protect human health. Resveratrol, kaempferol, and quercetin have been reported to have potent antioxidant activity; however, these compounds have many problems related to their practical application, such as instability and insolubility. Thus, a nanostructured lipid carrier (NLC) was utilized as a drug delivery system (DDS) to overcome these limitations. This study investigated the particle stability, drug loading performance, and antioxidant activity of polyphenols-incorporated NLCs. The particle size and distribution were suitable for DDS applications, and all the samples demonstrated good stability after 2 months of storage. Based on Raman spectroscopy analysis, polyphenols were successfully encapsulated in NLCs. Quantitative high-performance liquid chromatography analysis indicated that NLCs could load resveratrol more than kaempferol and quercetin. In addition, NLCs have successfully improved all the antioxidant activity per unit concentration of polyphenol (specific antioxidant activity) compared to the free polyphenols. Quercetin-incorporated NLCs showed the highest specific antioxidant activity. This result is the opposite of entrapment efficiency and actual antioxidant activity, most likely influenced by the location of entrapped polyphenol molecules. As it was performed, NLCs are highly recommended to be applied as an antioxidant delivery system.

Systematic Characterization of Nanostructured Lipid Carriers from Cetyl Palmitate/Caprylic Triglyceride/Tween 80 Mixtures in an Aqueous Environment.

Nanostructured lipid carriers (NLCs) are gaining attention as the new generation of lipid vehicles. These carriers consist of saturated lipids with small drops of liquid oil dispersed into the inner lipid matrix and are stabilized by a surfactant. Conventionally, NLC-based drug delivery systems have been widely studied, and many researchers are looking into the composition of NLC properties to improve the performance of NLCs. The membrane fluidity and polarity of self-assembling lipids are also essential properties that must be affected by membrane compositions; however, such fundamental characteristics have not been studied yet. In this study, NLCs were prepared from cetyl palmitate (CP), caprylic triglyceride (CaTG), and Tween 80 (T80). Structural properties, such as particle size and ζ-potential of the CP/CaTG/T80 ternary mixtures, were investigated. Then, the systematic characterization of self-assembly properties using fluorescence-based analysis was applied for the first time to the NLC system. As a final step, the ternary diagram was developed based on the self-assembly properties to summarize the possible structures formed at different compositions. The results showed four states: micelle-like, oil-in-water (O/W) emulsion-like, solid lipid nanoparticle-like, and intermediate (solid-liquid coexistence). For the purpose of making the lipid matrix more liquified, the heterogeneous state and the disordered state of the O/W emulsion-like structure might fulfill the criteria of NLCs. Finally, the ternary diagram provides new information about the assembly state of NLC constituents that could become an important reference for developing high-performance NLCs.