Biocompatibility and Antimicrobial Activity of Nanostructured Lipid Carriers for Topical Applications Are Affected by Type of Oils Used in Their Composition

Pharmaceutics. 2021 Nov 17;13(11):1950. doi: 10.3390/pharmaceutics13111950.

Abstract

Nanostructured lipid carriers (NLCs) have gained significant attention as tools for the dermal delivery of therapeutics due to their stability, biocompatibility, and ability to improve drug bioavailability. The use of natural plant oils (NPO) in NLC formulations has numerous benefits for the skin due to their therapeutic potential. This work shows the effect of NLC composition on bioavailability in epidermal cells and antimicrobial activity against Staphylococcus aureus. Sixteen systems containing fixed (sunflower, olive, corn, peanut, coconut, castor, and sweet almond) and essential (eucalyptus) oils, with different solid lipid (SL): liquid lipid (LL) ratios, were engineered. The structural properties, bioavailability, and antimicrobial action of the particles was studied. The choice of NPO influenced the physicochemical stability by changing the diameter of NLC formulations (between 160 nm and 185 nm) and Z-potential (between -46 mV and -61 mV). All of the systems were characterized by concentration-dependent cytocompatibility with human epidermal keratinocytes (HaCaT) and human dermal fibroblasts (HDFn). The SL:LL ratio in some NLC systems impacted cell cytotoxicity differently. Antimicrobial properties were observed in all 16 systems; however, the type of oil and SL:LL ratio affected the activity of the formulations. Two NLC-NPO systems were found to be non-cytotoxic to human cells lines at concentrations that completely inhibited bacterial growth. These results present a strong argument that the use of natural oils in NLC formulations presents a promising tool for the treatment of skin infections.

Keywords: NLCs; S. aureus; antimicrobial activity; cytotoxicity; plant oils.