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

Dragana P C De Barros,Rafaela Santos,Marta Alves,Patricia Reed,Abel Oliva

doi:10.3390/pharmaceutics13111950

Dragana P C De Barros, Rafaela Santos + Show 3 more

Open Access

https://doi.org/10.3390/pharmaceutics13111950

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Journal: Pharmaceutics	Publication Date: Nov 17, 2021
Citations: 10	License type: CC BY 4.0

Affiliation: Instituto de Biologia Experimental Tecnológica

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.

Highlights

The applications of nanoparticles (NPs) and other colloidal drug-delivery systems in cutaneous drug delivery modify the drug distribution and release profile [1]
To assess the role of Nanostructured lipid carriers (NLCs) composition in terms of cytotoxicity, we investigated cell viability in HaCaT and HDF cells incubated with eight different blank NLC formulations differing in their liquid lipid composition
It was shown that the systems with the solid lipid (SL):liquid lipid (LL) = 60:40 and SL:LL = 40:60 lipid ratios had the best characteristics regarding the stability of the lipid carriers

Summary

Introduction

The applications of nanoparticles (NPs) and other colloidal drug-delivery systems in cutaneous drug delivery modify the drug distribution and release profile [1]. The dermal absorption of nanoparticles assumes direct contact with the nanostructured material, ensuring close contact with the stratum corneum and increasing the amount of drug absorbed by the skin. Nanostructured lipid carriers (NLCs) have been shown to improve controlled drug release, lower toxicity, and increase the bioavailability of drugs, such as antibiotics [2,3,4,5,6]. The selection and good understanding of physicochemical properties of liquid lipids are some of the most critical factors affecting performance and stability of NLCs [9]. Yang et al reported that NLC suspension stability was strongly affected by the type and amount of the carrier oil [10]

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