Formulation design, production and characterisation of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for the encapsulation of a model hydrophobic active

Lipid nanoparticles have been widely investigated for their use as either carriers for poorly water soluble actives or as (Pickering) emulsion stabilisers. Recent studies have suggested that the fabrication of lipid nanostructures that can display both these performances concurrently, can enable the development of liquid formulations for multi-active encapsulation and release. Understanding the effects of different formulation variables on the microstructural attributes that underline both these functionalities is crucial in developing such lipid nanostructures.

Highlights

Lipid materials were chosen based on theoretical and experimental lipid screening.

SLNs and NLCs with high curcumin loading were produced using the selected lipids.

Nano-sized lipid particles fabricated by tuning the processing parameters.

Lipid matrix component compatibility affects thermal properties as shown by DSC.

Formation of distinct lipid structures in liquid lipid concentration-dependent manner.

In this study, two types of lipid-based nanoparticles, solid lipid nanoparticles and nanostructured lipid carriers, were fabricated using varying formulation parameters, namely type of solid lipid, concentration of liquid lipid and type/concentration of surface active species. The impact of these formulation parameters on the size, thermal properties, encapsulation efficiency, loading capacity and long-term storage stability of the developed lipid systems, was studied. Preliminary lipid screening and processing conditions studies, focused on creating a suitable lipid host matrix of appropriate dimensions that could enable the high loading of a model hydrophobic active (curcumin). Informed by this, selected lipid nanostructures were then produced.

These were characterised by encapsulation efficiency and loading capacity values as high as 99% and 5%, respectively, and particle dimensions within the desirable size range (100-200 nm) required to enable Pickering functionality. Compatibility between the lipid matrix components, and liquid lipid/active addition were shown to greatly influence the polymorphism/crystallinity of the fabricated particles, with the latter demonstrating a liquid lipid concentration-dependent behaviour. Successful long-term storage stability of up to 28 weeks was confirmed for certain formulations.

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Materials: Glyceryl behenate (Compritol® 888 ATO), glyceryl palmitostearate (Precirol® ATO 5), linoleoyl polyoxyl-6-glycerides (Labrafil® M 2125 CS), propylene glycol dicaprolate/dicaprate (Labrafac™ PG), cetyl palmitate and lauroyl polyoxyl-32 glycerides (Gelucire® 44/14) were kindly provided from Gattefossé (Saint-Priest, France). Glyceryl monostearate (Imwitor® 960K), glyceryl citrate/lactate/linoleate/oleate (Imwitor® 375) and medium chain triglycerides (MCTs) (Miglyol® 812), microcrystalline glyceryl tristearate (Dynasan® 118) were a kind gift from IOI Oleo (IOI Oleochemicals GmbH, Germany). Polyoxyethylene sorbitan monooleate (Tween® 80), Poloxamer 188 (Pluronic® F-68), poly(vinyl alcohol) (PVA, MW 89,000-98,000), castor oil and curcumin (≥65%, HPLC) were purchased from Sigma-Aldrich (Sigma-Aldrich, UK). All chemicals were used without further purification. Double distilled water from Milli-Q systems (Millipore, Watford, UK) was used for all experiments.

Article information: Georgia I. Sakellari, Ioanna Zafeiri, Hannah Batchelor, Fotis Spyropoulos, Formulation design, production and characterisation of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for the encapsulation of a model hydrophobic active, Food Hydrocolloids for Health, 2021. https://doi.org/10.1016/j.fhfh.2021.100024.