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

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          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.

          Abstract

          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. 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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          Most cited references84

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          Bioavailability of curcumin: problems and promises.

          Curcumin, a polyphenolic compound derived from dietary spice turmeric, possesses diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Phase I clinical trials have shown that curcumin is safe even at high doses (12 g/day) in humans but exhibit poor bioavailability. Major reasons contributing to the low plasma and tissue levels of curcumin appear to be due to poor absorption, rapid metabolism, and rapid systemic elimination. To improve the bioavailability of curcumin, numerous approaches have been undertaken. These approaches involve, first, the use of adjuvant like piperine that interferes with glucuronidation; second, the use of liposomal curcumin; third, curcumin nanoparticles; fourth, the use of curcumin phospholipid complex; and fifth, the use of structural analogues of curcumin (e.g., EF-24). The latter has been reported to have a rapid absorption with a peak plasma half-life. Despite the lower bioavailability, therapeutic efficacy of curcumin against various human diseases, including cancer, cardiovascular diseases, diabetes, arthritis, neurological diseases and Crohn's disease, has been documented. Enhanced bioavailability of curcumin in the near future is likely to bring this promising natural product to the forefront of therapeutic agents for treatment of human disease.
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            Hansen Solubility Parameters

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              Nanostructured lipid matrices for improved microencapsulation of drugs.

              At the beginning of the nineties solid lipid nanoparticles (SLN) have been introduced as a novel nanoparticulate delivery system produced from solid lipids. Potential problems associated with SLN such as limited drug loading capacity, adjustment of drug release profile and potential drug expulsion during storage are avoided or minimised by the new generation, the nanostructured lipid carriers (NLC). NLC are produced by mixing solid lipids with spatially incompatible lipids leading to special structures of the lipid matrix, i.e. three types of NLC: (I) the imperfect structured type, (II) the structureless type and (III) the multiple type. A special preparation process-applicable to NLC but also SLN-allows the production of highly concentrated particle dispersions (>30-95%). Potential applications as drug delivery system are described.
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                Author and article information

                Contributors
                Journal
                Food Hydrocoll Health
                Food Hydrocoll Health
                Food Hydrocolloids for Health
                Elsevier B.V
                2667-0259
                1 January 2021
                2021
                : 1
                : None
                Affiliations
                [a ]School of Chemical Engineering, University of Birmingham, Edgbaston, Birmingham, B15 2TT, UK
                [b ]Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral Street, Glasgow, G4 0RE, UK
                Author notes
                [* ]Corresponding author. gis823@ 123456bham.ac.uk
                Article
                S2667-0259(21)00016-9 100024
                10.1016/j.fhfh.2021.100024
                8721956
                35028634
                ff1de13d-b2b0-4218-97f7-a55a8f7f3054
                © 2021 The Author(s)

                This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

                History
                : 31 May 2021
                : 5 August 2021
                : 20 August 2021
                Categories
                Article

                solid lipid nanoparticles,nanostructured lipid carriers,hydrophobic active,crystallinity,pickering functionality,hansen solubility parameter

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