Astrocaryum vulgare M. oil-composed nanostructured lipid carriers for topical administration: optimization by 22 factorial design and development of a semi-solid formulation.
Maria Eugênia B Rocha, Raquel da Ana, Faezeh Fathi, M Beatriz P P Oliveira, Leticia Kakuda, Wanderley P Oliveira, Eliana B Souto
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引用次数: 0
Abstract
The selection of lipids and their ratios play a critical role in determining drug loading capacity and the structural properties of nanostructured lipid carriers (NLCs), directly impacting their stability. Among liquid lipids, vegetable oils have been explored both as active pharmaceutical ingredients (APIs) and as excipients in NLCs intended for topical use. The pulp oil of Tucumã, derived from Brazilian biodiversity, is known for its anti-inflammatory and antioxidant properties, attributed to its high content of flavonoids and carotenoids. This study focused on evaluating the compatibility of Tucumã oil with various solid lipids (SLs) commonly used in NLC production, developing an optimized NLC formulation containing this oil, and monitoring its stability over a 28-days' period. Lipid screening was performed to assess SL compatibility, followed by pilot formulations to determine the type and concentration range of SL and surfactant for the experimental design. A 22-factorial design was applied to understand and identify the significant effects and interactions of lipid and surfactant concentrations on Tucumã oil-loaded NLC, and the stability of the optimized formulation was monitored by determining the mean particle size (z-Ave), polydispersity index (PI), zeta potential (ZP), and recrystallization index (RI%) over 28 days. Compritol® was identified as the most suitable SL, resulting in round shaped NLC with z-Ave of 309nm, PI of 0.23 and high ZP (-25.5mV). The RI% was shown to be influenced by storage time and temperature. The optimal formulation contained 8% total lipid phase (at a 20:80 of oil to SL) and 3% of Tween® 80 as surfactant, showing stability at 5ºC, 25ºC and 40ºC. The experimental design revealed a positive effect of surfactant concentration on z-Ave and PI, with no significant impact on ZP. Over time, NLCs exhibited a gradual color loss (becoming whiter), with no other signs of instability. These findings support the potential use of Tucumã oil for producing stable NLC suitable for topical delivery.
期刊介绍：
Chemistry and Physics of Lipids publishes research papers and review articles on chemical and physical aspects of lipids with primary emphasis on the relationship of these properties to biological functions and to biomedical applications.
Accordingly, the journal covers: advances in synthetic and analytical lipid methodology; mass-spectrometry of lipids; chemical and physical characterisation of isolated structures; thermodynamics, phase behaviour, topology and dynamics of lipid assemblies; physicochemical studies into lipid-lipid and lipid-protein interactions in lipoproteins and in natural and model membranes; movement of lipids within, across and between membranes; intracellular lipid transfer; structure-function relationships and the nature of lipid-derived second messengers; chemical, physical and functional alterations of lipids induced by free radicals; enzymatic and non-enzymatic mechanisms of lipid peroxidation in cells, tissues, biofluids; oxidative lipidomics; and the role of lipids in the regulation of membrane-dependent biological processes.
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