Abstract
Excipient interaction has become essential knowledge for rational formulation design of nanoparticles. Nanostructured lipid carriers (NLCs) include at least three types of excipient, which enhance excipient interaction possibilities and relevance. The present article introduces an alternative approach for evaluating a great number of excipients with few samples, using NLC as a model delivery system. This approach is based on two sequential experiments using Hall-2 experimental design and analysis of excipient interactions in respect to their physicochemical properties by multilevel statistics. NLCs were prepared using a hot emulsification-ultrasonication method with lidocaine and nine excipients (solid lipids, oils and surfactants). The evaluated parameters were z-average size (DLS), dispersity (DLS), zeta potential (electrophoretic mobility) and entrapment efficiency (HPLC). Cetyl palmitate, beeswax, castor oil, capric/caprylic acid and polysorbate 80 all presented larger effects amongst the studied factors as well as a clear pattern of synergistic interactions. Following the verified trends, we produced an optimized NLC that exhibited all desirable physicochemical characteristics and a modified drug release profile. Our results demonstrate the methodology’s robustness, which can be applied to other nanoparticles and establish a cost-effective excipient evaluation.
Highlights
Excipient interaction has become essential knowledge for rational formulation design of nanoparticles
We study excipient interaction on physicochemical outcomes of Nanostructured lipid carriers (NLCs) loaded with lidocaine, but, since two-factor interactions are likely to appear in any significant formulation, this approach applies to any other excipient screenings, from the pharmaceutical to the cosmetics and food fields
According to the United States Pharmacopeia (USP) solubility definition, LD was very soluble in solid lipids, freely soluble in oils and slightly soluble in water and surfactants[17]
Summary
Excipient interaction has become essential knowledge for rational formulation design of nanoparticles. The present article introduces an alternative approach for evaluating a great number of excipients with few samples, using NLC as a model delivery system This approach is based on two sequential experiments using Hall-2 experimental design and analysis of excipient interactions in respect to their physicochemical properties by multilevel statistics. Nanostructured lipid carriers (NLCs) are the second generation of solid lipid nanoparticles (SLN), widely used as biodegradable and safe delivery systems for hydrophobic drugs and bioactive substances[1,2,3] They are submicron particles of a mixed solid-liquid lipid core coated with surfactants; the carried substance generally being located within the lipid core. In order to obtain reproducible and stable NLCs, they should present low particle size dispersity, high zeta potential in module and constant size range[4] To manipulate these properties, one could alter critical process parameters or formulation parameters. Due to the complex nature of NLCs, it is likely that excipients will interact with each other, making it impossible to separate this from the excipient’s individual behaviour using the techniques described
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