Synergistic stabilization of emulsion gel by nanoparticles and surfactant enables 3D printing of lipid-rich solid oral dosage forms

Pharmaceutical formulation of oral dosage forms is continuously challenged by the low solubility of new drug candidates. Pickering emulsions, emulsions stabilized with solid particles, are a promising alternative to surfactants for developing long-term stable emulsions that can be tailored for controlled release of lipophilic drugs. In this work, a non-emulsifying lipid-based formulation (LBF) loaded with fenofibrate was formulated into an oil-in-water (O/W) emulsion synergistically stabilized by stearic acid and silica (SiO₂) nanoparticles. The emulsion had a droplet size of 341 nm with SiO₂ particles partially covering the oil-water interface.

In vitro lipid digestion was faster for the emulsion compared to the corresponding LBF due to the larger total surface area available for digestion. Cellulose biopolymers were added to the emulsion to produce a gel for semi-solid extrusion (SSE) 3D printing into tablets. The emulsion gel showed suitable rheological attributes for SSE, with a trend of higher viscosity, yield stress, and storage modulus (Ǵ), compared to a conventional self-emulsifying lipid-based emulsion gel. The developed emulsion gel allows for a non-emulsifying LBF to be transformed into solid dosage forms for rapid lipid digestion and drug release of a poorly water-soluble drug in the small intestine.

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Materials

Maisine CC (mixed long-chain glycerides) was kindly provided by Azelis (Herlev, Denmark). Methocel A4M (methylcellulose), Methocel E4M (hydroxypropyl methylcellulose), and Ac-Di-Sol SD-711 (croscarmellose sodium) were donated by IFF Nutrition & Bioscience. Fasted state simulated intestinal fluid (FaSSIF) powder was purchased from biorelevant.com (Croydon, UK). Analytical solvents were purchased from VWR International (Spånga, Sweden). Soybean oil (long-chain triglycerides), Tween 85, fenofibrate (≥ 99%), Ludox TM-50 colloidal SiO2 (22 nm primary particle size specified by manufacturer, 50% w/w suspension in water, negatively charged particles stabilized with sodium counter ions), Nile red, stearic acid (95%), and porcine pancreatin extract (8 × USP specifications activity) were obtained from Merck (Darmstadt, Germany).

Jenny Johannesson, Malhar Manik Pathare, Mathias Johansson, Christel A.S. Bergström, Alexandra Teleki, Synergistic stabilization of emulsion gel by nanoparticles and surfactant enables 3D printing of lipid-rich solid oral dosage forms, Journal of Colloid and Interface Science, 2023, ISSN 0021-9797, https://doi.org/10.1016/j.jcis.2023.07.055.

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