Effects of solid lipid ratio in curcumin loaded emulsions on its gastrointestinal fate: Colloidal stability and mucus absorption efficiency

Abstract

Emulsions offer a promising approach for enhancing the bioavailability of lipophilic active compounds when administered orally. Nonetheless, the impact of lipid matrix composition on the efficacy of penetration and bioavailability remains uncertain. This research investigated the effects of solid lipid ratio in emulsions on colloidal stability, mucus permeability, and bioavailability in vivo. To assess colloidal stability in the gastrointestinal tract (GIT), Turbiscan was employed. The results indicated that an elevated solid lipid ratio improved intestinal stability through the formation of aggregations that resisted pancreatic absorption, as confirmed by TEM. The absorption in various intestinal sections was tested using the Ussing Chamber model. Notably, emulsion with 0 % solid lipid (G0M10) exhibited the highest cumulative permeation across the duodenum (221.2 ± 21.19 ng), jejunum (713.1 ± 20.93 ng), and ileum (1056.3 ± 392.06 ng) due to its higher in vitro release rate (>60 %) and smaller particle size. The cumulative permeation decreased with increasing solid lipid ratio. CLSM revealed that emulsions with a solid lipid ratio exceeding 50 % exhibited poor mucus permeability within 15 min due to aggregation during the passage in the GIT. However, over an extended penetration time (30 min), higher permeability was observed, reaching approximately 30 μm. In vitro release studies indicated that a higher solid lipid ratio resulted in a reduced release rate of curcumin (<60 %) compared to G0M10 (66.9 ± 3.58 %). Correlation analysis unveiled a positive link between bioavailability and in vitro release rate, while a negative correlation emerged with the solid lipid ratio. This work underscores the significance of solid lipid ratios in emulsions for optimizing bioavailability through their influence on stability, permeability, and release of lipophilic compounds in the GIT.