Abstract
Anthocyanins are potential bioactive compounds with less bioavailability due to instability in physicochemical and physiological harsh environments. This study synthesized a “nanolipo-fibersomes (NLFS)” using Lipoid® S75 and Nutriose® FB 06 (dextrinization of wheat starch) through a self-assembly technique with probe sonication. We aimed to encapsulate delphinidin-3-O-sambubioside (D3S) successfully and evaluate physicochemical and controlled release properties with improved antioxidant activity on palmitic acid (PA)-induced colonic cells (Caco-2 cells). D3S-loaded nanolipo-fibersomes (D3S-NLFS) were nanosized (<150 nm), spherical shaped, and homogenously dispersed in solution with promising encapsulation efficiency (~ 89.31 to 97.31 %). Particles formation was further verified by FTIR. NLFS were well-stable in thermal, storage, and gastrointestinal mimic environments. NLFS exhibited better-controlled release and mucoadhesive properties compared to nanoliposomes (NL). The NLFS showed better cellular uptake than NL, which was correlated to higher mucoadhesive properties. Furthermore, D3S-NLFS exhibited promising protective effects against PA-induced cytotoxicity, O2•− radicals generation, mitochondrial dysfunctions, and GSH depletion, while the free D3S was ineffective. Among D3S-loaded nanoparticles, D3S-NLFS 3 was the most efficient nanocarrier followed by D3S-NLFS 2, D3S-NLFS 1, and D3S-NL, respectively. The above data suggest that nanolipo-fibersomes can be considered as promising nanovesicles for improving colonic delivery of hydrophilic compounds with controlled release properties and greater antioxidant activity.
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