Engineered nanostructured lipid carrier encapsulating thymoquinone and resveratrol to prevent Bisphenol S induced cytotoxicity.
TL;DR
Proof of concept that TQRV-NLCs markedly enhance efficacy, confer superior cytoprotection, and offer preventive effects, presenting a promising strategy for renal protection against BPS is provided.
Abstract
Nanostructured lipid carriers (NLCs) are diverse colloidal systems that enhance the solubility, stability, and bioavailability of bioactive compounds. Herein, we developed a co-loaded NLC encapsulating thymoquinone (TQ) and resveratrol (RV) to enhance prevention against globally emerging endocrine disruptor bisphenol S (BPS) induced cytotoxicity in NRK-52E cells. The formulation components were rationally optimised, achieving high encapsulation efficiencies for TQ (99.42% ± 0.08) and RV (98.60% ± 0.12), a particle size of 123.66 ± 6.32 nm, and a polydispersity index of 0.37 ± 0.04, indicating stable, homogeneous, quasi-spherical particles as observed in TEM. Interfacial encapsulation and reduced crystallinity observed by FTIR and XRD analyses, respectively, supported the formation of an imperfect core-shell structure. The drug-release profile indicated a diffusion-dominated, matrix-relaxation-assisted transport mechanism. In vitro assays demonstrated a strong cytoprotective effect of TQRV-NLCs at 0.01 μg/mL, comparable to 1 μg/mL free drugs, indicating a significant improvement in therapeutic efficacy. TQRV-NLCs markedly reduced BPS-induced oxidative stress, mitochondrial depolarisation, loss of cell migration, and loss of membrane integrity, while restoring membrane integrity, normalising cell cycle distribution, and preserving nuclear morphology in NRK-52E cells. In summary, this study provides proof of concept that TQRV-NLCs markedly enhance efficacy, confer superior cytoprotection, and offer preventive effects, presenting a promising strategy for renal protection against BPS.