Selmi Mouna, Trabelsi Amine, Lautram Nolwenn, Dallerac David, Lefebvre Guillaume, Chekir Ghedira Leila, Roger Emilie
Laboratoire des substances naturelles bioactives et biotechnologie LR24ES14, Faculté de médecine dentaire, Université de Monastir, Tunisia.
Laboratoire de Pharmacognosie, Faculté de Pharmacie, Université de Monastir, Tunisia.
Pharm Dev Technol. 2025 Jan;30(1):69-78. doi: 10.1080/10837450.2024.2448616. Epub 2025 Jan 3.
This work explores two methods to encapsulate Thymoquinone (TQ) into lipid nanocapsules (LNCs) for oral administration. TQ was added during the phase inversion temperature method (TQ-LNCs-1) or to unload LNCs dispersion (TQ-LNCs-2). LNCs were evaluated for mean diameter, polydispersity index (PDI), ζ-potential, drug loading (DL), drop tensiometer, storage stability, stability in simulated gastrointestinal fluids (SGIF), and intestinal permeability across Caco-2 cells. TQ-LNCs-1 and TQ-LNCs-2 produced NPs (58.3 ± 3.7 nm and 61.5 ± 3.5 nm, respectively), with a DL of 8.7 ± 0.2 and 7.7 ± 0.6 mg/mL of suspension, respectively. For both, less than 14% of TQ was released in SGIF, and a minor increase in TQ intestinal permeability with LNCs compared to free TQ was observed. TQ-LNCs represented a promising formulation for oral delivery of TQ. Encapsulation of TQ by adding it at LNCs dispersion can be extended for further drugs.
本研究探索了两种将百里醌（TQ）包裹于脂质纳米囊（LNCs）中用于口服给药的方法。在相转变温度法过程中添加TQ（TQ-LNCs-1）或向LNCs分散液中加入TQ（TQ-LNCs-2）。对LNCs的平均直径、多分散指数（PDI）、ζ电位、载药量（DL）、滴体积张力计、储存稳定性、在模拟胃肠液（SGIF）中的稳定性以及跨Caco-2细胞的肠道通透性进行了评估。TQ-LNCs-1和TQ-LNCs-2分别产生了纳米颗粒（分别为58.3±3.7nm和61.5±3.5nm），悬浮液的载药量分别为8.7±0.2和7.7±0.6mg/mL。对于两者而言，在SGIF中释放的TQ均不到14%，并且观察到与游离TQ相比，LNCs使TQ的肠道通透性略有增加。TQ-LNCs是一种很有前景的TQ口服给药制剂。通过在LNCs分散液中添加TQ来包裹TQ的方法可扩展用于其他药物。
