
Pharmaceutics, Journal Year: 2025, Volume and Issue: 17(5), P. 540 - 540
Published: April 22, 2025
Background: Celastrol (Cela), a phytochemical extracted from Tripterygium wilfordii, has been extensively investigated for its potential anti-inflammatory, anti-psoriatic, antioxidant, neuroprotective, and antineoplastic properties. However, clinical translation is limited due to poor bioavailability, low solubility, nonspecific toxicity. This study aimed develop evaluate an inhalable Cela-loaded nanoemulsion (NE) formulation enhance targeted drug delivery therapeutic efficacy in non-small cell lung cancer (NSCLC). Methods: The NE was optimized using Capmul MCM (25%), Tween 80 (20%), Transcutol HP (5%), water (50%) as the oil, surfactant, co-surfactant, aqueous phase, respectively. Physicochemical characterization included globule size, zeta potential, release simulated fluid. In vitro aerosolization performance, cytotoxicity NSCLC lines (A549), scratch clonogenic assays, 3D tumor spheroid models were employed assess potential. Results: showed size of 201.4 ± 3.7 nm −15.7 0.2 mV. Drug sustained, with 20.4 5.5%, 29.1 10%, 64.6 4.1%, 88.1 5.2% released at 24, 48, 72, 120 h, studies indicated median aerodynamic particle 4.8 μm, confirming respirability lung. Cell culture higher toxicity NE-Cela cells. significantly reduced A549 viability, showing ~6-fold decrease IC50 (0.2 0.1 μM) compared Cela alone (1.2 μM). Migration assays demonstrated proliferation, supported activity tumor-like environments. Conclusions: improved Cela’s physicochemical limitations enhanced anti-cancer models. These findings support targeted, well-tolerated option treatment.
Language: Английский