Emmanuel Oshiogwe Okwuofu, Audrey Chee Hui Yong, Jonathan Chee Woei Lim, Johnson Stanslas
Liposomal nanocarrier represents a potential strategy to deliver the lipophilic compounds, AGP for improved pharmacokinetics profile and efficacy.
OBJECTIVES: This study aimed to develop, characterize, and evaluate the efficacy of a soy lecithin-based formulation of AGP (Lipo-AGP) in Balb/c.
METHODS: Lipo-AGP was formulated using thin-film hydration. The formulation was characterized, followed by pharmacokinetic evaluation. A 14-day house dust mite (HDM)-induced lung inflammation model in BALB/c mice was used, comprising sensitization and challenge phases. Bronchoalveolar lavage (BAL) fluid cell analysis, cytokine assays, gene expression, lung histology, serum HDM-specific IgE, and immunoblotting were evaluated.
KEY FINDINGS: The optimized Lipo-AGP formulation demonstrated a vesicle size of 178.9 ± 20.78 nm, a zeta potential of -27.73 ± 1.02 mV, and a PDI of 0.28 ± 0.001, alongside a high entrapment efficiency of 95.67 ± 1.78%. Stability analysis at 4°C and 25°C for 6 months did not show degradation. In vivo pharmacokinetics studies revealed that Lipo-AGP achieved a 1.5-fold improvement in both the rate and extent of AGP absorption compared to free AGP. Lipo-AGP exhibited a dose-dependent decrease in HDM-induced pulmonary cell infiltration, mucus hypersecretion, collagen deposition, and inhibition of nuclear NF-κB p65. These results suggest that Lipo-AGP exerts protective effects against HDM-induced lung inflammation, through inhibition of NF-κB signalling.
CONCLUSIONS: Liposomal nanocarrier represents a potential strategy to deliver the lipophilic compounds, AGP for improved pharmacokinetics profile and efficacy.