DEVELOPMENT AND CHARACTERIZATION OF LAPPAOL F LOADED FUNCTIONALIZED SOLID LIPID NANOCARRIERS FOR TARGETED DELIVERY IN CANCERS

Abstract

Objectives: To develop, optimize, and characterize lactoferrin-functionalized Lappaol F-loaded solid lipid nanocarriers (Lf-LpF-SLNs) for targeted anticancer delivery, addressing the poor solubility and limited bioavailability of Lappaol F.

Methods: Lappaol F-loaded solid lipid nanocarriers were prepared by melt emulsification–probe sonication and optimized using a three-factor, three-level Box–Behnken Design (BBD) with Compritol 888 ATO concentration, Poloxamer 188 concentration, and probe sonication pulse duty cycle as independent variables. The optimized formulation was surface functionalized with lactoferrin via EDC/NHS coupling, followed by evaluation of physicochemical properties, drug release, stability, and in vitro cytotoxicity.

Results: The quadratic models for particle size (R² = 0.8109) and entrapment efficiency (R² = 0.8370) were statistically significant (p < 0.05). Optimized batch JF10 (desirability 0.924) showed particle size of 1726 ± 4.34 nm, PDI 0.178 ± 0.016, zeta potential −30.4 ± 1.22 mV, and entrapment efficiency 81.46 ± 1.68%. Lactoferrin conjugation was confirmed by FTIR through Amide I (1653 cm⁻¹) and Amide II (1545 cm⁻¹) bands. Lf-LpF-SLNs exhibited enhanced cytotoxicity (IC₅₀ 14.82 ± 0.92 μg/mL) compared to LpF-SLNs (21.38 ± 1.06 μg/mL) and free Lappaol F (28.64 ± 1.24 μg/mL). Stability was confirmed over six months under accelerated conditions.

Conclusion: Lf-LpF-SLNs represent a promising receptor-targeted nanocarrier system with improved tumor selectivity and cytotoxic efficacy, warranting further in vivo investigation.