Double-loaded liposomes encapsulating lycopene β-cyclodextrin complexes: preparation, optimization, and evaluation

Abstract

In the present investigation, we attempted to develop a lycopene-in- β-CD -in-phospholipid vesicles (LCPV) with the sole aim of combining the solubilizing power of β-CD with the sustained-release pattern of phospholipid vesicles. Inclusion complexes of β-CD and lycopene were formed and characterized by using DSC and FT-IR. Double-loaded liposomes encapsulating lycopene β-CD complex were prepared using soy lecithin, cholesterol, and β-CD by thin film hydration method. The LCPV formulation was optimized using a 3³ full factorial design to understand the impact of independent variables on entrapment efficiency and particle size. The formulations were evaluated for particle size, entrapment efficiency, drug release, and <i>in vivo</i> activity. The particle size of the optimized formulation showed entrapment efficiency of 78.9 ± 4.8% with a size of 255.15 ± 3 nm and zeta potential of -32.6, indicated the formation of a stable formulation which sustained the release up to 49.5% in 12 h. The results of the <i>in vivo</i> study indicated significant cardio-protective activity in an experimental animal. From the above results, it can be concluded that, the LCPV could be effectively used for sustained release of the drug.