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

In the present investigation, we attempted to develop a lycopene-in- beta-CD -in-phospholipid vesicles (LCPV) with the sole aim of combining the solubilizing power of beta-CD with the sustained-release pattern of phospholipid vesicles. Inclusion complexes of beta-CD and lycopene were formed and characterized by using DSC and FT-IR. Double-loaded liposomes encapsulating lycopene beta-CD complex were prepared using soy lecithin, cholesterol, and beta-CD by thin film hydration method. The LCPV formulation was optimized using a 3(3) 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 in vivo 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 in vivo 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.