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 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.

Keywords:

• Lycopene
• β-cyclodextrin
• double-loaded liposome
• factorial design
• carotenoid

Acknowledgements

We are grateful to Dr. Prashant Kharkar, Professor, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management (SPPSPTM), SVKM’S NMIMS Mumbai for his valuable inputs in the manuscript, Dr. Khushwant Yadav, Associate Professor, SPPSPTM for his advice related to DoE and Dr. Mukesh Nandave Associate Professor, DIPSU, New Delhi and Mr. Ankit Laddha (PhD student, SPPSPTM) for animal studies protocol design. Authors are thankful to Dr. Bala Prabhakar, Dean, SPPSPTM SVKM’S NMIMS, Mumbai, for providing the laboratory facilities.

Disclosure statement

No potential conflict of interest was reported by the authors.