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

Saloni Jhan1, Anil M Pethe1

  • 1Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM'S NMIMS University, Mumbai, India.

Journal of Liposome Research
|May 3, 2019
PubMed
Summary

Researchers developed lycopene-in-β-cyclodextrin-in-phospholipid vesicles (LCPV) for sustained drug release. The optimized LCPV formulation demonstrated significant cardio-protective activity in vivo.

Keywords:
Lycopenecarotenoiddouble-loaded liposomefactorial designβ-cyclodextrin

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Area of Science:

  • Pharmaceutics
  • Drug Delivery Systems
  • Nanotechnology

Background:

  • Lycopene, a potent antioxidant, suffers from poor bioavailability due to low solubility.
  • Phospholipid vesicles offer sustained release, while β-cyclodextrin enhances solubility.
  • Combining these technologies can improve lycopene's therapeutic potential.

Purpose of the Study:

  • To develop and characterize lycopene-in-β-cyclodextrin-in-phospholipid vesicles (LCPV).
  • To optimize LCPV formulation for improved entrapment efficiency and particle size.
  • To evaluate the in vitro sustained release and in vivo cardio-protective activity of LCPV.

Main Methods:

  • Inclusion complexes of lycopene and β-cyclodextrin (β-CD) were formed and characterized using DSC and FT-IR.
  • LCPV were prepared using soy lecithin, cholesterol, and β-CD via thin film hydration.
  • A 3³ full factorial design was employed for formulation optimization, followed by evaluation of particle size, entrapment efficiency, drug release, and in vivo activity.

Main Results:

  • The optimized LCPV formulation exhibited an entrapment efficiency of 78.9 ± 4.8% and a particle size of 255.15 ± 3 nm with a zeta potential of -32.6.
  • Sustained release of lycopene was observed, with 49.5% released over 12 hours.
  • In vivo studies demonstrated significant cardio-protective effects of the LCPV formulation.

Conclusions:

  • LCPV formulation effectively combines the solubilizing properties of β-CD with the sustained-release characteristics of phospholipid vesicles.
  • The optimized LCPV formulation is stable and suitable for sustained drug delivery.
  • LCPV shows promising potential for enhancing lycopene's therapeutic efficacy, particularly in cardio-protection.