Development and evaluation of Chrysin-Phospholipid complex loaded solid lipid nanoparticles - storage stability and in vitro anti-cancer activity

J Microencapsul. 2018 Sep;35(6):600-617. doi: 10.1080/02652048.2018.1559369.

Abstract

Context: Flavonoids show promising anticancer potential but it is limited due to poor solubility.

Objective: The present investigation was to prepare Chrysin-Phospholipid complex loaded solid lipid nanoparticles (Ch-PC-SLNs) for improving its encapsulation as compared to that of Chrysin loaded SLNs (Ch-SLNs) and evaluated for potential increase in the anti-cancer activity against MCF-7 cell line.

Methods: The physiochemical characteristics and release kinetics for Ch-SLNs and Ch-PC-SLNs were evaluated and compared. Storage stability of Ch-PC-SLNs was evaluated up to 3 months. Solid state properties (DSC, XRD) and morphology (AFM) of Ch-PC-SLNs were also studied. In-vitro anticancer activity was investigated by using MTT assay.

Results and discussion: Ch-PC-SLNs exhibited higher encapsulation efficiency than Ch-SLNs and zero order release kinetics. Ch-PC-SLNs were found to be stable upto 3 months upon lyophilisation with mannitol as cryoprotectant. DSC and XRD study revealed the loss of highly crystalline nature of Chrysin in Ch-PC-SLNs. The Ch-PC-SLNs lead to significantly higher in-vitro anticancer activity than that of bulk Chrysin.

Conclusion: The study concludes that phospholipids complex with Chrysin lead to improve encapsulation, storage stability of SLNs and in vitro anticancer activity.

Keywords: Breast cancer (MCF-7) cell line; Chrysin; Chrysin-Phospholipid complex loaded SLNs; freeze drying; intracellular reactive oxygen species (ROS); solid lipid nanoparticles.

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Cell Survival / drug effects
  • Drug Liberation
  • Drug Screening Assays, Antitumor
  • Drug Stability
  • Female
  • Flavonoids / chemistry*
  • Flavonoids / pharmacology
  • Freeze Drying
  • Humans
  • Lipids / chemistry
  • MCF-7 Cells
  • Nanoparticles
  • Particle Size
  • Phospholipids / chemistry*

Substances

  • Antineoplastic Agents
  • Flavonoids
  • Lipids
  • Phospholipids
  • chrysin