Preparation, characterization and in vivo evaluation of curcumin self-nano phospholipid dispersion as an approach to enhance oral bioavailability

Int J Pharm. 2015 Jul 15;489(1-2):117-23. doi: 10.1016/j.ijpharm.2015.04.067. Epub 2015 Apr 29.

Abstract

The aim of this study was to examine the efficacy of self-nano phospholipid dispersions (SNPDs) based on Phosal(®) to improve the oral bioavailability of curcumin (CUR). SNPDs were prepared with Phosal(®) 53 and Miglyol 812 at different surfactant ratio. Formulations were evaluated for particle size, polydispersity index, zeta potential, and robustness toward dilution, TEM as well as in vitro drug release. The in vivo oral absorption of selected formulations in comparison to drug suspension was evaluated in rats. Moreover, formulations were assessed for in vitro characteristic changes before and after storage. The SNPDs were miscible with water in any ratio and did not show any phase separation or drug precipitation. All the formulas were monodisperse with nano range size from 158±2.6 nm to 610±6.24 nm. They passed the pharmacopeial tolerance for CUR dissolution. No change in dissolution profile and physicochemical characteristics was detected after storage. CUR-SNPDs are found to be more bioavailable compared with suspension during an in vivo study in rats and in vitro release studies failed to imitate the in vivo conditions. These formulations might be new alternative carriers that enhance the oral bioavailability of poorly water-soluble molecules, such as CUR.

Keywords: Bioavailability; Curcumin; In vivo evaluation; Nano Dispersion; Phospholipid.

MeSH terms

  • Animals
  • Biological Availability
  • Curcumin / administration & dosage
  • Curcumin / chemistry*
  • Curcumin / pharmacokinetics
  • Drug Compounding
  • Glycerol / analogs & derivatives
  • Glycerol / chemistry
  • Phospholipids / chemistry*
  • Polyethylene Glycols / chemistry
  • Rats, Wistar
  • Surface-Active Agents / chemistry
  • Triglycerides / chemistry

Substances

  • Phospholipids
  • Surface-Active Agents
  • Triglycerides
  • miglyol 812
  • Polyethylene Glycols
  • cremophor EL
  • Curcumin
  • Glycerol