A novel formulation of [6]-gingerol: Proliposomes with enhanced oral bioavailability and antitumor effect

Int J Pharm. 2018 Jan 15;535(1-2):308-315. doi: 10.1016/j.ijpharm.2017.11.006. Epub 2017 Nov 7.

Abstract

[6]-Gingerol, one of the components of the rhizome of Ginger, has a variety of biological activities such as anticoagulant, antioxidative, antitumor, anti-inflammatory, antihypertensive, and so forth. However, as one of the homologous phenolic ketones, [6]-gingerol is insoluble in water which limits its applications. Herein, we prepared [6]-gingerol proliposomes through modified thin-film dispersion method, which was spherical or oval, and physicochemically stable with narrow size distribution. Surprisingly, in vitro release of [6]-gingerol loaded proliposome compared with the free [6]-gingerol was significantly higher and its oral bioavailability increased 5-fold in vivo. Intriguingly, its antitumor effect was enhanced in the liposome formulation. Thus, our prepared [6]-gingerol proliposome proved to be a novel formulation for [6]-gingerol, which significantly improved its antitumor effect.

Keywords: Antitumor; Extraction; Proliposome; [6]-Gingerol.

MeSH terms

  • Administration, Oral
  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / therapeutic use
  • Biological Availability
  • Catechols / administration & dosage*
  • Catechols / chemistry*
  • Catechols / pharmacokinetics
  • Catechols / therapeutic use
  • Cell Survival / drug effects
  • Chemistry, Pharmaceutical
  • Drug Liberation
  • Fatty Alcohols / administration & dosage*
  • Fatty Alcohols / chemistry*
  • Fatty Alcohols / pharmacokinetics
  • Fatty Alcohols / therapeutic use
  • Hep G2 Cells
  • Humans
  • Liposomes
  • Male
  • Neoplasms / drug therapy
  • Rats, Sprague-Dawley

Substances

  • Antineoplastic Agents
  • Catechols
  • Fatty Alcohols
  • Liposomes
  • gingerol