Enhanced oral delivery and anti-gastroesophageal reflux activity of curcumin by binary mixed micelles

Abstract

The aim of this study was to improve the solubility, oral bioavailability, and anti-gastroesophageal reflux activity of curcumin (CM) by preparing two CM-loaded, novel, binary mixed micelles (CM-M). The two CM-M were prepared by ethanol thin-film hydration method. One (CM-T) was prepared using D-alpha-tocopheryl polyethylene glycol 1000 succinate and Solutol^®HS15, and the other (CM-F) was prepared using Pluronic^®F127 and Solutol^®HS15. The entrapment efficiency and drug loading of CM-T were 83.61 ± 0.54% and 2.20 ± 0.65%, respectively, which were lower than those of CM-F (88.66 ± 0.12% and 1.47 ± 0.26%, respectively). TEM results demonstrated that CM-T and CM-F were homogeneous and spherical. The permeability of CM delivered via CM-T and CM-F was enhanced across a Caco-2 cell monolayer, and CM-T and CM-F showed a 5.24- and 4.76-fold increase in relative oral bioavailability, respectively compared with free CM. In addition, the in vivo anti-gastroesophageal reflux study showed that CM-T and CM-F achieved higher anti-gastroesophageal reflux efficacy compared with free CM. Collectively, these findings were indicative of an oral micelle formulation of CM with increased solubility, oral bioavailability, and anti-gastroesophageal reflux activity.

Keywords:

• Curcumin
• micelles
• oral bioavailability
• Caco-2 monolayer
• anti-gastroesophageal reflux

Disclosure statement

The authors declare no competing financial interest.

Additional information

Funding

This work was supported by Nature Science Foundation of Shanghai under Grant No. 18ZR1436700 and National Nature Science Foundation of China under Grant No. 81874402.