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

Enhanced oral delivery and anti-gastroesophageal reflux activity of curcumin by binary mixed micelles. Drug Dev Ind Pharm. 2019 Jun 06;:1-25 Authors: Sun Y, Li Y, Shen Y, Wang J, Tang J, Zhao Z Abstract The aim of this study was to improve the solubility, oral bioavailability, and anti-gastroesophageal reflux activity of curcumin by preparing two curcumin-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 curcumin. 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 curcumin. Collectively, these findings were indicative of an oral micelle formulation of curcumin with increased solubility, oral bioavailabil...
Source: Drug Development and Industrial Pharmacy - Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research