Journal
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Volume 45, Issue 9, Pages 1444-1450Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/03639045.2019.1628041
Keywords
Curcumin; micelles; oral bioavailability; Caco-2 monolayer; anti-gastroesophageal reflux
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Funding
- Nature Science Foundation of Shanghai [18ZR1436700]
- National Nature Science Foundation of China [81874402]
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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 (R) HS15, and the other (CM-F) was prepared using Pluronic (R) F127 and Solutol (R) 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.
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