A Hydroxypropyl Methylcellulose-Based Solid Dispersion of Curcumin with Enhanced Bioavailability and its Hepatoprotective Activity

Curcumin is a polyphenol compound derived from the rhizomes of that exhibits antioxidant, anti-inflammatory, anticancer, and antimicrobial properties. However, its low solubility in aqueous solutions, low absorption following oral administration, and rapid degradation limit its use as a functional f...

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Published inBiomolecules (Basel, Switzerland) Vol. 9; no. 7; p. 281
Main Authors Shin, Myoung-Sook, Yu, Jun Sang, Lee, Jaemin, Ji, Young Seok, Joung, Hee Joung, Han, Yu-Mee, Yoo, Hye Hyun, Kang, Ki Sung
Format Journal Article
LanguageEnglish
Published Switzerland MDPI 15.07.2019
MDPI AG
Subjects
bioavailability
Biological Availability
curcumin
Curcumin - pharmacology
Hep G2 Cells
Hepatocytes - drug effects
Hepatocytes - metabolism
hepatoprotective
Humans
hydroxypropyl methylcellulose
Hypromellose Derivatives - chemistry
Hydroxypropyl methylcellulose
bioavailability
hepatoprotective
curcumin
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Summary:Curcumin is a polyphenol compound derived from the rhizomes of that exhibits antioxidant, anti-inflammatory, anticancer, and antimicrobial properties. However, its low solubility in aqueous solutions, low absorption following oral administration, and rapid degradation limit its use as a functional food material. In this study, a hydroxypropyl methylcellulose-based solid dispersion of curcumin (DW-CUR 20) was prepared and its bioavailability was evaluated. In addition, its therapeutic efficacy as a hepatoprotective agent was investigated using the model of tert-butyl hydroperoxide (t-BHP)-induced hepatocyte damage. The rat plasma pharmacokinetic study showed that the oral curcumin bioavailability of DW-CUR 20 significantly increased compared to that of non-formulated curcumin. DW-CUR 20 showed a concentration-dependent hepatocyte protective effect on t-BHP-induced HepG2 cells. DW-CUR 20 inhibited the release of lactate dehydrogenase and decreased apoptosis-related proteins such as Poly (ADP-ribose) polymerase, cleaved caspase-7 and cleaved caspase-8 on t-BHP-treated HepG2 cells. These findings suggest that DW-CUR 20 could be a promising formulation for enhancing the therapeutic efficiency of curcumin and for improving the safety.
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These authors contributed equally to this work.
ISSN:2218-273X
2218-273X
DOI:10.3390/biom9070281