1. Evaluation of anticancer activity of honokiol by complexation with hydroxypropyl-β-cyclodextrin.
- Author
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Wu, Weiwei and Xue, Wei
- Subjects
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CELL cycle , *AQUEOUS solutions , *INCLUSION compounds , *BIOAVAILABILITY , *SOLUBILITY , *HUMAN beings , *DRUG solubility - Abstract
• Honokiol suffer from low aqueous solubility and low overall bioavailability. • Cyclodextrin inclusion techniques are strong tools to solve the solubility issues. • >The HK-HP-β-CD has excellent solubility, dissolution rate and oral bioavailability. • The HK-HP-β-CD exhibited higher antitumor activity against HepG2 than free HK. Honokiol (HK), an active compound derived from Magnolia officinalis Rehd. et Wils , possesses many beneficial biological activities for human beings. However, its poor solubility and low bioavailability severely limits its application. In this way, to improve the pharmaceutical properties, the HK was complexed in hydroxypropyl-β-cyclodextrin (HP-β-CD) and its oral bioavailability and antitumor effects were evaluated. The HK/HP-β-CD inclusion complex (1:1) was prepared by saturated aqueous solution method. The inclusion complex (HK-HP-β-CD) obtained had a higher solubility, about 1497 times that of the free HK. The dissolution rate and the oral bioavailability of HK was also significantly higher from inclusion complex than from free HK. Furthermore, the HK-HP-β-CD exhibited higher antitumor activity against Human Hepatoma Cell Line (HepG2) than free HK. More cells were arrested in the sub-G1 phase of the cell cycle and were induced to undergo late apoptosis when treated with the HK-HP-β-CD than when treated with free HK. [ABSTRACT FROM AUTHOR]
- Published
- 2020
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