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Development of a myricetin/hydroxypropyl-β-cyclodextrin inclusion complex: preparation, characterization, and
Yashu Yao1, Yan Xie2, Chao Hong2
1Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China; Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Carbohydrate Polymers
|June 8, 2014
Summary
Myricetin, a natural compound, has poor absorption. Complexing it with hydroxypropyl-β-cyclodextrin (HP-β-CD) significantly boosts its solubility, bioavailability, and antioxidant effects in rats.
Area of Science:
- Pharmacology
- Materials Science
- Physical Chemistry
Background:
- Myricetin exhibits diverse pharmacological activities but suffers from low oral bioavailability (<10% in rats) due to poor aqueous solubility.
- Cyclodextrin complexation is a recognized strategy to enhance the bioavailability of poorly soluble drugs.
Purpose of the Study:
- To prepare and characterize a myricetin/hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex.
- To investigate the structural and energetic aspects of the inclusion complex formation.
- To evaluate the impact of complexation on myricetin's solubility, dissolution rate, oral bioavailability, and antioxidant activity.
Main Methods:
- Preparation and characterization of the myricetin/HP-β-CD inclusion complex using DSC, PXRD, and SEM.
- Detailed investigation of the inclusion mode via phase solubility studies, 1H NMR, NOESY, and FT-IR spectroscopy.
- Assessment of enhanced solubility, dissolution rate, oral bioavailability (9.4-fold increase), and antioxidant activity in a rat model.
Main Results:
- The myricetin/HP-β-CD inclusion complex was successfully prepared and characterized.
- Complexation significantly enhanced the water solubility and dissolution rate of myricetin.
- Oral bioavailability of myricetin was increased 9.4-fold, and its antioxidant activity was also improved.
Conclusions:
- Complexation with HP-β-CD effectively overcomes the poor aqueous solubility and low oral bioavailability of myricetin.
- The study demonstrates the potential of cyclodextrin complexation for improving the therapeutic efficacy of myricetin, a valuable natural compound from herbal medicine.
