title: Development of a myricetin/hydroxypropyl-β-cyclodextrin inclusion complex: preparation, characterization, and evaluation.
abstract: Myricetin shows low oral bioavailability (<10%) in rats due to poor aqueous solubility, though it has various pharmacological activities. Complexation with cyclodextrins (CDs) is a potent pharmaceutical method to enhance the bioavailability of poorly soluble compounds. The myricetin/HP-β-CD inclusion complex was prepared and confirmed by DSC, PXRD, and SEM. Here, the inclusion mode is described in detail with regard to structural and energetic aspects using a phase solubility diagram and 1H NMR, NOESY, and FT-IR spectra. The water solubility and dissolution rate of myricetin were greatly enhanced by forming the myricetin/HP-β-CD inclusion complex. Consequently, the oral bioavailability of the myricetin/HP-β-CD inclusion complex in rats was effectively increased 9.4-fold over free myricetin, and its antioxidant activity was also improved. The present study provides useful information for the potential application of complexation with myricetin, a naturally occurring hydrophobic phenolic compound in herbal medicine.
authors.affiliation: Institute 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.
authors.forename: Yashu
authors.initials: Y
authors.lastname: Yao
authors.affiliation: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai, China. Electronic address: rosexie_1996@hotmail.com.
authors.forename: Yan
authors.initials: Y
authors.lastname: Xie
authors.affiliation: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
authors.forename: Chao
authors.initials: C
authors.lastname: Hong
authors.affiliation: Pharmacy Department, Shanghai TCM-Integrated Hospital, Shanghai, China. Electronic address: lgwshutcm@163.com.
authors.forename: Guowen
authors.initials: G
authors.lastname: Li
authors.affiliation: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
authors.forename: Hongyi
authors.initials: H
authors.lastname: Shen
authors.affiliation: Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
authors.forename: Guang
authors.initials: G
authors.lastname: Ji
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D001713:Biphenyl Compounds / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D005419:Flavonoids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D008297:Male; D010851:Picrates / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000975:Antioxidants; D001713:Biphenyl Compounds; D004337:Drug Carriers; D005419:Flavonoids; D010851:Picrates; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C040015:myricetin; C004931:1,1-diphenyl-2-picrylhydrazyl
keywords: Characterization; Hydroxypropyl-β-cyclodextrin; In vitro dissolution; Inclusion complex; Myricetin; Pharmacokinetics