title: Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: an in vitro and in vivo evaluation.
abstract: Although myricetin has various pharmacological applications, it shows low oral bioavailability (<10%) in rats due to its poor aqueous solubility. To overcome this issue, myricetin nanosuspensions were developed and the effects of stabilizers were investigated. Based on the particle size and zeta potential, stabilizers soya lecithin, TPGS, HP-β-CD, and/or a combination thereof were used. The prepared nanosuspensions were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRD). The resulting myricetin nanosuspensions contained particles in the size range of 300-500 nm and were physically stable. Myricetin was partially transformed from crystalline to amorphous forms in the presence of different excipients after the nanosizing process. The solubility and in vitro dissolution of all myricetin nanosuspensions were greatly increased compared with those of the myricetin powder. Consequently, the relative bioavailability in rats were 2.44, 3.57, 1.61, and 2.96 for nanosuspensions stabilized with TPGS, soya lecithin, soya lecithin+TPGS, and HP-β-CD+TPGS, respectively, relative to that of the coarse myricetin. This research demonstrated that nanosuspension is a promising strategy for delivering poor water-soluble drugs such as myricetin and that stabilizers played a critical role in the formulation design of myricetin nanosuspensions.
authors.affiliation: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China.
authors.forename: Chao
authors.initials: C
authors.lastname: Hong
authors.affiliation: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Dang
authors.affiliation: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China.
authors.forename: Guobei
authors.initials: G
authors.lastname: Lin
authors.affiliation: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China; Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Yashu
authors.initials: Y
authors.lastname: Yao
authors.affiliation: Pharmacy Department, Shanghai TCM-integrated Hospital, Shanghai 200082, China.
authors.forename: Guowen
authors.initials: G
authors.lastname: Li
authors.affiliation: Institute of Digestive Diseases, Long Hua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200032, China.
authors.forename: Guang
authors.initials: G
authors.lastname: Ji
authors.affiliation: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China.
authors.forename: Hongyi
authors.initials: H
authors.lastname: Shen
authors.affiliation: Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China. Electronic address: rosexie_1996@hotmail.com.
authors.forename: Yan
authors.initials: Y
authors.lastname: Xie
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004355:Drug Stability; D005419:Flavonoids / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry*; D008297:Male; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013499:Surface Properties; D013535:Suspensions; D014961:X-Ray Diffraction
chemical_list: D005419:Flavonoids; D013535:Suspensions; C040015:myricetin
keywords: Baicalein (PubChem CID: 5281605); Bioavailability; HP-β-CD (PubChem CID: 44134771); HPMC (PubChem CID: 57503849); Kaempferol (PubChem CID: 5280863); Myricetin; Myricetin (PubChem CID: 5281672); Nanosuspension; Poloxamer (PubChem CID: 24751); Quercetin (PubChem CID: 5280343); Silybin (PubChem CID: 31553); Solubility; Stabilizer; TPGS (PubChem CID: 71406); Vitexin (PubChem CID: 5280441)