Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: an in vitro and in vivo evaluation

doi:10.1016/j.ijpharm.2014.10.044

	Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: an in vitro and in vivo evaluation
	Hong, Chao 4; Dang, Yang 4; Lin, Guobei 4; Yao, Yashu 3,4; Li, Guowen 2; Ji, Guang 1; Shen, Hongyi 4; Xie, Yan 4
刊名	International journal of pharmaceutics
	2014-12-30
卷号	477 期号:1-2 页码:251-60
ISSN号	1873-3476
DOI	10.1016/j.ijpharm.2014.10.044
文献子类	Article
英文摘要	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.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/266415]
专题	中国科学院上海药物研究所
通讯作者	Xie, Yan
作者单位	1.Institute of Digestive Diseases, Long Hua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200032, China 2.Pharmacy Department, Shanghai TCM-integrated Hospital, Shanghai 200082, China; 3.Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; 4.Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China;
推荐引用方式 GB/T 7714	Hong, Chao,Dang, Yang,Lin, Guobei,et al. Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: an in vitro and in vivo evaluation[J]. International journal of pharmaceutics,2014,477(1-2):251-60.
APA	Hong, Chao.,Dang, Yang.,Lin, Guobei.,Yao, Yashu.,Li, Guowen.,...&Xie, Yan.(2014).Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: an in vitro and in vivo evaluation.International journal of pharmaceutics,477(1-2),251-60.
MLA	Hong, Chao,et al."Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: an in vitro and in vivo evaluation".International journal of pharmaceutics 477.1-2(2014):251-60.