title: In vitro and in vivo evaluation of riccardin D nanosuspensions with different particle size.
abstract: Riccardin D (RD) is a novel compound extracted from Chinese liverwort Marchantia polymorpha L. It exhibits various anticancer activities and can be used during lung cancer treatment. However, the compound's low solubility hinders its development. Recently nanosuspension has been developed as one of the most promising formulations for poorly water-soluble drugs. In order to understand the dissolution behavior of riccardin D in vitro and in vivo, two nanosuspensions of riccardin D with markedly different sizes were prepared. The particle size of nanosuspension A prepared by bottom-up method was 184.1±3.15 nm, while that of nanosuspension B prepared by top-down method was 815.4±9.65 nm. The main purpose of this study was to investigate the effects of particle size on pharmacokinetics and tissue distribution after intravenous administration. Riccardin D dissolving in organic solution was studied as control group. In pharmacokinetics study in Wistar rats, nanosuspension A showed properties similar to the control group, while nanosuspension B exhibited rather different properties. In tissue distribution research on Kunming strain mice, nanosuspension A had a multi-peak phenomenon because of reticulate endothelial system (RES) while nanosuspension B showed a high uptake in RES organs that passively target to the lungs. In conclusion, particle size of riccardin D nanosuspensions had obvious effects on pharmacokinetics and tissue distribution.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Guangpu
authors.initials: G
authors.lastname: Liu
authors.forename: Dianrui
authors.initials: D
authors.lastname: Zhang
authors.forename: Yang
authors.initials: Y
authors.lastname: Jiao
authors.forename: Hejian
authors.initials: H
authors.lastname: Guo
authors.forename: Dandan
authors.initials: D
authors.lastname: Zheng
authors.forename: Lejiao
authors.initials: L
authors.lastname: Jia
authors.forename: Cunxian
authors.initials: C
authors.lastname: Duan
authors.forename: Yue
authors.initials: Y
authors.lastname: Liu
authors.forename: Xiaona
authors.initials: X
authors.lastname: Tian
authors.forename: Jingyi
authors.initials: J
authors.lastname: Shen
authors.forename: Caiyun
authors.initials: C
authors.lastname: Li
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
authors.forename: Hongxiang
authors.initials: H
authors.lastname: Lou
mesh_terms: D000818:Animals; D004355:Drug Stability; D035926:Hepatophyta / Q000737:chemistry; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D010647:Phenyl Ethers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013267:Stilbenes / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D010647:Phenyl Ethers; D013267:Stilbenes; C547185:riccardin D