title: Preparation Nanocrystals of Poorly Soluble Plant Compounds Using an Ultra-Small-Scale Approach.
abstract: The usage of downscaling technology for producing nanosuspensions/nanocrystals can be beneficial for formulation development, which has attracted increased attention recently. An ultra-small bead milling method (5 mg compound per batch, smallest scale to date) was tested to produce nanocrystals of four poorly soluble plant compounds, i.e., quercetin, rutin, resveratrol, and hesperidin. A particle size of ranged from 200 to 500 nm was obtained for nanosuspensions of four compounds and the stabilizer selection could be achieved within 2 h by using this ultra-small bead milling method. Six months stability was observed for selected samples. In addition, the scalability of the ultra-small lab-scale milling was confirmed when it was conducted under optimal conditions. A simple and fast ultra-small-scale approach for nanosuspension production was established. Freeze-drying was applied to convert nanosuspensions into solid forms. Finally, freeze-dried intermediates with good redispersity and physical stability were obtained, which could be used for further application.
authors.affiliation: Department of Pharmaceutical Engineering, Qingdao University of Science and Technology, Qingdao, China. taoyanghe@hotmail.com.
authors.forename: Tao
authors.initials: T
authors.lastname: Liu
authors.affiliation: Department of Pharmaceutical Engineering, Qingdao University of Science and Technology, Qingdao, China.
authors.forename: Guili
authors.initials: G
authors.lastname: Yao
authors.affiliation: Department of Pharmaceutical Engineering, Qingdao University of Science and Technology, Qingdao, China.
authors.forename: Xiaotian
authors.initials: X
authors.lastname: Liu
authors.affiliation: Department of Internal Medicine, Qingdao Shibei District People Hospital, Qingdao, China.
authors.forename: Haipeng
authors.initials: H
authors.lastname: Yin
mesh_terms: D005612:Freeze Drying; D006569:Hesperidin / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry; D011794:Quercetin / Q000737:chemistry; D000077185:Resveratrol; D012431:Rutin / Q000737:chemistry; D012995:Solubility; D013267:Stilbenes / Q000737:chemistry; D013535:Suspensions; D013678:Technology, Pharmaceutical
chemical_list: D013267:Stilbenes; D013535:Suspensions; D012431:Rutin; D011794:Quercetin; D006569:Hesperidin; D000077185:Resveratrol
keywords: drug nanosuspensions/nanocrystals; poorly soluble plant compounds; ultra-small scale; wet bead milling