title: D-Alpha-tocopherol acid polyethylene glycol 1000 succinate, an effective stabilizer during solidification transformation of baicalin nanosuspensions.
abstract: Baicalin nanosuspensions, stabilized with 10% TPGS (relative to the weight of baicalin), were transformed into nanosuspensions powders by solidification process. Solidification methods for this transformation included freeze-drying, spray drying or vacuum drying. High pressure homogenization was applied for production of baicalin nanosuspensions used TPGS, SDS, P188, HPMC and MC as stabilizer, respectively. The influence of the different solidification transformation methods on the redispersibility of solid drug nanosuspensions was systemically investigated, such as freeze-drying, spray drying and vacuum drying. Each method was applied with three grades of process stresses called as "conservative", "moderate" and "aggressive" conditions, and the redispersibility index (RDI) of nanosuspensions stabilized by stabilizers (such as TPGS, SDS, P188, HPMC and MC) during those process was investigated. The results showed that there was significant difference in RDI of nanosuspensions after solidification process. The RDI(a) (1.09, 1.01, 1.05, 0.99), RDI(b) (1.03, 0.99, 1.06, 1.02) and RDI(c) (1.01, 1.01, 1.09, 1.08) of nanosuspensions stabilized by TPGS were more small during different solidification process, compared with those of nanosuspensions stabilized by other stabilizer. It was concluded that the baicalin nanosuspensions were subjected to agglomeration or crystal growth during solidification transformation, especially at high aggressive stress conditions. Meanwhile, compared to other stabilizer, the TPGS was more effective for stability of baicalin nanosuspensions, which could exhibit higher affinity to the drug crystal and stronger surface adsorption at different solidification stresses.
authors.affiliation: Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China. P.F.YueJxtcmi@gmail.com
authors.forename: Peng-Fei
authors.initials: PF
authors.lastname: Yue
authors.forename: Jing
authors.initials: J
authors.lastname: Wan
authors.forename: Yong
authors.initials: Y
authors.lastname: Wang
authors.forename: Yu
authors.initials: Y
authors.lastname: Li
authors.forename: Yue-Qin
authors.initials: YQ
authors.lastname: Ma
authors.forename: Ming
authors.initials: M
authors.lastname: Yang
authors.forename: Peng-Yi
authors.initials: PY
authors.lastname: Hu
authors.forename: Hai-Long
authors.initials: HL
authors.lastname: Yuan
authors.forename: Chang-Hong
authors.initials: CH
authors.lastname: Wang
mesh_terms: D003460:Crystallization; D004339:Drug Compounding / Q000379:methods*; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry*; D005419:Flavonoids / Q000737:chemistry*; D005612:Freeze Drying; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D044367:Phase Transition; D011092:Polyethylene Glycols; D012995:Solubility; D013386:Succinates / Q000737:chemistry*; D013499:Surface Properties; D013535:Suspensions; D014810:Vitamin E / Q000031:analogs & derivatives* / Q000737:chemistry
chemical_list: D005079:Excipients; D005419:Flavonoids; D013386:Succinates; D013535:Suspensions; D014810:Vitamin E; C038044:baicalin; D011092:Polyethylene Glycols; C014225:tocophersolan