title: Process optimization and evaluation of novel baicalin solid nanocrystals.
abstract: The objective of this study was to prepare baicalin solid nanocrystals (BCN-SNS) to enhance oral bioavailability of baicalin. A Box-Behnken design approach was used for process optimization. The physicochemical properties and pharmacokinetics of the optimal BCN-SNS were investigated. Multiple linear regression analysis for process optimization revealed that the fine BCN-SNS was obtained wherein the optimal values of homogenization pressure (bar), homogenization cycles (cycles), amount of TPGS to drug (w/w), and amount of MCCS to drug (w/w) were 850 bar, 25 cycles, 10%, and 10%, respectively. Transmission electron microscopy and scanning electron microscopy results indicated that no significant aggregation or crystal growth could be observed in the redispersed freeze-dried BCN-SNS. Differential scanning calorimetry and X-ray diffraction results showed that BCN remained in a crystalline state. Dissolution velocity of the freeze-dried BCN-SNS powder was distinctly superior compared to those of the crude powder and physical mixture. The bioavailability of BCN in rats was increased remarkably after oral administration of BCN-SNS (P < 0.05), compared with those of BCN or the physical mixture. The SNS might be a good choice for oral administration of poorly soluble BCN, due to an improvement of the bioavailability and dissolution velocity of BCN-SNS.
authors: Key Laboratory of Modern Preparation of TCM, Jiangxi University of Traditional Chinese Medicine, Xingwan, Nanchang, People's Republic of China. p.f.yuejxtcmi@gmail.com
authors: Peng-Fei
authors: PF
authors: Yue
authors: Yu
authors: Y
authors: Li
authors: Jing
authors: J
authors: Wan
authors: Yong
authors: Y
authors: Wang
authors: Ming
authors: M
authors: Yang
authors: Wei-Feng
authors: WF
authors: Zhu
authors: Chang-Hong
authors: CH
authors: Wang
authors: Hai-Long
authors: HL
authors: Yuan
mesh_terms: D000704:Analysis of Variance; D000818:Animals; D001682:Biological Availability; D005419:Flavonoids / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility
chemical_list: D005419:Flavonoids; C038044:baicalin
keywords: baicalin; in vivo/vitro evaluation; optimization; solid nanocrystals
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