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Article type: Research Article
Authors: Dong, Qiannian; * | Yuan, Hui-Ling; * | Qian, Jia-Jia | Zhang, Cai-Yun; ** | Chen, Wei-Dong
Affiliations: School of Pharmacy, Anhui University of Chinese Medicine, Anhui Academy of Chinese Medicine, Hefei 230038, P.R. China
Correspondence: [**] Corresponding author. E-mail: [email protected].
Note: [*] These authors contributed equally.
Abstract: Nanosuspensions technique is an important tool to enhance the saturation solubility and dissolution velocity of poorly soluble drugs. Trans-resveratrol (t-Res) with extensive pharmacological effects was severely restricted by poor solubility and short biological half-life. In this study, anti-solvent precipitation was employed to development trans-resveratrol nanosuspensions (t-Res NS) with PVPK30 as stabilizer. The physicochemical properties, in vitro release and in vivo pharmacokinetics of t-Res NS were investigated. The mean particle size, zeta potential, encapsulation efficiency and drug loading of t-Res NS prepared by the optimal prescription were 96.9 nm, −20.4mV, 78% and 28.1%, respectively. The morphology of t-Res nanoparticles was spherical indicated by SEM with amorphous phase verified by XRD and DSC. The t-Res NS present a good physical stability as well as enhanced chemical stability. Compared to crude drug, the in vitro dissolution rate of t-Res NS was increased with fitting Higuchi equation (Q=0.3215t1/2+0.0070). The in vivo pharmacokinetic test in rats showed that the AUC0∼t of t-Res NS (559.4 μg/mL·min) was about 3.6-fold higher than that of t-Res solution. Meanwhile, the MRT of t-Res nanosuspensions was longer than that of t-Res solution. These results suggested that NS may be a potentially nanocarrier for clinical delivery of t-Res.
Keywords: Nanosuspensions, trans-resveratrol, anti-solvent precipitation, in vitro dissolution, in vivo pharmacokinetics
DOI: 10.3233/BME-181729
Journal: Bio-Medical Materials and Engineering, vol. 29, no. 3, pp. 333-345, 2018
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