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Enhancement of Oral Bioavailability of Puerarin by Polybutylcyanoacrylate Nanoparticles

2011; Hindawi Publishing Corporation; Volume: 2011; Linguagem: Inglês

10.1155/2011/126562

1687-4129

Lixia Zhao, Anchang Liu, Min Sun, Jinsong Gu, Haigang Wang, Shuang Wang, Jing Zhang, Chenyu Guo, Rui Duan, Guangxi Zhai,

Advanced Drug Delivery Systems

The interest using novel drug delivery systems to improve oral bioavailability of drug with poor solubility is increasing. In this study, a new oral delivery system, polybutylcyanoacrylate nanoparticles (PBCNs), was introduced to improve the oral bioavailability of puerarin (PUE). PUE-loaded PBCN was successfully prepared by anionic polymerization method. Characterization of PUE-loaded PBCN was evaluated with morphology, size, zeta potential, and in vitro release study. The PBCN loading PUE exhibited a spherical shape under transmission electron microscopy with an average size of 159.4 nm, and the zeta potential was −15.0 mV. The in vitro release of PUE-loaded PBCN showed an initial burst release followed by a sustained release. Physicochemical state of PUE in PBCN was investigated by differential scanning colorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy. The results indicated that PUE in PBCN was in a noncrystalline state. The oral pharmacokinetic study in rats showed that the relative bioavailability of PUE-encapsulated PBCN to the crude PUE was more than 550%. It can be concluded that PBCN as an oral drug carrier can significantly improve the oral bioavailability of PUE.