Enhancement of Oral Bioavailability of Puerarin byPolybutylcyanoacrylate Nanoparticles

[摘要] The interest using novel drug delivery systems to improve oralbioavailability of drug with poor solubility is increasing. In thisstudy, a new oral delivery system, polybutylcyanoacrylatenanoparticles (PBCNs), was introduced to improve the oralbioavailability of puerarin (PUE). PUE-loaded PBCN was successfullyprepared by anionic polymerization method. Characterization ofPUE-loaded PBCN was evaluated with morphology, size, zeta potential,and in vitro release study. The PBCN loading PUE exhibited a sphericalshape under transmission electron microscopy with an average size of159.4 nm, and the zeta potential was −15.0 mV. The in vitro release of PUE-loaded PBCN showed an initial burstrelease followed by a sustained release. Physicochemical state of PUEin PBCN was investigated by differential scanning colorimetry, X-raydiffraction, and Fourier transform infrared spectroscopy. The resultsindicated that PUE in PBCN was in a noncrystalline state. The oralpharmacokinetic study in rats showed that the relative bioavailabilityof PUE-encapsulated PBCN to the crude PUE was more than 550%. Itcan be concluded that PBCN as an oral drug carrier can significantlyimprove the oral bioavailability of PUE.

[学科分类] 材料工程