Enhancement of Oral Bioavailability of Puerarin by Polybutylcyanoacrylate Nanoparticles

Abstract

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.

Poly(n-butylcyanoacrylate) nanoparticles for oral delivery of quercetin: preparation, characterization, and pharmacokinetics and biodistribution studies in Wistar rats

“…It might have further been incorporated in polymer NPs by emulsion during the polymerization. 18 This rapid polymerization reaction occurred gradually when the pH was adjusted stepwise (pH .5.0).…”

“…In the present study, the difference in pharmacokinetics results and the in vitro release profile of QT-PBCA NPs may be caused by the possible enterohepatic recirculation. 18 The result indicated that the relative bioavailability of QT-PBCA NPs and QT-PBCA+P-80 enhanced the QT bioavailability by 2.38-and 4.93-fold respectively as compared to that of free QT. The increased bioavailability of PBCA NPs may be a co-work of direct uptake of NPs through the GI tract.…”

“…16 A recent study has shown that PBCA NPs have been widely investigated to enhance the oral absorption of poorly soluble polyphenols and isoflavones such as curcumin and puerarin. 17,18 Most interestingly, PBCA NPs have been employed as effective delivery systems in the brain because the particles entrap the compounds and prevent rapid elimination or degradation as well as promote penetration through the BBB and distribution in the brain tissue when coated with polysorbate-80 (P-80) on their surfaces. 19 There have been several reports of PBCA NPs coated with P-80 that could significantly improve the delivery to the brain of anticancer agents, 20 antifungal drugs, 21 peptides, 22 MRZ 2/576 (N-methyl-d-aspartate receptor antagonists), 23 antibiotics, 24 nonsteroidal anti-inflammatory drugs, 25 and antiviral drugs.…”

“…49 Elsewhere in the literature, puerarin-PBCA NPs caused a significant enhancement in oral bioavailability of puerarin by more than 5.5-fold to overcome enterohepatic recirculation. 18 Other research groups have reported an improvement in bioavailability of both oral and intravenous administration by NP coupled to QT that has shown promising results.…”

Absorptive interactions of concurrent oral administration of (+)-catechin and puerarin in rats and the underlying mechanisms

“…They both have potent antioxidant activity, which allows them to scavenge free radicals, they are widely used for the treatment of cardiocerebrovascular diseases [13][14][15] , they are readily metabolized by certain enzymes, and they can undergo methylation, glucuronidation and sulfation in vivo [16,17] . Although both (+)-C and Pue showed poor oral bioavailability when individually administered at a single dose [18,19] , co-administration of both drugs achieved enhanced therapeutic effects. Songlingxuemaikang Capsule ® , which is a type of traditional Chinese medicine (TCM) compound preparation that is utilized for the treatment of some cardiocerebrovascular diseases and hypertension in clinical applications [20] , mainly contains Pinus massoniana Lamb needle and Pueraria lobata (Willd) Ohwi root extracts, the bioactive substances of which are (+)-C and Pue [21,22] .…”