Enhanced oral bioavailability of acetylpuerarin by poly(lactide-co-glycolide) nanoparticles optimized using uniform design combined with response surface methodology

Abstract

Acetylpuerarin (AP), an acetylated derivative of puerarin, shows brain-protective effects in animals. However, AP has low oral bioavailability because of its poor water solubility. The objective of this study was to design and develop poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs) to enhance the oral bioavailability of AP. The NPs were prepared using a solvent diffusion method optimized via uniform design (UD) combined with response surface methodology (RSM) and characterized by their morphology, particle size, zeta (ζ)-potential, encapsulation efficiency (EE), drug loading (DL), and in vitro drug release. A pharmacokinetic study was conducted in Wistar rats administered a single oral dose of 30 mg/kg AP. The optimized NPs were spherical and uniform in shape, with an average particle size of 145.0 nm, a polydispersity index (PI) of 0.153, and a ζ-potential of −14.81 mV. The release of AP from the PLGA NPs showed an initial burst release followed by a sustained release, following Higuchi’s model. The EE and DL determined in the experiments were 90.51% and 17.07%, respectively. The area under the plasma concentration-time curve (AUC0−∞) of AP-PLGA-NPs was 6,175.66±350.31 h ng/mL, which was 2.75 times greater than that obtained from an AP suspension. This study showed that PLGA NPs can significantly enhance the oral bioavailability of AP.

Oral delivery of lycopene-loaded microemulsion for brain-targeting: preparation, characterization, pharmacokinetic evaluation and tissue distribution

“…(2) The ME system might facilitate intestinal cellular uptake and lymphatic transport, which could contribute to the enhancement of lycopene absorption (Tang et al., 2013; Bala et al., 2016). (3) Tween 80 and Transcutol HP could exert synergistically as inhibitors of P-glycoprotein multidrug efflux system (Takahashi et al., 2002; Sun et al., 2016), which is mainly localized in the columnar epithelial cells of the lower gastrointestinal tract (Zakeri-Milani & Valizadeh, 2014). Thus, these microemlusion excipients could potentially enhance oral bioavailability of lycopene.…”

Novel amoxicillin nanoparticles formulated as sustained release delivery system for poultry use

“…It was observed that the release profile of nano amoxicillin in simulated gastrointestinal environment emerged in two stages: first as a rapid burst effect and, then as a relatively slow release. The rapid release (within 1.5 hr) is thought to be associated with the drug which is absorbed or weakly bound to the surface area of the nps, while the slow release is thought to be associated with the release of the remaining portion of the drug that mostly trapped in the nps (Parsian et al., ; Sun et al., ). Although the results of in vitro drug release studies were evaluated within a limited period (24 hr), it was determined that amoxicillin nps has a relatively low (~2.5‐fold) initial burst release rate compared to free amoxicillin and its total cumulative release rate is 51.96% in 24 hr.…”

Development and characterization of polymeric-based nanoparticles for sustained release of amoxicillin – an antimicrobial drug

“…A possible explanation of this situation could be that the faster migration of the weakly localized or bound drug molecules on the surface of particles. The subsequent slow release is likely due to slower migration of the remaining drug entrapped in the inner region of the particles [43,44].…”