Nuclear chemistry

Nanoparticle

Biotechnology

Biology

Pharmacokinetics

Materials science

Chromatography

Paeonol

Jejunum

Chitosan

Biochemistry

Particle size

Bioavailability

Physical chemistry

Drug delivery

Alternative medicine

In vivo

Drug carrier

Nanotechnology

Organic chemistry

In vitro

Pharmacology

Zeta potential

Mucoadhesion

Medicine

Chemistry

PLGA

Pathology

International Journal of Pharmaceutics

Herein, we report a novel type of NPs by loading paeonol (Pae) into PLGA NPs, to enhance drug stability and oral bioavailability. The paeonol (Pae)-loaded polylactic-co-Gly-colic acid (PLGA) nanoparticles (Pae-PLGA-NPs) were prepared by nanoprecipitation method. The resultant NPs were in spherical shape with an average particle size around 237.7 ± 4.92 nm, and the PDI and zeta potential were 0.110 ± 0.01 and −25.33 ± 1.37 mV, respectively. The encapsulation efficiency (EE) and drug loading (DL) of the Pae-PLGA-NPs were 86.26 ± 1.12 and 12.74 ± 0.37% respectively. The in vitro drug release, in vivo pharmacokinetics and in situ single-pass intestinal perfusion (SPIPs) of Pae-PLGA-NPs was investigated. In vivo, the AUC(0-t), C max, MRT(0-t), and T1/2z of the Pae-PLGA-NPs group were 3.79-, 1.89-, 1.40- and 1.49-fold greater than those of the Pae suspension group, respectively. The in situ single-pass intestinal perfusion of NPs results showed the Ka values in the duodenum, jejunum, ileum and colon were 1.12-, 1.40-, 1.52- and 2.21-fold higher than those of Pae solution, respectively. Moreover, the Papp values of the ileum and colon were 1.27- and 1.31-fold higher than those of the solution group. Such findings suggested the Pae-PLGA-NPs can significantly improve the intestinal absorption characteristics, and have a beneficial effect on oral administration as a nanometer-sized carrier.

Paeonol-loaded PLGA nanoparticles as an oral drug delivery system: Design, optimization and evaluation