title: Optimised nano-formulation on the bioavailability of hydrophobic polyphenol, curcumin, in freely-moving rats.
abstract: This study has optimised the poly lactic-co-glycolic acid (PLGA) nano-formulation of curcumin to prolong its retention time in the body and improve bioavailability. High-pressure emulsification-solvent-evaporation was designed to obtain curcumin-loaded PLGA nanoparticles (C-NPs) prepared with 2% of PVA containing 20% sucrose as aqueous phase and dichloromethane as oil phase. The size and entrapment efficiency of C-NPs was 158±10nm and 46.6±13.5%, respectively. The stable storage time of C-NPs was one month at 4°C. When curcumin was formulated, a significant increase of curcumin exposure in rat plasma was revealed from the intravenous study (AUC/Dose raised 55%) and the oral study (AUC/Dose increased 21-fold). The oral bioavailability of curcumin at C-NPs was 22-fold higher than conventional curcumin. Excretion results support oral study that absorption of curcumin was significantly increased by nano-formulation. These findings demonstrate that PLGA nano-formulation could potentially be applied to increase bioavailability of hydrophobic polyphenols.
authors.affiliation: Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei 112, Taiwan.
authors.forename: Yin-Meng
authors.initials: YM
authors.lastname: Tsai
authors.affiliation: Department of Nursing, Mackay Medicine, Nursing and Management College, Taiwan.
authors.forename: Woan-Ching
authors.initials: WC
authors.lastname: Jan
authors.affiliation: Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei 112, Taiwan.
authors.forename: Chao-Feng
authors.initials: CF
authors.lastname: Chien
authors.affiliation: Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei 112, Taiwan.
authors.forename: Wen-Chuan
authors.initials: WC
authors.lastname: Lee
authors.affiliation: Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei 112, Taiwan; National Research Institute of Chinese Medicine, Taipei, Taiwan.
authors.forename: Lie-Chwen
authors.initials: LC
authors.lastname: Lin
authors.affiliation: Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei 112, Taiwan; Graduate Institute of Acupuncture Science, China Medical University, Taichung, Taiwan; Department of Education and Research, Taipei City Hospital, Taipei, Taiwan. Electronic address: thtsai@ym.edu.tw.
authors.forename: Tung-Hu
authors.initials: TH
authors.lastname: Tsai
keywords: Curcumin; Herbal medicine; Nanoparticles; Oral bioavailability; PLGA; Pharmacokinetics