N-trimethyl chitosan (TMC)-modified microemulsions for improved oral bioavailability of puerarin: preparation and evaluation

Abstract

The aim of this research was to increase the oral bioavailability of puerarin by N-trimethyl chitosan-modified microemulsions (TMC-MEs) loaded with puerarin. Different concentrations of TMC-modified microemulsions were prepared in our study, and then evaluated for particle size, zeta potential, morphological observation and changes of the microenvironment polarity of inner oil core. It was shown that the zeta potential of the microemulsion was increased with the increasing concentration of TMC, and the peak value was achieved when the concentration of TMC was 3.0 mg/mL. The enhancement of the ratio of I 1 /I 3 (the ratio between the first band and the third band of the emission fluorescence spectrum of pyrene, I 1 ¼ 373 nm, I 3 ¼ 384 nm) indicated that polarity of the inner core of TMC-MEs was increased with the addition of the modifier. Pharmacokinetic studies demonstrated that after oral administration of puerarin N-trimethyl chitosan (TMC)-modified microemulsions (PUE-TMEs) and puerarin microemulsions (PUE-MEs) to rats at a dose of 100 mg/kg, relative bioavailability was enhanced about 6.8-and 1.2-fold, respectively, compared to puerarin suspension (PUE-SUS) as control. It indicated that the TMC-MEs could be used as an effective formulation for enhancing the oral bioavailability of puerarin.

Antiviral activity of puerarin as potent inhibitor of influenza virus neuraminidase

“…Puerarin has poor water solubility and intestinal permeability, which limits its clinical application. To prepare effective, strong, and long‐term preparations of puerarin with a high oral bioavailability, the structural and dosage form of puerarin can be improved via structural modification, microemulsion, nanoparticles, and other methods (Liao et al, 2015; Luo et al, 2011; Wu et al, 2018; Zhao et al, 2011).…”

Nano-traditional Chinese medicine: a promising strategy and its recent advances

“…Compared with free puerarin, 93 the bioavailability of puerarin MEs was significantly enhanced in treating neurodegenerative diseases and tumors. 94–98 They could also act as a transdermal drug delivery system to improve skin penetration. The total flavonoids of araceae were encapsulated into MEs and it was found that the transdermal flux of its two main active ingredients, schaftoside and isoschaftoside, was 3.72 times and 5.92 times higher than that of the aqueous suspension, respectively.…”

Pharmacokinetics and drug delivery systems for puerarin, a bioactive flavone from traditional Chinese medicine

“…Powerful absorption enhancing agents such as ethyl oleate (Yu et al., 2011; Tang et al., 2013) and N-trimethyl chitosan chloride (Liao et al., 2015) were added into the formulation, not only as the oil phase, but also improved the oral bioavailability of puerarin. When N-trimethyl chitosan chloride was added to the microemulsion formulation, the relative bioavailability was enhanced more than five times compared with control microemulsion (Liao et al., 2015). Through combining phospholipid complex technology and microemulsion, the relative oral bioavailability of puerarin phospholipid complex was 3.16-fold higher than puerarin(Wu et al., 2018).…”

“…Upon oral administration, puerarin-loaded microemulsions significantly improved the bioavailability of puerarin from 1.2-fold to 15.2-fold compared with corresponding puerarin control groups (Wu et al, 2009;Yu et al, 2011;Tang et al, 2013;Liao et al, 2015;. Powerful absorption enhancing agents such as ethyl oleate (Yu et al, 2011;Tang et al, 2013) and N-trimethyl chitosan chloride (Liao et al, 2015) were added into the formulation, not only as the oil phase, but also improved the oral bioavailability of puerarin. When N-trimethyl chitosan chloride was added to the microemulsion formulation, the relative bioavailability was enhanced more than five times compared with control microemulsion (Liao et al, 2015).…”