N-trimethyl chitosan (TMC)-modified microemulsions for improved oral bioavailability of puerarin: preparation and evaluation.
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) = 373 nm, I(3) = 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.
Department of Pharmacy, The Second Xiangya Hospital of Central South University , Changsha , China .
Dehua
D
Liao
Xinyi
X
Liu
Wei
W
Dai
Tiantian
T
Tang
Ge
G
Ou
Kai
K
Zhang
Meng
M
Han
Rongrong
R
Kang
Sufang
S
Yang
Daxiong
D
Xiang
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions; D007529:Isoflavones / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008297:Male; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D014665:Vasodilator Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics
D004337:Drug Carriers; D004655:Emulsions; D007529:Isoflavones; C118071:N-trimethyl chitosan chloride; D014665:Vasodilator Agents; D048271:Chitosan; C033607:puerarin
Bioavailability; microenvironment polarity; puerarin; puerarin TMC-modified microemulsions; puerarin microemulsions