Preparation, characterization, and evaluation of liposomal ferulic acid in vitro and in vivo.
In the present study, various gradients were evaluated for efficient loading of weak acid into liposomes. Several salt gradients showed efficient loading of ferulic acid (FA) into liposomes and the optimized conditions were established in calcium acetate gradient method to obtain 80.2 +/- 5.2% entrapment efficiency (EE). Unilamellar vesicles were observed in micrographs and liposomal FA showed good stability. 80% of FA was released from liposomes within 5 h in vitro. There is a novel finding in this study: that drugs could be entrapped with a high solubility in the intraliposomal buffer in contrast to the low solubility in the extraliposomal buffer. The results of body distribution in rats indicated that liposomes could improve the body distribution of FA. For FA liposome, the concentration of FA in brain was two-fold higher than that of free FA. Liposomal FA was a promising approach to improve the body distribution of FA.
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
Jing
J
Qin
DaWei
D
Chen
WeiGen
W
Lu
Huan
H
Xu
ChenYun
C
Yan
HaiYang
H
Hu
BaoYu
B
Chen
MingXi
M
Qiao
XiuLi
X
Zhao
D000085:Acetates / Q000737:chemistry; D000818:Animals; D001921:Brain / Q000378:metabolism; D017610:Calcium Compounds / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D003373:Coumaric Acids / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D004339:Drug Compounding; D004355:Drug Stability; D008081:Liposomes; D008297:Male; D010713:Phosphatidylcholines / Q000737:chemistry / Q000302:isolation & purification; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013025:Glycine max / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet; D014018:Tissue Distribution
D000085:Acetates; D017610:Calcium Compounds; D003373:Coumaric Acids; D008081:Liposomes; D010713:Phosphatidylcholines; C004999:ferulic acid; C120662:calcium acetate