Formulation optimization and in situ absorption in rat intestinal tract of quercetin-loaded microemulsion.
A new microemulsion system has been developed to increase the solubility and oral absorption of quercetin, a poorly water-soluble drug. The formulation of quercetin-loaded microemulsion was optimized by a simplex lattice experiment design. The optimized microemulsion formulation consisted of oil (7%, w/w), surfactant (48%, w/w), and cosurfactant (45%, w/w). Under this condition, the mean droplet diameter of microemulsion was 38.9 nm and solubility of quercetin in the microemulsion was 4.138 mg/ml. The in situ absorption property of quercetin-loaded microemulsion in rat intestine was studied and the results showed there was significant difference in absorption parameters such as K(a), t(1/2) and uptake percentages between microemulsion and micelle solution containing quercetin. The study on absorption percentage in different regions of rat intestine attested that the colon had the best permeability, followed by ileum, duodenum in order. It can be concluded that microemulsion can improve the solubility and oral absorption of quercetin, a poorly water-soluble drug.
Gao
Yan
Y
Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, China.
Wang
Yuqiang
Y
Ma
Yukun
Y
Yu
Aihua
A
Cai
Fengqun
F
Shao
Wei
W
Zhai
Guangxi
G
D000284:Administration, Oral; D000818:Animals; D002626:Chemistry, Pharmaceutical; D004655:Emulsions; D007408:Intestinal Absorption / Q000502:physiology*; D008297:Male; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D010477:Perfusion; D011794:Quercetin / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility / Q000187:drug effects; D012996:Solutions
D004655:Emulsions; D008823:Micelles; D012996:Solutions; D011794:Quercetin