title: In vivo evaluation of curcumin loaded nanosuspensions by oral administration.
abstract: The current study was aimed at preparing the curcumin nanosuspension (CUR-NS) to improve the solubility and oral absorption of CUR. Prepared from a tandem of ultra-turrax homogenization and high pressure homogenization, the CUR-NS showed spherical shape under transmission electron microscopy with an average diameter of 210.2 nm. The absorption of CUR-NS in the gastrointestinal (GI) tract was studied in rats using an in situ single pass perfusion method. It was found that the absorption percentage in stomach was 9.20% within 2 h. The absorption process in intestine was first-process with passive diffusion mechanism, and the main absorptive segments were proven to be in the duodenum and jejunum. A pharmacokinetic study was conducted in mice after oral administration of CUR at 250 mg/kg in the form of either CUR-NS or CUR suspension. The plasma concentration-time curves were both fitted to a one-compartment model and the relative bioavailability of CUR-NS to CUR suspension was 680.03%. The effects of CUR-NS on the structural properties of the intestinal mucosal membrane of rats were investigated by fluorescence polarization and circular dichroism in vitro. After treatment with CUR-NS, not only the fluidity of intestinal mucosal membrane increased but also the conformation of the membrane protein loosed, which increased the gastrointestinal absorption of CUR-NS. These studies provided the evidence that NS was valuable as an oral delivery carrier to enhance the absorption of CUR.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University Jinan 250012, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Gao
authors.forename: Chao
authors.initials: C
authors.lastname: Wang
authors.forename: Min
authors.initials: M
authors.lastname: Sun
authors.forename: Xin
authors.initials: X
authors.lastname: Wang
authors.forename: Aihua
authors.initials: A
authors.lastname: Yu
authors.forename: Aiguo
authors.initials: A
authors.lastname: Li
authors.forename: Guangxi
authors.initials: G
authors.lastname: Zhai
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D005753:Gastric Mucosa / Q000378:metabolism; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000187:drug effects / Q000378:metabolism; D007422:Intestines / Q000187:drug effects; D008297:Male; D051379:Mice; D054118:Nanospheres / Q000008:administration & dosage* / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D013270:Stomach / Q000187:drug effects
chemical_list: D003474:Curcumin