title: Lipids-based nanostructured lipid carriers (NLCs) for improved oral bioavailability of sirolimus.
abstract: The main purpose of this study was to improve the oral bioavailability of sirolimus (SRL), a poorly water-soluble immunosuppressant, by encapsulating into lipids-based nanostructured lipid carriers (NLCs). SRL-loaded NLCs (SRL-NLCs) were prepared by a high-pressure homogenization method with glycerol distearates (PRECIROL ATO-5) as the solid lipid, oleic acid as the liquid lipids, and Tween 80 as the emulsifier. The SRL-NLCs prepared under optimum conditions was spherical in shape with a mean particle size of about 108.3 nm and an entrapment efficiency of 99.81%. In vitro release of SRL-NLCs was very slow, about 2.15% at 12 h, while in vitro lipolysis test showed fast digestion of the NLCs within 1 h. Relative oral bioavailability of SRL-NLCs in Beagle dogs was 1.81-folds that of the commercial nanocrystalline sirolimus tablets Rapamune®. In conclusion, the NLCs show potential to improve the oral bioavailability of SRL.
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA , Shanghai , China and.
authors.forename: Qin
authors.initials: Q
authors.lastname: Yu
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA , Shanghai , China and.
authors.forename: Xiongwei
authors.initials: X
authors.lastname: Hu
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA , Shanghai , China and.
authors.forename: Yuhua
authors.initials: Y
authors.lastname: Ma
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA , Shanghai , China and.
authors.forename: Yunchang
authors.initials: Y
authors.lastname: Xie
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA , Shanghai , China and.
authors.forename: Yi
authors.initials: Y
authors.lastname: Lu
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA , Shanghai , China and.
authors.forename: Jianping
authors.initials: J
authors.lastname: Qi
authors.affiliation: b Department of Pharmacy , Shanghai Xuhui Dahua Hospital , Shanghai , China.
authors.forename: Li
authors.initials: L
authors.lastname: Xiang
authors.affiliation: b Department of Pharmacy , Shanghai Xuhui Dahua Hospital , Shanghai , China.
authors.forename: Fengqian
authors.initials: F
authors.lastname: Li
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA , Shanghai , China and.
authors.forename: Wei
authors.initials: W
authors.lastname: Wu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004285:Dogs; D004337:Drug Carriers / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D020123:Sirolimus / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D012995:Solubility
chemical_list: D004337:Drug Carriers; D008055:Lipids; D020123:Sirolimus
keywords: Drug delivery; nanoparticles; nanostructured lipid carriers; oral bioavailability; sirolimus