title: Ethyl oleate-containing nanostructured lipid carriers improve oral bioavailability of trans-ferulic acid ascompared with conventional solid lipid nanoparticles.
abstract: trans-Ferulic acid (TFA) has antioxidative, anti-inflammatory, and cardioprotective effects, but its poor solubility in water results in unsatisfactory oral bioavailability when administered conventionally at a standard dosage. However, the limited bioavailability of TFA can be overcome by delivering it in nanostructured lipid carriers (NLCs). In this study, a microemulsion (ME)-based method was used to prepare NLCs with ethyl oleate as the liquid lipid component and glyceryl behenate as the solid lipid component. These NLCs and solid lipid nanoparticles (SLNs) were then used as vehicles for TFA. Their entrapment efficiencies (EE), stability during storage, in vitro release profiles, and in vivo pharmacokinetics were compared. The NLC formulation afforded a drug entrapment efficiency that was significantly greater than that of the SLN formulation, which was made using a single solid lipid. Furthermore, the TFA that was dispersed in the disordered binary lipid matrix of the NLC formulation was more stable than that in the SLN formulation, and thus showed less expulsion from the vehicle during storage. In in vivo pharmacokinetic studies, the NLC TFA formulation yielded a greater Cmax and AUC than that produced by the SLN formulation and an aqueous TFA suspension. This showed that the oral bioavailability of TFA was markedly improved by packaging in NLCs. NLCs are thus a promising vehicle for oral TFA administration, with significant advantages over SLNs.
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Yongtai
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Zhe
authors.initials: Z
authors.lastname: Li
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Gang
authors.initials: G
authors.lastname: Yang
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Zhi
authors.initials: Z
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Jihui
authors.initials: J
authors.lastname: Zhao
authors.affiliation: Anhui University of Chinese Medicine, Hefei 230012, China.
authors.forename: Rongfeng
authors.initials: R
authors.lastname: Hu
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. Electronic address: npfeng@hotmail.com.
authors.forename: Nianping
authors.initials: N
authors.lastname: Feng
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D003373:Coumaric Acids / Q000008:administration & dosage / Q000378:metabolism*; D004337:Drug Carriers / Q000008:administration & dosage / Q000378:metabolism*; D041981:Gastrointestinal Tract / Q000187:drug effects / Q000378:metabolism; D008055:Lipids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage / Q000378:metabolism*; D049329:Nanostructures / Q000008:administration & dosage; D009829:Oleic Acids / Q000008:administration & dosage / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D003373:Coumaric Acids; D004337:Drug Carriers; D008055:Lipids; D009829:Oleic Acids; C004999:ferulic acid; C033180:ethyl oleate
keywords: Lipid nanoparticles; Microemulsion; Nanocarrier; Pharmacokinetics; Sustained release