title: Enhanced bioavailability of tripterine through lipid nanoparticles using broccoli-derived lipids as a carrier material.
abstract: Chemotherapy via the oral route remains a considerable challenge due to poor water-solubility and permeability of anticancer agents. This study aimed to construct lipid nanoparticles using broccoli-derived lipids for oral delivery of tripterine (Tri), a natural anticancer candidate, and to enhance its oral bioavailability. Tri-loaded broccoli lipid nanoparticles (Tri-BLNs) were prepared by a solvent-diffusion method. The resulting Tri-BLNs were 75±10 nm in particle size with entrapment efficiency over 98%. In vitro release study indicated that Tri was almost not released from Tri-BLNs (<2%), whereas the lipolytic experiment showed that Tri-BLNs possessed a relatively strong anti-enzymatic degradation ability to Tri-CLNs (Tri-loaded common lipid nanoparticles). In situ single-pass intestinal perfusion manifested that the effective permeability of Tri-BLNs were significantly higher than that of Tri-CLNs. Further, Tri-BLNs exhibited more efficient cellular uptake in MDCK-II cells as evidenced by flow cytometry and confocal microscopy. The relative bioavailability of Tri-BLNs and Tri-CLNs was 494.13% and 281.95% compared with Tri suspensions, respectively. Depending on the ability in enhancement of biomembrane permeability, broccoli-derived lipids as an alternative source should be useful to construct lipid nanoparticles for bettering oral delivery of drugs with low bioavailability.
authors.affiliation: Division of Pharmaceutics, College of Pharmacy, Jinan University, 601 West Huangpu Avenue, Guangzhou 510632, PR China.
authors.forename: Wan
authors.initials: W
authors.lastname: Li
authors.affiliation: Division of Pharmaceutics, College of Pharmacy, Jinan University, 601 West Huangpu Avenue, Guangzhou 510632, PR China.
authors.forename: Tianpeng
authors.initials: T
authors.lastname: Zhang
authors.affiliation: Division of Pharmaceutics, College of Pharmacy, Jinan University, 601 West Huangpu Avenue, Guangzhou 510632, PR China.
authors.forename: Yanghuan
authors.initials: Y
authors.lastname: Ye
authors.affiliation: Division of Pharmaceutics, College of Pharmacy, Jinan University, 601 West Huangpu Avenue, Guangzhou 510632, PR China. Electronic address: pharmazxw@gmail.com.
authors.forename: Xingwang
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Division of Pharmaceutics, College of Pharmacy, Jinan University, 601 West Huangpu Avenue, Guangzhou 510632, PR China. Electronic address: bj.wu@hotmail.com.
authors.forename: Baojian
authors.initials: B
authors.lastname: Wu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D001937:Brassica / Q000737:chemistry*; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D065546:Drug Liberation; D007413:Intestinal Mucosa / Q000378:metabolism; D008055:Lipids / Q000737:chemistry* / Q000302:isolation & purification / Q000493:pharmacokinetics; D008066:Lipolysis; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D010316:Particle Size; D053978:Pentacyclic Triterpenes; D010539:Permeability; D051381:Rats; D012995:Solubility; D014315:Triterpenes / Q000008:administration & dosage* / Q000493:pharmacokinetics*
chemical_list: D004337:Drug Carriers; D008055:Lipids; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; C050414:celastrol
keywords: Bioavailability; Broccoli; Lipid nanoparticles; Permeability; Tripterine