title: Solid lipid nanoparticles for sustained pulmonary delivery of Yuxingcao essential oil: Preparation, characterization and in vivo evaluation.
abstract: The objective of this study was to prepare solid lipid nanoparticles (SLNs) for sustained pulmonary delivery of Yuxingcao essential oil (YEO). Three YEO loaded SLNs (SLN-200, SLN-400 and SLN-800) with different particle size were prepared and separated following a high-shear homogenization technique using Compritol 888 ATO as lipid and polyvinyl alcohol as an emulsifier. The particle size, zeta potential, drug encapsulation efficiency and drug loading of the SLNs were determined to be between 171 and 812nm, -17.1 and -19.3mV, between 76.6 and 90.2% and between 2.34 and 3.12%, respectively whereas the in vitro release data showed that the SLNs led to sustained drug release up to 48h. In addition, the SLN suspensions after nebulization conferred the fine particle fractions (<5.4μm) of 67.4-75.8%. Following intratracheal administration to rats, YEO loaded SLNs not only prolonged pulmonary retention up to 24h, but also increased AUC values (15.4, 18.2 and 26.3μg/gh for SLN-200, SLN-400 and SLN-800, respectively) by 4.5-7.7 folds compared to the intratracheally dosed YEO solution and by 257-438 folds to the intravenously dosed YEO solution, respectively. The present results were the first to show that YEO loaded SLNs may sustain YEO inhalation delivery and improve local bioavailability, representing a promising inhalable carrier to attain once daily application.
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, China.
authors.forename: Yun
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, China.
authors.forename: Yue-Xing
authors.initials: YX
authors.lastname: Chang
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Hu
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, China.
authors.forename: Chun-Yu
authors.initials: CY
authors.lastname: Liu
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, China.
authors.forename: Li-Hui
authors.initials: LH
authors.lastname: Quan
authors.affiliation: Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, China. Electronic address: yhliao@implad.ac.cn.
authors.forename: Yong-Hong
authors.initials: YH
authors.lastname: Liao
mesh_terms: D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage* / Q000493:pharmacokinetics; D005227:Fatty Acids / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008168:Lung / Q000378:metabolism; D008297:Male; D053758:Nanoparticles; D009822:Oils, Volatile / Q000008:administration & dosage* / Q000493:pharmacokinetics; D010316:Particle Size; D011142:Polyvinyl Alcohol / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D013997:Time Factors; D014018:Tissue Distribution
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; D005227:Fatty Acids; D008055:Lipids; D009822:Oils, Volatile; C086409:glyceryl behenate; D011142:Polyvinyl Alcohol
keywords: Pulmonary delivery; Pulmonary retention; Solid lipid nanoparticles; Sustained release; Traditional Chinese medicine; Yuxingcao essential oil