title: Preparation and evaluation of lipid emulsified docetaxel-loaded nanoparticles.
abstract: OBJECTIVE
  Lipid emulsified nanoparticles (LPNPs) have been developed to load anticancer drug docetaxel (DTX) in this work.
  
  
  METHODS
  We evaluated DTX-loaded lipid emulsified nanoparticles (DTX-LPNPs) in vitro compared with the conventional nanoparticles (DTX-NPs). The newly developed formulation was compared with DTX-NPs in terms of physicochemical properties and in-vitro efficacy.
  
  
  RESULTS
  These two formulations had similar physicochemical properties in our results. And it has been proven that phosphatidylethanolamine had higher emulsification efficiency (20-fold of polyvinyl alcohol) in the same preparation procedure. The in-vitro release of DTX from DTX-LPNPs showed burst release initially and then followed by a sustained release, which prolonged the half time. The cytotoxicity test indicated that the DTX-LPNPs were more effective against tumour growth, and the IC50 of Duopafei, DTX-NPs and DTX-LPNPs for the inhibition of human lung cancer A549 cells at 48 h (n = 3) were found to be 3.53 ± 0.43, 1.15 ± 0.06 and 0.55 ± 0.08 μm, respectively. The evaluation of the cellular uptake showed that DTX-LPNPs improved the drug delivery into cytoplasm compared with the commercial product Duopafei and DTX-NPs.
  
  
  CONCLUSIONS
  DTX-LPNPs may be a promising formulation for cancer therapy.
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Minglu
authors.initials: M
authors.lastname: Chang
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Yanna
authors.initials: Y
authors.lastname: Yu
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Yongchun
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Guangpu
authors.initials: G
authors.lastname: Liu
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Ting
authors.initials: T
authors.lastname: Wei
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Tiantian
authors.initials: T
authors.lastname: Zuo
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Yuanyuan
authors.initials: Y
authors.lastname: Guan
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Guimei
authors.initials: G
authors.lastname: Lin
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Zhongxi
authors.initials: Z
authors.lastname: Zhao
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003593:Cytoplasm / Q000378:metabolism; D003692:Delayed-Action Preparations; D000077143:Docetaxel; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004655:Emulsions; D006801:Humans; D020128:Inhibitory Concentration 50; D008055:Lipids / Q000737:chemistry*; D008175:Lung Neoplasms / Q000188:drug therapy / Q000473:pathology; D053758:Nanoparticles; D043823:Taxoids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D043823:Taxoids; D000077143:Docetaxel
keywords: cell-cycle analysis; cellular uptake; docetaxel; drug delivery; lipid emulsified nanoparticles