title: Targeting nevirapine delivery across human brain microvascular endothelial cells using transferrin-grafted poly(lactide-co-glycolide) nanoparticles.
abstract: OBJECTIVE
  Poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs) were grafted with transferrin (Tf) to enhance the transport of nevirapine (NVP) across human brain microvascular endothelial cells (HBMECs).
  
  
  METHODS
  NVP-loaded PLGA NPs with surface-grafting Tf (Tf/NVP-PLGA NPs) were incubated with HBMECs and immunochemical staining characterized Tf receptors (TfRs).
  
  
  RESULTS
  The polydispersity index of Tf/NVP-PLGA NPs was lower than 0.008. The entrapment efficiency of NVP and loading efficiency of Tf was 20-75% and 15-80%, respectively. Tf slightly retarded the release of NVP from PLGA. Dioctadecyldimethylammonium bromide (DODAB)-stabilized Tf/NVP-PLGA NPs reduced the viability of HBMECs to 70-75%. The secretion of TNF-α was inhibited by Tf and stimulated by DODAB. The permeability of NVP across HBMECs reached maxima at 67% DODAB and 0.1-0.2% Tf. An increase in the concentration of Tf enhanced the uptake of Tf/NVP-PLGA NPs via a TfR-mediated mechanism.
  
  
  CONCLUSIONS
  Tf/NVP-PLGA NPs are efficacious carriers in targeting delivery across HBMECs for viral therapy.
authors.affiliation: Department of Chemical Engineering, National Chung Cheng University, Chia-Yi, Taiwan 62102, Republic of China. chmyck@ccu.edu.tw
authors.forename: Yung-Chih
authors.initials: YC
authors.lastname: Kuo
authors.forename: Pei-I
authors.initials: PI
authors.lastname: Lin
authors.forename: Cheng-Chin
authors.initials: CC
authors.lastname: Wang
mesh_terms: D001921:Brain / Q000166:cytology*; D002460:Cell Line; D004337:Drug Carriers / Q000737:chemistry*; D042783:Endothelial Cells / Q000378:metabolism* / Q000648:ultrastructure; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D019829:Nevirapine; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D014168:Transferrin / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D014168:Transferrin; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D019829:Nevirapine