Journal
NANOMEDICINE
Volume 6, Issue 6, Pages 1011-1026Publisher
FUTURE MEDICINE LTD
DOI: 10.2217/NNM.11.25
Keywords
brain microvascular endothelial cell; nanoparticle; nevirapine; permeability; poly(lactide-co-glycolide); transferrin
Funding
- National Science Council of the Republic of China
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Aims: 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-alpha 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. Conclusion: Tf/NVP-PLGA NPs are efficacious carriers in targeting delivery across HBMECs for viral therapy.
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