Please use this identifier to cite or link to this item: https://ir.swu.ac.th/jspui/handle/123456789/11970
ชื่อเรื่อง: Anti-angiogenesis by dual action of R5K peptide conjugated itraconazole nanoparticles
ผู้แต่ง: Chittasupho C.
Kengtrong K.
Chalermnithiwong S.
Sarisuta N.
Keywords: arginylarginyllysylarginylarginylarginine
hexapeptide
hyaluronic acid
itraconazole
nanoparticle
polyglactin
unclassified drug
vasculotropin
angiogenesis inhibitor
cytochrome P450 3A inhibitor
itraconazole
peptide fragment
vasculotropin A
antiangiogenic activity
Article
cell migration
cell proliferation
cell viability
dispersity
drug bioavailability
drug delivery system
drug release
human
human cell
IC50
particle size
priority journal
signal transduction
temperature
vascular endothelial cell
zeta potential
cell survival
dose response
drug effect
metabolism
physiology
umbilical vein endothelial cell
visual acuity
wet macular degeneration
Angiogenesis Inhibitors
Cell Survival
Cytochrome P-450 CYP3A Inhibitors
Dose-Response Relationship, Drug
Human Umbilical Vein Endothelial Cells
Humans
Itraconazole
Nanoparticles
Peptide Fragments
Vascular Endothelial Growth Factor A
Visual Acuity
Wet Macular Degeneration
วันที่เผยแพร่: 2020
บทคัดย่อ: Neovascular age-related macular degeneration (AMD) is a leading cause of central vision loss and irreversible blindness. Vascular endothelial growth factor (VEGF) plays an important role in neovascularization under the retina and macula by promoting endothelial cell proliferation, migration, and angiogenesis. Although anti-VEGF drugs have shown their efficacy in visual improvement, long-term use of these drugs leads to ocular and systemic complications due to the non-selectivity of the drug. In this study, the dual-mode anti-angiogenic drug delivery system, which potentially inhibited VEGF in two different ways, was developed. The itraconazole encapsulated nanoparticles, conjugated with R5K peptide, were fabricated to allow multivalent binding interactions with VEGF. The R5K peptide blocked VEGF binding to its receptor, while itraconazole altered the signaling pathway of VEGF stimulation. The dual action of this novel drug delivery system aimed to enhance the anti-angiogenic effects of individual drugs. R5K-ITZ-NPs demonstrated potent, cell-type specific, and dose-dependent inhibition of vascular endothelial cell proliferation, migration, and tube formation in response to VEGF stimulation. The physical stability study showed that R5K-ITZ-NPs were stable when stored at 4 °C. However, the drug remaining in R5K-ITZ-NPs when stored at 4 °C for 28 days were only 17.2%. The chemical stability test revealed that the degradation of R5K-ITZ-NPs followed second-order kinetics. The release profile showed the burst release of ITZ followed by sustained release of the drug This novel drug delivery system may be an option for neovascular AMD patients who are resistant to ITZ and may represent a novel therapy for AMD. © 2020, American Association of Pharmaceutical Scientists.
URI: https://ir.swu.ac.th/jspui/handle/123456789/11970
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85078246456&doi=10.1208%2fs12249-019-1568-8&partnerID=40&md5=00b1886bbab77ef0cb61d81cace0439d
ISSN: 15309932
Appears in Collections:Scopus 1983-2021

Files in This Item:
There are no files associated with this item.


Items in SWU repository are protected by copyright, with all rights reserved, unless otherwise indicated.