期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 89, 期 -, 页码 18-29出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejpb.2014.11.016
关键词
CCR2 antagonist; Endothelium; Monocyte; Target-sensitive liposomes; Targeted drug delivery; VCAM-1
资金
- UEFISCDI (Executive Agency for Higher Education Research Development and Innovation Funding), Romania [4-001]
- VDI (The Association of German Engineers), Germany [FKZ 13N115437]
- Swiss National Science Foundation, Switzerland [31NM30-136033]
- European Commission [PN-II-ID-PCE-2011-3-0928, 143]
- ERDF
- European Social Fund [POSDRU/89/1.5/S/55216]
- Doctoral Fellowship Programme [POSDRU/107/1.5/S/82839, POSDRU/159/1.5/S/133391]
- Swiss National Science Foundation (SNF) [31NM30_136033] Funding Source: Swiss National Science Foundation (SNF)
Chemokines are critically involved in the development of chronic inflammatory-associated diseases such as atherosclerosis. We hypothesized that targeted delivery of compounds to the surface of activated endothelial cells (EC) interferes with chemokine/receptor interaction and thereby efficiently blocks inflammation. We developed PEGylated target-sensitive liposomes (TSL) encapsulating a CCR2 antagonist (Teijin compound 1) coupled with a specific peptide recognized by endothelial VCAM-1 (Vp-TSL-Tj). TSL were characterized for size (by dynamic light scattering), the amount of peptide coupled at the liposomal surface and Teijin release (by HPLC). We report that Vp-TSL-Tj binds specifically to activated EC in vitro and in situ, release the entrapped Teijin and prevent the transmigration of monocytes through activated EC. This is the first evidence that nanocarriers which transport and release chemokine inhibitors at specific pathological sites can reduce chemokine-dependent inflammatory processes. (C) 2014 Elsevier B.V. All rights reserved.
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