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In vitro characterization of a dual‐receptor targeted drug delivery system for treating vascular diseases
Author(s) -
Lamberti Giuseppina,
Wu Fan,
Kiani Mohammad F.,
Wang Bin
Publication year - 2011
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.25.1_supplement.lb441
Subject(s) - selectin , microsphere , drug delivery , adhesion , in vitro , biomedical engineering , receptor , drug , biophysics , chemistry , targeted drug delivery , materials science , pharmacology , nanotechnology , medicine , biochemistry , chemical engineering , biology , composite material , engineering
Drug delivery systems targeted to the vasculature provide an effective mean for increasing the therapeutic efficacy of various drugs. In this study we present a novel dual‐receptor (selectins and ICAMs) targeting approach to enhance the drug carrier's binding efficiency to the inflamed tissue in vascular diseases. Methods Florescent microspheres were prepared by coating the surface with different ratios of antibodies against ICAM‐1 (aICAM‐1) and E‐selectin (aE‐selectin). A flow chamber was used to study the interaction of the microspheres with TNF‐α activated HUVEC under different shear flow conditions. Results Microspheres coated with 2:1 ratio of aICAM‐1 and aE‐selectin had the highest binding efficacy compared to the single antibody coated microspheres. The number of aICAM‐1+aE‐selectin microspheres bound to HUVECs appeared to decrease with increase in wall shear stress in the flow chamber. Moreover, the number of adherent aICAM‐1+aE‐selectin microspheres was significantly higher than the adherent aE‐selectin microspheres under different flow conditions. Conclusions We conclude that the adhesion efficiency of the two‐receptor targeting microspheres is significantly higher than the single‐ligand microspheres under various flow conditions and that the drug carrier adhesion ability can be optimized by optimizing the ratio of the two ligands on the surface of the microsphere.

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