Journal
PHARMACEUTICAL RESEARCH
Volume 36, Issue 7, Pages -Publisher
SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-019-2609-4
Keywords
L-selectin; peripheral blood neutrophils; rheumatoid arthritis; rheumatoid arthritis-targeting treatment; sialic acid-cholesterol conjugate
Funding
- National Natural Science Foundation of China [81703456, 81373334]
- Student's Platform for Innovation and Entrepreneurship Training Program [201810163012]
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PurposeThe aim of this research was to design dexamethasone palmitate (DP) loaded sialic acid modified liposomes, with the eventual goal of using peripheral blood neutrophils (PBNs) that carried drug-loaded liposomes to improve the therapeutic capacity for rheumatoid arthritis (RA).MethodsA sialic acid - cholesterol conjugate (SA-CH) was synthesized and anchored on the surface of liposomal dexamethasone palmitate (DP-SAL). The physicochemical characteristics and in vitro cytotoxicity of liposomes were evaluated. Flow cytometry and confocal laser scanning microscopy were utilized to investigate the accumulation of liposomes in PBNs. The adjuvant-induced arthritis was adopted to investigate the targeting ability and anti-inflammatory effect of DP loaded liposomes.ResultsBoth DP-CL and DP-SAL existed an average size less than 200nm with remarkably high encapsulation efficiencies more than 90%. In vitro and in vivo experiments manifested SA-modified liposomes provided a reinforced accumulation of DP in PBNs. As well, DP-SAL displayed a greater degree of accumulation in the joints and a stronger anti-inflammatory effect in terms of RA suppression.ConclusionsSA-modified liposomal DP was a promising candidate for RA-targeting treatment through the neutrophil-mediated drug delivery system.
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