Please use this identifier to cite or link to this item: http://hdl.handle.net/1822/22655

TitleFolic acid-functionalized human serum albumin nanocapsules for targeted drug delivery to chronically activated macrophages
Author(s)Rollett, Alexandra
Reiter, Tamara
Nogueira, Patrícia
Cardinale, Massimiliano
Loureiro, Ana
Gomes, Andreia
Paulo, Artur Cavaco
Moreira, Alexandra
Carmo, Alexandre M.
Guebitz, G. M.
KeywordsTargeted;
Drug delivery
Albumin nanocapsules
Folate receptor
Macrophages
Issue date2012
PublisherElsevier
JournalInternational Journal of Pharmaceutics
Abstract(s)Activated synovial macrophages play a key role in Rheumatoid Arthritis (RA). Recent studies have shown that folate receptor beta (FRβ) is specifically expressed by activated macrophages. Therefore a folate-based nanodevice would provide the possibility of delivering therapeutic agents to activated macrophages without affecting normal cells and tissues. This study shows for the first time the sonochemical preparation of HSA nanocapsules avoiding toxic cross linking chemicals and emulsifiers used in other methods. Production of HSA nanocapsules was optimized leading to a diameter of 443.5 ± 9.0 nm and a narrow size distribution indicated by a polydispersity index (PDI) of 0.066 ± 0.080. Nanocapsules were surface modified with folic acid (FA) and the FA content was determined to be 0.38 and 6.42 molecules FA per molecule HSA, depending on the surplus of FA employed. Dynamic light scattering was used to determine size, PDI and zetapotential of the produced nanocapsules before and after surface modification. FA distribution on the surface of HSA nanocapsules was localized three-dimensionally after fluorescence labeling using confocal laser scanning microscopy (CLSM). Furthermore, specific binding and internalization of HSA nanocapsules by FRβ-positive and FRβ-negative macrophages, obtained from human peripheral blood mononuclear cells, was demonstrated by flow cytometry. FRβ-expressing macrophages showed an increased binding for FA-modified capsules compared with those without FA.
TypeArticle
URIhttp://hdl.handle.net/1822/22655
DOI10.1016/j.ijpharm.2012.02.028
ISSN0378-5173
Publisher versionhttp://dx.doi.org/10.1016/j.ijpharm.2012.02.028
Peer-Reviewedyes
AccessOpen access
Appears in Collections:DET/2C2T - Artigos em revistas internacionais com arbitragem científica

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