Folic acid-functionalized human serum albumin nanocapsules for targeted drug delivery to chronically activated macrophages

• Type: Article in International Scientific Journal
• Date: 2012

Authors

Rollett, A (Author) Other; Reiter, T (Author) Other; Nogueira, P (Author) Other; Cardinale, M (Author) Other; Loureiro, A (Author) Other; Gomes, A (Author) Other; Cavaco Paulo, A (Author) Other; Moreira, A (Author) REIT; Alexandre Carmo (Author) ICBAS; Guebitz, GM (Author) Other

Journal

Title: International Journal of Pharmaceutics

Vol. 427

Pages: 460-466

ISSN: 0378-5173

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 47 Citations

Scopus - 15 Citations

Other information

Authenticus ID: P-002-A48

DOI: 10.1016/j.ijpharm.2012.02.028

Abstract (EN): Activated synovial macrophages play a key role in Rheumatoid Arthritis (RA). Recent studies have shown that folate receptor beta (FR beta) 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 FR beta-positive and FR beta-negative macrophages, obtained from human peripheral blood mononuclear cells, was demonstrated by flow cytometry. FR beta-expressing macrophages showed an increased binding for FA-modified capsules compared with those without FA.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 7