Hydrolyzed Galactomannan-Modified Nanoparticles and Flower-Like Polymeric Micelles for the Active Targeting of Rifampicin to Macrophages
Inhalable nanocarriers that are uptaken by macrophages represent an appealing approach for the targeting of antibiotics to the tuberculosis reservoir. In the present work, we report on the development of rifampicin (RIF)-loaded nanoparticles and flower-like polymeric micelles surface-modified
with hydrolyzed galatomannan (GalM-h), a polysaccharide of mannose and galactose, two sugars that are recognized by lectin-like receptors. Initially, pure or GalM-h-associated chitosan nanoparticles (NPs) were produced by ionotropic gelation. Despite the composition, NPs displayed positive
zeta potential values between +18.0 and +24.5 mV and a size ranging between 263 and 340 nm. In addition, RIF payloads were approximately 1.0% w/w. To increase the encapsulation efficiency, a more complex nanocarrier based on poly(ε-caprolactone)-b-poly(ethylene-glycol)-b-poly(epsilon-caprolactone)
flower-like polymeric micelles (PMs) coated with chitosan or GalM-h/chitosan were engineered. These polymeric micelles displayed a bimodal size distribution with a positive zeta potential between +6.7 and +8.1 mV. More importantly, the drug encapsulation capacity was increased 12.9-fold with
respect to the NPs. An agglutination assay with concanavalin A confirmed the presence of GalM-h on the surface. Qualitative uptake studies by fluorescence microscopy revealed that GalM-h-modified systems were taken-up by RAW 264.7 murine macrophages. Finally, the intracellular/cell associated
levels of RIF following the incubation of cells with free or encapsulated drug indicated that while chitosan hinders the uptake, GalM-h leads to a significant increase of the intracellular concentration.
Keywords: ACTIVE DRUG TARGETING TO MACROPHAGES; CHITOSAN NANOPARTICLES; FLOWER-LIKE POLYMERIC MICELLES; HYDROLYZED GALACTOMANNAN; RIFAMPICIN; TUBERCULOSIS
Document Type: Research Article
Publication date: 01 June 2013
- Journal of Biomedical Nanotechnology (JBN) is a peer-reviewed multidisciplinary journal providing broad coverage in all research areas focused on the applications of nanotechnology in medicine, drug delivery systems, infectious disease, biomedical sciences, biotechnology, and all other related fields of life sciences.
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