Recently, the layer-by-layer (LbL) self-assembly technology has attracted the enormous interest of researchers in synthesizing various pharmaceutical dosage forms. Herewith, we designed a biocompatible drug delivery system containing the calcium carbonate microparticles (CaCO MPs) that coated with the alternatively charged polyelectrolytes, i.e., poly-L-ornithine (PLO)/fucoidan by LbL self-assembly process (LbL MPs). Upon coating with the polyelectrolytes, the mean particle size of MPs obtained from SEM observations increased from 1.91 to 2.03 μm, and the surface of LbL MPs was smoothened compared to naked CaCO MPs. In addition, the reversible zeta potential changes have confirmed the accomplishment of layer upon a layer assembly. To evaluate the efficiency of cancer therapeutics, we loaded doxorubicin (Dox) in the LbL MPs, which resulted in high (69.7%) drug encapsulation efficiency. The controlled release of Dox resulted in the significant antiproliferative efficiency in breast cancer cell line (MCF-7 cells), demonstrating the potential of applying this innovative drug delivery system in the biomedical field.
Layer-by-Layer (LbL) self-assembly of nanocarriers has garnered the interest of researchers for a wide variety of biomedical applications. In this study, we demonstrated the preparation of poly(lactide-coglycolide) (PLGA)-(poly-L-ornithine (PLO)/fucoidan) 4 core-shell nanoparticles (LbL NPs) by a LbL-based self-assembly process, which possessed a mean size of 170 nm. In LbL NPs, a drug carrying PLGA nanocore is coated with alternating PLO and sulfated polysaccharide fucoidan composite films as a shell on the surface. The anti-tumor drug doxorubicin (DOX) loaded into the PLGA core, resulted in better encapsulation efficiency and its in vitro release from LbL NPs demonstrates that this core-shell strategy takes an advantage of its ability to hold the drug cargo and exhibit controlled release. Further, in vitro cell uptake studies by confocal laser scanning microscopy (CLSM) examination in breast tumor cells (MCF-7 cell line) have confirmed that the nanocarriers are successfully internalized and outlined their presence in the cytoplasm after 4 h of incubation. These intracellularly delivered DOX-loaded LbL NPs exhibited significant anti-tumor activity against breast tumor cells. This innovative chemotherapeutic design taking above advantages of successful internalization along with controlled release property signifies as a promising interventional therapeutic delivery system.
Layer-by-layer (LbL) self-assembly is the technology used in intermolecular static electricity, hydrogen bonds, covalent bonds and other polymer interactions during film assembling. This technology has been widely studied in the drug carrier field. Given their use in drug delivery systems, the biocompatibility of these potential compounds should be addressed. In this work, the primary biocompatibility of poly(lactide-co-glycolide)-(poly-L-orithine/fucoidan) [PLGA-(PLO/fucoidan)] core–shell nanoparticles (NPs) was investigated. Atomic force microscopy revealed the PLGA-(PLO/Fucoidan)4 NPs to be spherical, with a uniform size distribution and a smooth surface, and the NPs were stable in physiological saline. The residual amount of methylene chloride was further determined by headspace gas chromatography, in which the organic solvent can be volatilized during preparation. Furthermore, cell viability, acridine orange/ethidium bromide staining, haemolysis and mouse systemic toxicity were all assessed to show that PLGA-(PLO/fucoidan)4 NPs were biocompatible with cells and mice. Therefore, these NPs are expected to have potential applications in future drug delivery systems.
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