Layer-by-layer assembly of hyaluronic acid/carboxymethylchitosan polyelectrolytes on the surface of aminated mesoporous silica for the oral delivery of 5-fluorouracil

Abstract

The aim of the present work is to develop the polyelectrolyte complexes (PEc) coated on the surface of aminated mesoporous silica nanoparticles (AMSN) through layer by layer (LbL) assembly for the controlled delivery of 5-fluorouracil (5-FU). The polyelectrolyte complexes coated aminated mesoporous silica nanoparticles were characterized by FTIR, XRD, DLS, SEM, TEM and NMR. The optimum pH value for the encapsulation of 5-FU into AMSN-HA/CMC (AMSN-PEc) was found to be 5.4. The controlled release behavior of 5-FU was examined with two different pHs at 1.2 and 7.4. The release rate of the loaded drug molecules was high and controlled level at stimulated intestinal pH 7.4 but decreased considerably at gastric pH 1.2. Release data were fitted to empirical equations to understand the nature of drug release profiles. The drug release profile followed Korsemeyer-Peppas model. The cytotoxicity of 5-FU loaded (AMSN-PEc) towards HT-29 and L929 cells was investigated. The results showed that 5-FU loaded AMSN-PEc retained significant antitumor activities. This study demonstrated that the prepared drug delivery system (DDS) has potential application as a drug carrier. The intracellular uptake of the drug loaded drug delivery system was confirmed by Confocal Raman microscopy.