Eudragit encapsulated cationic poly (lactic-co-glycolic acid) nanoparticles in targeted delivery of capecitabine for augmented colon carcinoma therapy

The present study was aimed at developing capecitabine loaded poly(lactic-co-glycolic acid) (PLGA Cap) based nanoparticles (NPs) formulation as a biodegradable polymeric drug carrier to treat colon cancer. NPs were prepared by the double emulsion solvent evaporation technique, then surface modified using chitosan and encapsulated in Eudragit (R) S100. Full factorial design (FFD) matrix was used to study the influence of three different independent variables on the responses particle size, Zeta potential, and encapsulation efficiency. For that, a three-level factorial design experiment was used for obtaining a mathematical model and prediction of the optimized formulation. The optimized PLGA Cap NPs were analyzed using DSC, AFM and Raman chemical spectral mapping. The particle size was found to be 386.13 +/- 54.18 nm with polydispersity index 0.28 and Zeta potential of +12.3 +/- 2.1 mV with an encapsulation efficiency of 63.81 +/- 5.69%. In vitro drug release studies results showed a burst release followed by sustained release of Cap in the simulated colonic media with matrix-diffusion assisted drug release. The optimized NPs depicted higher in vitro mucoadhesion compared to the unmodified NPs. In vitro cell line studies showed that the PLGA Cap NPs exhibited significant anti-proliferative activity. The NPs were stable according to studies carried out following ICH Guidelines. All these outcomes signify the promising applicability of the formulated PLGA Cap NPs as a novel and targeted drug delivery system for colon carcinoma therapy with better patient compliance.