Bulletin of the National Research Centre (Aug 2022)
Enhancing cellular uptake and membrane permeability of gallic acid for breast cancer therapy via folate-tagged PEGylated iron oxide nanoparticles has theronastic agent
Abstract
Abstract Background In an attempt to prove biological activity enhancement upon escalating the cellular uptake response through ligand and carrier-based via nanoframework, gallic acid was chosen to be formulated into PLGA-based polymeric nanoparticles with iron oxide as the theranostic agent. Results The pre-formulation studies like FTIR, DSC, XRD, and TGA were carried out, which implies good compatibility between drug and polymer. Furthermore, the nanoparticles were prepared by using a single nanoprecipitation method, and the prepared nanoparticles were optimized using the Box–Behnken design. This design was used to optimize the gallic acid-loaded PEGylated nanoparticles by considering the effects of three factors (X 1; lipid, X 2; PLGA, and X 3; drug) on the response variables Y 1 (EE), Y 2 (size), and Y 3 (drug release). The findings of surface response plots are attributed to an optimized nanoparticle. The in vitro drug release followed a biphasic release profile in both tested media, pH 4.8 and 7.4. The desirable physicochemical characteristics involved small particle size with considerable stability, which was attained due to the anionic nature of PLGA. The in vitro cytotoxicity assay of gallic acid, GA/PLGA-IONPs, and optimized FA-GA/PLGA-PEGylated-LIONPs were evaluated using the MTT assay, which showed an inhibition effect on MCF-7 cells to induce apoptosis. Cellular uptake and fluorescence studies show higher cellular uptake and destruction of cells based on concentration dependence. Conclusions The above results show that prepared nanoparticles sustain the therapeutic concentration of the drug on target cells by enhancing permeability through the PEGylated lipid delivery system.
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