A promising targeting system to enrich irinotecan antitumor efficacy: Folic acid targeted nanoparticles

As folic acid receptors are overexpressed in various cancers including the colon, therefore, nanoparticles of folic acid-polyethylene glycol -poly lactic-co-glycolic acid were fabricated and loaded with irinotecan by emulsification/solvent evaporation technique to target the folic acid receptors in colorectal tumors. The chemical structure of synthesized polymer was examined by 1H NMR, and Box-Behnken design was utilized to determine the combined impact of independent variables for choosing the appropriate formulation. Dynamic light scattering, scanning electron microscope and differential scanning calorimetry (DSC) were utilized to scrutinize irinotecan in nanoparticles. The Box-Behnken design indicated a reasonable correlation between the predicted and experimented values which proves the efficiency of the selected statistical model. The optimized nanoparticles had an acceptable size and morphology. DSC analysis exhibited that irinotecan in nanoparticles is in an amorphous state. The optimized formulation exhibited a prolonged release profile. In addition, the higher drug release from nanoparticles in acidic pH indicates that they can be used to target the extracellular pH of the tumor. The activity of targeted nanoparticles against tumors was higher than the irinotecan and simple nanoparticles. Evaluation of folic acid decorated nanoparticles containing irinotecan confirmed their suitability for targeted delivery of irinotecan in folate positive cancers. © 2021 Elsevier B.V