Synthesis of core@shell nanoparticles functionalized with folic acid-modified PCL-co-PEGMA copolymer for methotrexate delivery

Abstract

Cancer is responsible for many fatalities and it is considered a public health problem. The side effects caused by conventional treatment are aggressive and painful to patients and can be reduced using nanomaterials that allows action in specific sites, making the cancer treatment more efficient, improving patient life's quality. Many kinds of nanoparticles that can be used, among these the block copolymer functionalized iron oxide nanoparticles stand out due to their simultaneous interaction with hydrophobic and hydrophilic drugs. The evaluation of these platforms properties allows optimizing their action in the human body, enhancing its biodistribution and targeting a specific region in the organism. The encapsulation efficiency and the controlled release profile is strictly dependent on the size, morphology, and interactions of the copolymer blocks. In this work, it was studied the synthesis of a hybrid nanoplatform composed of an inorganic core (iron oxide) and a polymeric shell (PCL-co-PEGMA block copolymer modified with folic acid). FTIR and 1H NMR allowed the confirmation of the nanoplatform synthesis. Particles around 180 nm stable at physiological pH were obtained, allowing its application in different regions of the human body. The encapsulation efficiency of methotrexate was approximately 95%. The drug delivery assays indicated that the nanoplatform is less active at pH 2; the presence of reduced glutathione enhanced the methotrexate release, reaching almost 50% methotrexate release after 96 h of analysis. The release efficiency of the nanoplatform allowed to identify its potential as a controlled drug delivery system.