Brain glioma is the most lethal type of cancer, with extremely poor prognosis and high relapse. Unfortunately, the treatment of brain glioma is often limited because of the low permeability of anticancer drugs across the blood–brain barrier (BBB). To circumvent this, magnetic mesoporous nanoparticles were synthesized and loaded with doxorubicin as an anticancer agent. These nanoparticles were fabricated with Pluronic F-127 and subsequently conjugated with transferrin (Tf) to achieve the sustained release of the drug at the targeted site. The physicochemical properties of the conjugated nanoparticles were analyzed using different techniques. The magnetic saturation of the nanoparticles determined by a vibration sample magnetometer was found to be 26.10 emu/g. The cytotoxicity study was performed using the MTT assay at 48 and 96 h against the U87 cell line. The Tf-conjugated nanoparticles (DOX-MNP-MSN-PF-127-Tf) exhibited a significant IC₅₀ value (0.570 μg/mL) as compared to the blank nanoparticles (121.98 μg/mL). To understand the transport mechanism of drugs across the BBB, an in vitro BBB model using human brain microvascular endothelial cells was developed. Among the nanoparticles, the Tf-conjugated nanoparticles demonstrated an excellent permeability across the BBB. This effect was predominant in the presence of an external magnetic field, suggesting that magnetic particles present in the matrix facilitated the uptake of drugs in U87 cells. Finally, it is concluded that nanoparticles conjugated with Tf effectively crossed the BBB. Thus, the developed nanocarriers can be considered as potential candidates to treat brain tumor.

Human serum albumin is the most abundant protein in plasma with the ability to bind to a variety of drug molecules. Magnetic nanoparticles are being extensively used in drug delivery due to its intrinsic magnetic properties. In this work, we have synthesized human serum albumin-coated citrate-functionalized iron oxide nanoparticles by CDI coupling. Furthermore, folic acid was decorated on human serum albumin by EDC and NHS coupling to confer targetability. Two cytotoxic drugs 5-fluorouracil (5FU) and curcumin were co-delivered. Wherein, the former is an anticancer agent and latter is a drug resistance depressor of former. The nanoparticles showed good aqueous dispersibility with a zeta potential of − 49.1 mV and magnetic core size in the range of 10–15 nm, thus exhibiting good magnetic property with magnetic saturation of 33.59 emu/g. Controlled drug release behavior was noticed in both drugs with faster release profile of 5FU. Nanoparticles also showed good cytotoxicity with lower IC₅₀ values in the presence of magnetic field. The contrasting difference was noticed in folic acid-decorated and non-decorated composites, similarly in the presence of magnetic field where cell uptake was enhanced.