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.
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.
Active targeting of folic acid and passive targeting of magnetic nanoparticles to bring about co-delivery of hydrophobic chemotherapeutic agents were the focus of this work. Co-precipitation in alkaline environment was employed for synthesizing Fe3O4 nanoparticles and stabilized by oleic acid. Aqueous dispersibility of oleic acid coated nanoparticles was brought about by folic acid modified Pluronic F127 and Pluronic F127 mixture. Folic acid is used as a targeting agent which was joined to Pluronic F127 via diethylene glycol bis(3-aminopropyl) ether spacer. The nanocomposite was used to delivery hydrophobic anticancer drugs, paclitaxel, and curcumin. Successful modification at each step was confirmed by FTIR and NMR. Quantitative analysis of attached folic acid indicated a total of 84.34% amount of conjugation. Nanoparticles characterization revealed the hydrodynamic size of and nanocomposite to be 94.2 nm nanometres. Furthermore, transmission electron micrograph reveals the size of the nanoparticle to be 12.5 nm hence also shows the superparamagnetic activity. Drug encapsulation efficiency of 34.7% and 59.5% was noted for paclitaxel and curcumin, respectively. Cytotoxic property of drug-loaded nanocomposites was increased in case of folic acid functionalized nanoparticles and further increased in the presence of an external magnetic field. Cellular uptake increased in the folic acid conjugated sample. Further many folds in the presence of an external magnetic field.Graphic abstract Electronic supplementary materialThe online version of this article (10.1007/s40204-019-0118-5) contains supplementary material, which is available to authorized users.
Development of TiO2 incorporated crosslinked PVA scaffolds with required characteristics for bone tissue engineering.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.