The influence of carboxylate moieties for efficient loading and pH-controlled release of doxorubicin in Fe3O4 magnetic nanoparticles

• Published in: Colloids and surfaces. A, Physicochemical and engineering aspects Vol. 602; p. 125137
• Main Authors: Saepudin, Endang, Fadhilah, Hasna Resti, Khalil, Munawar
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 05-10-2020
• Subjects: Doxorubicin; Drug delivery; Fe3O4 nanoparticles; Surface functionalization; Surface functionalization; Drug delivery; Doxorubicin; Fe3O4 nanoparticles
• ISSN: 0927-7757; 1873-4359
• DOI: 10.1016/j.colsurfa.2020.125137

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•Carboxylates functionalized Fe3O4 magnetic nanoparticles were prepared using co-precipitation method.•The effect surface modifiers, i.e. succinic, ascorbic, and citric acids was assessed on conjugation and release of DOX.•Maximum DOX loading efficiency was achieved for AA-MNPs.•The highest DOX release was achieved for SA-MNP.•In-vitro MTT assay demonstrated that SA-MNP had the lowest toxicity to HeLa cells.
One of the significant challenges in a nanoparticles-based anticancer drug delivery system for cancer therapy application is to design nanoparticles with specific functionality for efficient drug conjugation and release. In the present study, different carboxylate molecules, i.e., succinic acid (SA), ascorbic acid (AA), and citric acid (CA), were used as surface modifiers for delivery of an anticancer drug, doxorubicin (DOX), using Fe3O4 magnetic nanoparticles (MNPs). Here, a simple one-pot co-precipitation method was successfully used to fabricate monodisperse and uniform carboxylates functionalized Fe3O4 nanoparticles with excellent superparamagnetic properties and colloidal stabilities. Based on the result, the as-prepared MNPs exhibited high drug loading due to the formation of intermolecular forces between DOX and carboxylates moieties or MNPs surface. Besides, the release of the loaded DOX could quickly be released by simply reducing the pH of the suspension. However, it was observed that both loading efficiency and release of DOX were significantly affected by the type of carboxylate moieties. Finally, in vitro MTT assay of HeLa cell lines also revealed that the as-prepared DOX-loaded nanoparticles were able to induce the death of the cancer cell efficiently.