Folic acid- terminated poly (2- diethyl amino ethyl 3 methacrylate) brush -gated magnetic mesoporous 4 nanoparticles as smart drug delivery system
Alswieleh, Abeer M. Beagan 1,*,† , Ahlam A. Alghamdi 1, Shatha S. Lahmadi 1, Majed A. Halwani 2 , Mohammed S. Almeataq 3, Abdulaziz N. Alhazaa 4 , Khalid M. Alotaibi 1 and Abdullah M. . 2020
Currently, chemotherapy is an important method for the treatment of various cancers.
Nevertheless, it has many limitations, such as poor tumour selectivity and multi-drug resistance. It is
necessary to improve this treatment method by incorporating a targeted drug delivery system aimed
to reduce side effects and drug resistance. The present work aims to develop pH-sensitive nanocarriers
containing magnetic mesoporous silica nanoparticles (MMSNs) coated with pH-responsive
polymers for tumour-targeted drug delivery via the folate receptor. 2-Diethyl amino ethyl methacrylate
(DEAEMA) was successfully grafted on MMSNs via surface initiated ARGET atom transfer
radical polymerization (ATRP), with an average particle size of 180 nm. The end groups of poly
(2-(diethylamino)ethyl methacrylate) (PDEAEMA) brushes were converted to amines, followed by a
covalent bond with folic acid (FA) as a targeting agent. FA conjugated to the nanoparticle surface
was confirmed by X-ray photoelectron spectroscopy (XPS). pH-Responsive behavior of PDEAEMA
brushes was investigated by Dynamic Light Scattering (DLS). The nanoparticles average diameters
ranged from ca. 350 nm in basic media to ca. 650 in acidic solution. Multifunctional pH-sensitive
magnetic mesoporous nanoparticles were loaded with an anti-cancer drug (Doxorubicin) to investigate
their capacity and long-circulation time. In a cumulative release pattern, doxorubicin (DOX)
release from nano-systems was ca. 20% when the particle exposed to acidic media, compared to ca.
5% in basic media. The nano-systems have excellent biocompatibility and are minimally toxic when
exposed to MCF-7, and -MCF-7 ADR cells
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