Synthesis of Novel Conjugated Linoleic Acid (CLA)-Coated Superparamagnetic Iron Oxide Nanoparticles (SPIONs) for the Delivery of Paclitaxel with Enhanced In Vitro Anti-Proliferative Activity on A549 Lung Cancer Cells

Abstract

The application of Superparamagnetic Iron Oxide Nanoparticles (SPIONs) as a nanomedicine for Non-Small Cell Lung Carcinoma (NSCLC) can provide effective delivery of anticancer drugs with minimal side-effects. SPIONs have the flexibility to be modified to achieve enhanced oading of hydrophobic anticancer drugs such as paclitaxel (PTX). The purpose of this study was to synthesize novel trans-10, cis-12 conjugated linoleic acid (CLA)-coated SPIONs loaded with PTX to enhance the anti-proliferative activity of PTX. CLA-coated PTX-SPIONs with a particle size and zeta potential of 96.5 ± 0.6 nm and −27.3 ± 1.9 mV, respectively, were synthesized. The superparamagnetism of the CLA-coated PTX-SPIONs was confirmed, with saturation magnetization of 60 emu/g and 29 Oe coercivity. CLA-coated PTX-SPIONs had a drug loading efficiency of 98.5% and demonstrated sustained site-specific in vitro release of PTX over 24 h (i.e., 94% at pH 6.8 mimicking the tumor microenvironment). Enhanced anti-proliferative activity was also observed with the CLA-coated PTX-SPIONs against a lung adenocarcinoma (A549) cell line after 72 h, with a recorded cell viability of 17.1%. The CLA-coated PTX-SPIONs demonstrated enhanced suppression of A549 cell proliferation compared to pristine PTX, thus suggesting potential application of the nanomedicine as an effective site-specific delivery system for enhanced therapeutic activity in NSCLC therapy.

Surface Immobilization of Anti-VEGF Peptide on SPIONs for Antiangiogenic and Targeted Delivery of Paclitaxel in Non-Small-Cell Lung Carcinoma

“…The fabricated nanosystem exhibited a sustained release of PTX at pH 6.8, with maximal cumulative release of 99.4% recorded at 16 h. The sustained PTX release at acidic pH is consistent with previous studies which have reported a similar release behavior when PTX is loaded onto fatty acids such as oleic acid and its derivatives . The high and sustained release of PTX at pH 6.8 could be attributed to the weakening of the hydrophobic–hydrophobic strength between CLA ∼ PTX at relatively acidic pH, thus allowing PTX to detach from CLA ends and is released over time . Meanwhile, the PTX release was comparatively lower at physiological pH 7.4, with only 19.6% of PTX released in over 24 h. This low cumulative release rate relates to the stability of the hydrophobic CLA-PTX complex at physiological pH, keeping PTX intact over time.…”

“…There is already compelling evidence in literature that HRH peptide suppresses cancer cell proliferation in vitro by halting angiogenesis . Moreover, the results obtained support our previous findings which showed that CLA-coated PTX-SPIONs confer enhanced anti-proliferative activity on A549 cells owing to additional anticancer activity of 10E, 12Z CLA in synergy with PTX …”

“…Moreover, 10E, 12Z CLA is an excellent coating agent, allowing maximal partitioning of PTX, a hydrophobic anticancer drug, owing to its poor aqueous solubility. , SPIONs coated with CLA have demonstrated enhanced antitumor activity against mouse breast cancer cells (4T1) . Meanwhile, peptides generally exhibit high selectivity and good efficacy for biomedical application. , This study reports on a holistic fabrication approach in achieving a targeted nanosystem that is safe by design, through the formulation of HRH-functionalized CLA-coated PTX-SPIONs (CLA-coated PTX-SPIONs@HRH) and its in vitro and in vivo evaluation.…”

New insights into nanosystems for non-small-cell lung cancer: diagnosis and treatment

“…The CLA-coated PTX-SIONs showed a drug loading efficiency of 98.5% and persistent site-specific release of PTX in vitro over 24 h, thus suggesting that the nanomedicine is a promising alternative for an effective drug delivery system targeted NSCLC. 145 Interestingly, Qin et al 146 designed a hybrid nanosystem (SIONs + RPPs) in which phase transition nanodroplets with immunomodulatory capabilities were used to potentiate SION-mediated mild magnetic hyperthermia (MHT, <44 °C) and further inhibit tumour proliferation and metastasis. Magnetic-thermal sensitive phase-transition nanodroplets (RPPs) were fabricated from the immune adjuvant resiquimod (R848) and the phase transition agent perfluoropentane (PFP) encapsulated in a PLGA shell.…”

Ultrasmall Superparamagnetic Particles of Iron Oxide and Cardiac Magnetic Resonance: Novel Imaging in Everyday Conditions

“…Apart from the above, the coating that surrounds the core of the nanoparticle also acts like a 'harbour' to which ligands, drug molecules, and other molecular targets can bind [6]. Taking all of these into consideration, it is obvious why molecular imaging and targeted drug delivery are some of the areas where iron oxide nanoparticles have been successfully applied [23][24][25].…”