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PEGylated Lecithin-Chitosan Nanoparticle–Encapsulated Alphα-Terpineol for In Vitro Anticancer Effects

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  • Theme: Inhaled Drug Delivery of Biologics for Therapeutic and Vaccination
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Abstract

The aim of this study was to fabrication PEGylated lecithin-chitosan nanoparticles (PLC-NPs) as alphα-Terpineol’s (αT-PLC-NPs) delivery system and examine its anti-cancer effects. αT-PLC-NPs were synthesized by self-assembling method; after characterization, entrapment efficiency of α-T was measured by HPLC procedure. MTT test was conducted for cytotoxicity evaluation. Chick chorioallantoic membrane (CAM) and quantitative polymerase chain reaction (qPCR) analysis were used to determine the angiogenesis properties, and qPCR, flow cytometry, and acridine orange and propidium iodide (AO/PI) staining were used to evaluate the pro-apoptotic effects of αT-PLC-NPs. Finally, the anti-inflammatory and antibacterial activity of the αT-PLC-NPs was also evaluated. αT-PLC-NPs with a size of 220.8 nm, polydispersity index (PDI) of 0.3, zeta potential of +29.03 mV, and encapsulation efficiency of 82% showed higher inhibitory effect on MCF7 cells (IC50: 750 μg/mL) compared to HFF cells (above 1000 μg/mL). Decreased angiogenesis indices and embryonic growth factors in CAM assay, decreased expression of VEGF and VEGF-R genes, and decreased cell migration showed the inhibitory effect of αT-PLC-NPs on angiogenesis. Increased expression of P53, P21, and caspase9 genes, as well as the results of AO/PI staining along with increasing the number of SubG1 phase cells in flow cytometry, confirmed the pro-apoptotic effects of αT-PLC-NPs. Also, its anti-inflammatory effects were demonstrated by inhibiting the expression of pro-inflammatory cytokines (TNF-α and IL-6). The inhibitory power of αT-PLC-NPs in suppressing gram-positive and negative bacterial strains was demonstrated by disk diffusion (DD), minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) methods. PLC-NPs are a promising carrier for α-T transfer for preclinical studies.

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Acknowledgements

This work was supported by Islamic Azad University, Mashhad, Iran, and thus is appreciated by the author.

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This research was performed at personal expense in the laboratory of Islamic Azad University of Mashhad.

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  1. Department of Biology, Mashhad Branch, Islamic Azad University, Mashhad, Iran

    Bahar Zarei, Masoud Homayouni Tabrizi & Amir Rahmati

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  1. Bahar Zarei
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Masoud Homayouni Tabrizi conceived of the presented idea. Bahar Zarei, Masoud Homayouni Tabrizi, and Amir Rahmati performed the experiments and computations.

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Correspondence to Masoud Homayouni Tabrizi.

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Zarei, B., Tabrizi, M.H. & Rahmati, A. PEGylated Lecithin-Chitosan Nanoparticle–Encapsulated Alphα-Terpineol for In Vitro Anticancer Effects. AAPS PharmSciTech 23, 94 (2022). https://doi.org/10.1208/s12249-022-02245-5

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