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Optimization, Characterization and in vivo Evaluation of Paclitaxel-Loaded Folate-Conjugated Superparamagnetic Iron Oxide Nanoparticles

Authors Gui G, Fan Z, Ning Y, Yuan C, Zhang B, Xu Q

Received 23 October 2020

Accepted for publication 19 February 2021

Published 19 March 2021 Volume 2021:16 Pages 2283—2295

DOI https://doi.org/10.2147/IJN.S287434

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 3

Editor who approved publication: Dr Ebrahim Mostafavi


Gang Gui,1,* Ziqi Fan,1,* Yihuan Ning,1 Cancan Yuan,2 Baolin Zhang,3 Qin Xu1

1College of Pharmacy, Guilin Medical University, Guilin, 541004, People’s Republic of China; 2Department of Pharmacy, Luohe City People’s Hospital, Luohe, 462000, People’s Republic of China; 3College of Materials Science and Engineering, Guilin University of Technology, Guilin, 541004, People’s Republic of China

*These authors contributed equally to this work

Correspondence: Qin Xu
College of Pharmacy, Guilin Medical University, Guilin, 541004, People’s Republic of China
Email [email protected]
Baolin Zhang
College of Materials Science and Engineering, Guilin University of Technology, Guilin, 541004, People’s Republic of China
Email [email protected]

Background: Paclitaxel (PTX) has interesting anticancer activity. However, it is insoluble in water, which seriously hinders its use in clinical. Superparamagnetic iron oxide nanoparticles (SPIONs) are used as an ideal drug delivery system. Therefore, we proposed a folic acid (FA) targeting drug-loaded SPIONs to reduce its adverse reaction.
Methods: To improve the hydrophilicity of PTX, the structure of PTX was modified by succinic anhydride to obtain 2ʹ-succinate paclitaxel (SPTX). FA conjugated Polyethylene glycol (PEG)/polyethyleneimine (PEI)-SPIONs SPTX-loaded nanoparticles ([email protected]@PEG/PEI-SPIONs) were prepared by solvent volatilization and hydrogen bond adsorption, and the nano-formulation was optimized by response surface methodology (RSM). The characteristics, antitumor effect in vitro, pharmacokinetics, and biodistribution of [email protected]@PEG/PEI-SPIONs were evaluated.
Results: SPTX was successfully loaded on the surface of [email protected]/PEI-SPIONs. The formation of [email protected]@PEG/PEI-SPIONs was exhibited water-dispersive monodispersity with high stability by RSM, and dynamic light scattering (DLS) was 178.1± 3.12 nm, particle size observed in the transmission electron microscope (TEM) was 13.01± 1.10 nm, and the encapsulation efficiency (EE) and loading efficiency (LE) were 81.1± 1.66% and 14.8± 1.46%, respectively. It enhanced the stability in normal physiological condition, accelerated drug release at tumorous pH, and preferentially prolonged the circulation time. In vitro, the [email protected]@PEG/PEI-SPIONs significantly targeted to folate receptor (FR) positive cancers cell (HNE-1) via the receptor-ligand mediated pathway, resulting in effective cytotoxic activity. Pharmacokinetic results demonstrated that [email protected]@PEG/PEI-SPIONs (t1/2=3.41 h) had longer than free SPTX or PTX (t1/2=1.67 h) in rats in vivo. Tissue distribution studies showed that [email protected]@PEG/PEI-SPIONs were present at high levels in the liver and help in targeting the folate receptors present on the kidneys.
Conclusion: These results suggest that [email protected]@PEG/PEI-SPIONs offer a highly promising approach to control drug release, improve drug pharmacokinetics and actively target the nasopharyngeal carcinoma.

Keywords: paclitaxel, folic acid, superparamagnetic iron oxide nanoparticles, targeted drug delivery, response surface methodology, anti-nasopharyngeal carcinoma

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