Abstract
Photodynamic therapy (PDT) as a non-aggressive therapy with fewer side effects has unique advantages over traditional treatments. However, PDT still has certain limitations in clinical applications, mainly because most photosensitizers utilized in PDT are hydrophobic compounds, which will self-aggregate in the aqueous phase and cause undesirable effects. In order to resolve this, we utilized the self-polymerization of dopamine molecules under alkaline conditions to coat cerium oxide nanorods (CeONR) with a dense polydopamine (PDA) film. Thereafter, thiolated galactose (Gal-SH) and hypericin (Hyp) were modified and loaded onto the surface to construct CeONR@PDA-Gal/Hyp, respectively, which can be used for targeted photodynamic therapy of human hepatoma HepG2 cells. CeONR@PDA-Gal/Hyp was characterized by transmission electron microscope (TEM), Zeta potential, Ultraviolet-visible (UV-Vis), and fluorescence spectroscopy, respectively. This hypericin delivery system possesses good biocompatibility and specific targeting ability, where the galactose units on the surface of CeONR@PDA-Gal/Hyp can specifically recognize the asialo-glycoprotein receptors (ASGP-R), which overexpress on HepG2 cell membrane. Furthermore, Hyp will detach from the surface of CeONR@PDA-Gal/Hyp after the nanorods enter cancer cells, and shows excellent PDT effect under the irradiation of light with a wavelength of 590 nm. Our work exemplifies a novel targeted delivery of hydrophobic photosensitizers for cancer treatment.
Highlights
Cancer is one of the major causes leading to death worldwide [1,2]
The construction process of cerium oxide nanorods (CeONR)@PDA-Gal/Hyp is illustrated in Scheme 1
Thereafter, Hyp can be loaded onto the surface of CeONR@PDA-Gal by π–π stacking and hydrogen bonding to overcome the problem of poor solubility of Hyp in an aqueous phase [34,35]
Summary
Cancer is one of the major causes leading to death worldwide [1,2]. Traditional treatments, such as surgery, chemotherapy, and radiotherapy do not have ideal therapeutic effects due to various side effects [3,4]. Hypericin (Hyp) has been recognized as a potential excellent photosensitizer due to its unique photochemical property [10]. Hyp has a high singlet oxygen yield (0.17–0.80) and a maximum absorption wavelength (590 nm), which is close to an optimal wavelength range (600 to 1000 nm) [11]. Hyp has the characteristics of low cost and low dark toxicity
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