Abstract

We designed a biodegradable hybrid nanostructure for near-infrared (NIR)-induced photodynamic therapy (PDT) using an ultrasmall upconversion (UC) phosphor (β-NaYF4:Yb3+, Er3+ nanoparticle: NPs) and a hydrocarbonized rose bengal (C18RB) dye, a hydrophobized rose bengal (RB) derivative. The UC-NPs were encapsulated along with C18RB in the hydrophobic core of the micelle composed of poly(ethylene glycol) (PEG)-block-poly(ε-caprolactone) (PCL). The UC-NPs were well shielded from the aqueous environment, owing to the encapsulation in the hydrophobic PCL core, to efficiently emit green UC luminescence by avoiding the quenching by the hydroxyl groups. The hydrophobic part of C18 of C18RB worked well to be involved in the PCL core and located RB on the surface of the PCL core, making the efficient absorption of green light and the emission of singlet oxygen to surrounding water possible. Moreover, as the location is covered by PEG, the direct contact of RB to cells is prohibited to avoid their irradiation-free toxic effect on the cells. The hybrid nanostructure proved to be degradable by the hydrolysis of PEG-b-PCL. This degradation potentially results in renal excretion by the decomposition of the nanostructure into sub-10 nm size particles and makes them viable for clinical uses. These nanostructures can potentially be used for PDT of cancer in deep tissues.

Highlights

  • Photodynamic therapy (PDT) is a cancer treatment method that utilizes singlet oxygen generated by the irradiation of the accumulated photosensitizers in tumor tissues with visible light

  • We have reported the design methodology of dye conjugates made up of UC-NPs that emit red UC emission (660 nm), coated with the biocompatible polymer poly(ethylene glycol) (PEG) for PDT applications

  • We proposed and proved the effectiveness of a unique nanostructure using ultrasmall UC-NPs coupled with rose bengal (RB) for NIR-induced photodynamic therapy

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Summary

■ INTRODUCTION

Photodynamic therapy (PDT) is a cancer treatment method that utilizes singlet oxygen generated by the irradiation of the accumulated photosensitizers in tumor tissues with visible light. While free RB significantly decreased the cell viability at 0.13 mg/mL without irradiation for excitation, the hybrid NPs did not show cytotoxicity at ≤0.91 mg/mL RB (prepared with a C18RB/ PEG-b-PCL mass ratio of ≤0.75:15) (Figure 5a). This result suggested that encapsulating the RB compound into the hybrid.

■ CONCLUSIONS
■ ACKNOWLEDGMENTS
■ REFERENCES
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