Ligand-targeted Theranostic Liposomes combining methylene blue attached upconversion nanoparticles for NIR activated bioimaging and photodynamic therapy against HER-2 positive breast cancer

• Published in: Journal of luminescence 2021-09, Vol.237, p.118143, Article 118143
• Main Authors: Panikar, Sandeep Surendra, Ramírez-García, Gonzalo, Banu, Nehla, Vallejo-Cardona, Alba A., Lugo-Fabres, Pavel, Camacho-Villegas, Tanya A., Salas, Pedro, De la Rosa, Elder
• Format: Article
• Language: English
• Subjects: Anti-HER2 peptide; Lipid nanoparticle; Liposome; Methylene blue dye; Photodynamic therapy (PDT); Theranostics; Upconversion bioimaging
• ISSN: 0022-2313; 1872-7883
• DOI: 10.1016/j.jlumin.2021.118143

Methylene Blue (MB) based Photodynamic therapy (PDT) has gained much interest recently due to its FDA approval for treating various diseased conditions in human. Herein, we report for the first time the systematic evaluation of NIR-controlled PDT efficiency of free MB and MB attached on NaYF4:Yb, Er nanoparticles (UCNPs) i.e., MB@UCNPs encapsulated within Liposomes (LPs). The UCNPs act as an upconverting energy source for the photosensitizers dye MB for enhanced ROS generation and utilizing the remnant energy for selective tracking or bioimaging. The specificity of our nano LPs system was achieved by conjugating our newly discovered anti-HER2 peptides by phage display technique and demonstrated its specificity by confocal imaging of HER-2 overexpressing in vitro model. A significant decline in the cell viability by 83% and 64% was achieved by the LPs containing MB@UCNPs and free MB with UCNPs, respectively after 975 nm NIR laser exposure (0.60 W/cm−2) for 5 min continuous exposure. Also, the flowcytometry assay confirmed that enhanced ROS generation capability of LPs with MB@UCNPs was higher than the free MB with UCNPs, which states the relevance of the minimal distance between MB and UCNPs for higher anti-cancer efficiency. Enhancing the Photodynamic efficiency of Methylene blue by capping on Upconverting nanoparticle and, delivering efficiently within the cancer cells using Liposome as drug-delivery vehicle. [Display omitted] •Anti-HER2 Theranostic Liposome for Photodynamic therapy (PDT) and selective bioimaging.•Enhancing PDT efficiency of methylene Blue by capping with upconverting nanoparticle v/s free methylene Blue.•Liposome loaded with upconversion nanoparticle (UCNPs) and methylene blue.•Enhanced Reactive oxygen species (ROS) generation after NIR-light exposure.