Tamoxifen Loaded Conjugate of Self‐Assembled Fluorescent Organic Nanoparticle and Vesicle for p53‐Activated Breast Cancer Therapy
Abstract
Fluorescent organic nanoparticles (FONPs) with intrinsic fluorescence and self-assembled vesicles (VES) are receiving widespread interest in biomedicine. Both FONPs and VES have individual drawbacks like cytotoxicity of FONPs while VES gets eliminated through reticuloendothelial system impeding their applications. Development of nanoconjugates through amalgamation of individual nanocarrier with complementing features would find greater significance by overcoming individual hurdles. Herein, we report design and synthesis of FONP-VES nanoconjugate by combining naphthalimide-based pH-responsive hydrazone moiety containing FONP (NIHYDH) and cholesterol-based vesicle (CBAV) via electrostatic interaction. FONP, VES and FONP-VES conjugate were characterized by spectroscopy and microscopy. Orange emitting NIHYDH-CBAV nanoconjugate was utilised in bioimaging and as delivery vehicle which demonstrated targeted transport of tamoxifen (TAM) to (ER+) MCF7 cells through pH-responsive dissipation of nanoconjugate owing to cleavage of hydrazone bond under acidic pH gradient. TAM has demonstrated clinical drug resistance along with limited bioavailability. Upon encapsulation within nanoconjugate, NIHYDH-CBAV-TAM offered ∼2.8-fold higher cytotoxicity toward MCF7 cells compared to normal NIH3T3 cells alongside demonstrating ∼2.1-fold reduction in the size of MCF7 3D tumour spheroids. TAM loaded nanoconjugate was ∼2.2-3.4-fold more cytotoxic than TAM loaded individual nanocarrier. Cytotoxicity…
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