Dual-ligand functionalized pH- and thermo-sensitive niosomes for precise targeted therapy and imaging of HER-2-positive breast cancer


Saharkhiz S., Nasri N., Naderi N., Saharkhiz S., ZAREPOUR A., Ghalehshahi S. S., ...More

Materials Today Chemistry, vol.47, 2025 (SCI-Expanded, Scopus) identifier identifier

  • Publication Type: Article / Article
  • Volume: 47
  • Publication Date: 2025
  • Doi Number: 10.1016/j.mtchem.2025.102829
  • Journal Name: Materials Today Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Keywords: Dual-targeted, pH-sensitive, Smart-delivery, Theranostic, Thermo-sensitive
  • Kocaeli University Affiliated: Yes

Abstract

In current study, we examined dual-targeted pH- and thermo-sensitive niosome platforms (pTSNs) for targeted delivery of Gemcitabine (GEM) and CdSe/ZnS QDs to HER-2-positive breast cancer cells for therapeutic and imaging purposes. The niosomal particles were prepared using thin-film hydration method and functionalized with Trastuzumab monoclonal antibody (Trz) and Folic acid (FA), as targeting agents. The fabricated formulation was characterized through different analyses, including DLS, Zeta potential, FTIR, SEM, and Fluorescence Microscopy. Besides, bioactivite features of the fabricated particles were evaluated using different analysis included determining loading and release profile, cell viability assessment, and relative cellular uptake. Characteristics results revealed a neutral, round-shaped, homogenous population of dual-targeted pTSNs with an average size of 200 nm that were correctly functionalized with conjugates. Moreover, it showed about 94.5 % entrapment efficiency (EE%), as well as up to 92 % drug release at pH 6.5 and 42 °C, while that amount was about 35 % at pH 7.4 and 37 °C. MTT and relative assessments demonstrated a 4.5-fold higher growth inhibition of SKBR-3 cells and 2600 times more cellular uptake by Trz and FA-conjugated pTSNs compared to non-targeted and non-sensitive particles. Overall, the developed platform proves to be a suitable carrier for the effective delivery of chemotherapeutic agents to cancer cells.