Spermidine and folic acid dual-functionalized PLGA nanoparticles for co-delivery of doxorubicin and tariquidar to overcome multidrug resistance in breast cancer


TONBUL H., ULTAV G., ÖZTÜRK N., ARISOY S., ATEŞ M., ŞALVA E.

Journal of Drug Delivery Science and Technology, cilt.125, 2026 (SCI-Expanded, Scopus)

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 125
  • Basım Tarihi: 2026
  • Doi Numarası: 10.1016/j.jddst.2026.108713
  • Dergi Adı: Journal of Drug Delivery Science and Technology
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, EMBASE
  • Anahtar Kelimeler: Folic acid, MDR, P-gp, PLGA nanoparticles, Spermidine
  • İnönü Üniversitesi Adresli: Evet

Özet

Multidrug resistance (MDR) remains a major challenge in breast cancer treatment, mainly due to the overexpression of efflux transporters such as P-glycoprotein (P-gp), which reduces intracellular drug accumulation. In this study, spermidine–folic acid dual-functionalized PLGA nanoparticles were developed to co-deliver doxorubicin and the P-gp inhibitor tariquidar as a strategy to overcome MDR in breast cancer cells. The nanoparticles were physicochemically characterized and evaluated in doxorubicin-resistant EMT6/AR1 breast cancer cells. Drug release studies showed a sustained release behavior under physiological and mildly acidic conditions. Cytotoxicity and fluorescence microscopy studies demonstrated that the dual-functionalized, co-loaded nanoparticles produced the strongest reduction in cell viability and showed increased intracellular doxorubicin accumulation compared to free drug solutions and non-modified nanoparticle formulations. The improved activity is attributed to a combination of folate receptor–mediated uptake, spermidine-related cellular interactions, surface charge modulation, and inhibition of P-gp–mediated drug efflux by tariquidar. Overall, the developed dual-functionalized nanoparticle system offers a promising approach to improve intracellular drug delivery and overcome multidrug resistance in breast cancer therapy.