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<p>Exemestane (EXE), a steroidal aromatase inhibitor widely prescribed for estrogen receptor-positive breast cancer in postmenopausal women, is hindered by significant pharmacokinetic and delivery challenges. Its poor aqueous solubility, limited oral bioavailability, and severe systemic side effects compromise both therapeutic efficacy and patient adherence. Moreover, monotherapy with EXE often falls short of its full anticancer potential. Recent advancements in nanotechnology have introduced a spectrum of innovative delivery platforms designed to address these limitations. This review comprehensively examines the pharmacokinetics, mechanism of action, and clinical delivery obstacles of EXE. It highlights a diverse array of nanocarrier systems—including polymeric-based nanoparticles, nanostructured lipid carriers, and stimuli-responsive nanoparticles—that offer improved solubility, targeted delivery, and controlled release. Additionally, emerging approaches such as inorganic nanoparticles and nanoparticle-enabled co-delivery strategies are discussed for their potential to enhance combination therapy. Finally, nanotechnology-driven monitoring tools are explored as promising adjuncts for optimizing EXE-based cancer treatment. Collectively, these nanoformulation strategies represent a transformative shift toward more effective, patient-centric breast cancer therapeutics.</p> Graphical Abstract <p></p>

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Advancements in Exemestane-Loaded Nanocarriers For Targeted Breast Cancer Therapy: A Comprehensive Review

  • 期刊论文

  • 发表日期：

    2025年10月1日

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  • Nadia Talebibidhendi,
  • Mehrab Pourmadadi,
  • Fatemeh Yazdian,
  • Hamid Rashedi,
  • Abbas Rahdar,
  • Suresh Ghotekar

摘要

Exemestane (EXE), a steroidal aromatase inhibitor widely prescribed for estrogen receptor-positive breast cancer in postmenopausal women, is hindered by significant pharmacokinetic and delivery challenges. Its poor aqueous solubility, limited oral bioavailability, and severe systemic side effects compromise both therapeutic efficacy and patient adherence. Moreover, monotherapy with EXE often falls short of its full anticancer potential. Recent advancements in nanotechnology have introduced a spectrum of innovative delivery platforms designed to address these limitations. This review comprehensively examines the pharmacokinetics, mechanism of action, and clinical delivery obstacles of EXE. It highlights a diverse array of nanocarrier systems—including polymeric-based nanoparticles, nanostructured lipid carriers, and stimuli-responsive nanoparticles—that offer improved solubility, targeted delivery, and controlled release. Additionally, emerging approaches such as inorganic nanoparticles and nanoparticle-enabled co-delivery strategies are discussed for their potential to enhance combination therapy. Finally, nanotechnology-driven monitoring tools are explored as promising adjuncts for optimizing EXE-based cancer treatment. Collectively, these nanoformulation strategies represent a transformative shift toward more effective, patient-centric breast cancer therapeutics.

Graphical Abstract