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<p>Letrozole (LTZ), a non-steroidal aromatase inhibitor that suppresses estrogen biosynthesis, is widely prescribed for hormone receptor-positive breast cancer but its therapeutic use is limited by poor aqueous solubility, low bioavailability, and gastrointestinal side effects. To overcome these challenges, LTZ-loaded silver nanoparticles (LTZ-AgNPs) were synthesized and optimized, and subsequently incorporated into a chitosan-based transdermal patch for sustained delivery. The nanoparticles showed sizes ranging from 73.6 to 203.1&#xa0;nm, polydispersity indices of 0.368–0.398, and zeta potentials of −22.6 to −26.8 mV, indicating colloidal stability. SEM confirmed a spherical morphology with smooth surfaces, while FTIR, DSC, and TGA analyses verified drug-polymer interactions, amorphization of LTZ, and enhanced thermal stability. The formulated patches exhibited uniform thickness (0.041–0.046&#xa0;mm) and weight (72–76&#xa0;mg), high drug content (97.5–99.2%), folding endurance of 85–89, tensile strength of 2.78–4.49&#xa0;MPa, and balanced moisture uptake of 5.4–16.4% with water vapor transmission rates of 0.05–0.45&#xa0;g cm⁻² h⁻¹. In vitro studies showed sustained cumulative % drug release of ~72% LTZ after 24&#xa0;h, while ex vivo permeation through rabbit skin reached ~78%, compared with ~40% from the ointment controls. In vivo pharmacokinetic evaluation demonstrated a Tmax of 8&#xa0;h, Cmax of 42.8 ng/mL, and significantly prolonged systemic exposure (AUC₀₋∞ 2010 ± 160 ng·h/mL) compared with the control formulation (<i>p</i> &lt; 0.05), with detectable plasma drug levels maintained up to 72&#xa0;h. These findings confirm that LTZ-AgNP-loaded chitosan patches provide a stable, biocompatible, and effective platform for sustained transdermal delivery of LTZ, offering improved bioavailability, reduced gastrointestinal adverse effects, and enhanced patient compliance for long-term breast cancer therapy.</p>

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Letrozole-Loaded Silver Nanoparticles in Chitosan Transdermal Patches for Improved Skin Permeation and Sustained Release

  • 期刊论文

  • 发表日期：

    2026年6月30日

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  • Iram Batool,
  • Nadiah Zafar,
  • Nariman Shahid,
  • Muhammad Akhlaq,
  • Mehrin Sherazi,
  • Khalid J. Alzahrani,
  • Khalaf F. Alsharif,
  • Abul Kalam Azad

摘要

Letrozole (LTZ), a non-steroidal aromatase inhibitor that suppresses estrogen biosynthesis, is widely prescribed for hormone receptor-positive breast cancer but its therapeutic use is limited by poor aqueous solubility, low bioavailability, and gastrointestinal side effects. To overcome these challenges, LTZ-loaded silver nanoparticles (LTZ-AgNPs) were synthesized and optimized, and subsequently incorporated into a chitosan-based transdermal patch for sustained delivery. The nanoparticles showed sizes ranging from 73.6 to 203.1 nm, polydispersity indices of 0.368–0.398, and zeta potentials of −22.6 to −26.8 mV, indicating colloidal stability. SEM confirmed a spherical morphology with smooth surfaces, while FTIR, DSC, and TGA analyses verified drug-polymer interactions, amorphization of LTZ, and enhanced thermal stability. The formulated patches exhibited uniform thickness (0.041–0.046 mm) and weight (72–76 mg), high drug content (97.5–99.2%), folding endurance of 85–89, tensile strength of 2.78–4.49 MPa, and balanced moisture uptake of 5.4–16.4% with water vapor transmission rates of 0.05–0.45 g cm⁻² h⁻¹. In vitro studies showed sustained cumulative % drug release of ~72% LTZ after 24 h, while ex vivo permeation through rabbit skin reached ~78%, compared with ~40% from the ointment controls. In vivo pharmacokinetic evaluation demonstrated a Tmax of 8 h, Cmax of 42.8 ng/mL, and significantly prolonged systemic exposure (AUC₀₋∞ 2010 ± 160 ng·h/mL) compared with the control formulation (p < 0.05), with detectable plasma drug levels maintained up to 72 h. These findings confirm that LTZ-AgNP-loaded chitosan patches provide a stable, biocompatible, and effective platform for sustained transdermal delivery of LTZ, offering improved bioavailability, reduced gastrointestinal adverse effects, and enhanced patient compliance for long-term breast cancer therapy.