ArticleAAPS PharmSciTech2026
Folic Acid-Conjugated Solid Lipid Nanoparticles for Ratiometric Combination Delivery of Docetaxel and Erlotinib in Triple-Negative Breast Cancer Therapy.
Article in AAPS PharmSciTech, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Authors and funding
5 authors.
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Abstract
Triple-negative breast cancer (TNBC) is an aggressive subtype with limited therapeutic options and poor clinical outcomes. This study evaluated folic acid-functionalized solid lipid nanoparticles co-loaded with docetaxel and erlotinib (FA-DOC/ERL-SLNs) as an oral targeted therapy for TNBC. FA-DOC/ERL-SLNs exhibited the lowest IC₅₀ values of 0.82 ± 0.05 μM and 0.92 ± 0.03 μM in MDA-MB-231 and 4T1 cells, respectively, with enhanced cellular uptake compared with free drugs and non-targeted SLNs. The formulation also induced higher apoptosis (apoptosis indices of 1.42 and 1.45), greater G2/M cell-cycle arrest, autophagy inhibition, and reduced clonogenicity and migration. Pharmacokinetic studies demonstrated markedly improved oral bioavailability, with AUC₀-t increasing from 1.03 to 45.69 μg·h/mL for docetaxel and from 18.30 to 87.76 μg·h/mL for erlotinib. In 4T1 tumor-bearing mice, FA-DOC/ERL-SLNs reduced tumor volume by approximately 1.5-fold compared with non-targeted SLNs and 2.5-3.0-fold compared with free drugs, without significant body weight loss or systemic toxicity. These findings demonstrate that FA-DOC/ERL-SLNs enhance the efficacy and safety of oral docetaxel-erlotinib combination therapy and represent a promising targeted nanocarrier platform for TNBC treatment.
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