Development and <i>in vivo</i> biodistribution of folate-targeted nanolipid system for erlotinib in breast cancer treatment

The aim of the study was to develop folate targeted nanolipid carrier system (FA-ERT-NLCs) and study its in vivo oral biodistribution study for its absorption mechanism. Folic acid was conjugated through pyridine and EDC chemistry. FA-ERT-NLCs was developed by high-pressure homogenization and parameters were optimized through design expert software. FA-ERT-NLCs were evaluated through <i>in vitro</i> characterization, <i>Ex vivo</i> and <i>in vivo</i> biodistribution studies. Moreover, female Wistar rats were used in this study. Findings showed that targeted NLCs were found in nanometric range (182.34 nm) with negatively charge surface and PDI was found to be −16.2 mV and 0.203. The folate content in the conjugate was measured and found to be 71.33%. The depth of ERT and FC-ERT-NLCs was found to be 20 µm and 80.2 µm in rat intestine. Developed formulation was effective against MCF-7 cell lines. The IC50 values were found to be 526.2 µg/mL for ERT and 333.7 µg/mL for FC-ERT-NLCs. FA-ERT-NLCs are absorbed through intestine by lymphatic system. This study showed a promising targeted strategy for effective and safer breast cancer treatment.

Publication Details

Journal
Figshare
Published
2025-01-01
DOI
https://doi.org/10.6084/m9.figshare.29149444.v1
Primary Topic
Nanoparticle-Based Drug Delivery
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article
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article

Development and in vivo biodistribution of folate-targeted nanolipid system for erlotinib in breast cancer treatment

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Nanoparticle-Based Drug Delivery
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Development and in vivo biodistribution of folate-targeted nanolipid system for erlotinib in breast cancer treatment

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Abstract

The aim of the study was to develop folate targeted nanolipid carrier system (FA-ERT-NLCs) and study its in vivo oral biodistribution study for its absorption mechanism. Folic acid was conjugated through pyridine and EDC chemistry. FA-ERT-NLCs was developed by high-pressure homogenization and parameters were optimized through design expert software. FA-ERT-NLCs were evaluated through <i>in vitro</i> characterization, <i>Ex vivo</i> and <i>in vivo</i> biodistribution studies. Moreover, female Wistar rats were used in this study. Findings showed that targeted NLCs were found in nanometric range (182.34 nm) with negatively charge surface and PDI was found to be −16.2 mV and 0.203. The folate content in the conjugate was measured and found to be 71.33%. The depth of ERT and FC-ERT-NLCs was found to be 20 µm and 80.2 µm in rat intestine. Developed formulation was effective against MCF-7 cell lines. The IC50 values were found to be 526.2 µg/mL for ERT and 333.7 µg/mL for FC-ERT-NLCs. FA-ERT-NLCs are absorbed through intestine by lymphatic system. This study showed a promising targeted strategy for effective and safer breast cancer treatment.

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Nanoparticle-Based Drug Delivery
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