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<p>Folate receptor (FR)-mediated drug delivery has emerged as a promising approach for improving the specificity and efficacy of chemotherapy while minimizing systemic toxicity. In this study, we developed and characterized Folate Functionalized Nanostructured Lipid Carriers (FF-NLCs) for the targeted delivery of Paclitaxel in A549 lung adenocarcinoma cells. FF-NLCs prepared by hot homogenization followed by probe sonication method. Physicochemical characterization of FF-NLCs showed a size of 175.3 ± 1.2&#xa0;nm, PDI of 0.415 ± 0.12 and Zeta potential 5.02 ± 0.4&#xa0;mV respectively. Entrapment efficiency was found to be 76.24 ± 1.6%, while drug loading 26.2 ± 1.2%, respectively. In-vitro cytotoxicity studies on A549 lung adenocarcinoma cells revealed superior anti-cancer effects of FF-NLCs, with growth inhibition increasing from 18.7% at 10&#xa0;µg/ml to 46.1% at 80&#xa0;µg/ml, compared to Pacli-NLCs (15.5% to 26.0%) and ADR (7.6% to 23.7%). Fluorescence-based cell uptake studies confirmed enhanced internalization of FF-NLCs via receptor-mediated endocytosis, supporting their superior targeting ability. In vivo anticancer evaluation highlighted tumour suppression trends, with FF-NLCs demonstrating the greatest reduction in tumour volume (13.15 ± 10.601 mm<sup>3</sup>), tumour weight (0.29 ± 0.240&#xa0;g), and tumour incidence (66.67%) compared to Pacli-NLCs (27.60 ± 13.927 mm<sup>3</sup>, 0.75 ± 0.401&#xa0;g, 83.33%) and PDS (35.90 ± 18.169 mm<sup>3</sup>, 0.77 ± 0.398&#xa0;g, 83.33%). Although tumour volume initially declined, progression was observed at later stages, emphasizing the need for optimizing nanoparticle stability, sustained drug release, and resistance mitigation strategies. Overall, FF-NLCs exhibit superior therapeutic potential, enabling a 1.25-fold increase in lung carcinoma treatment efficacy over conventional drug solutions.</p>

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Folate Functionalized Nanostructured Lipid Carriers of Paclitaxel for site specific A549 Lung Adenocarcinoma Targeting

  • 期刊论文

  • 发表日期：

    2025年8月26日

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  • Vaibhav Rajoriya,
  • Ravikant Gupta

摘要

Folate receptor (FR)-mediated drug delivery has emerged as a promising approach for improving the specificity and efficacy of chemotherapy while minimizing systemic toxicity. In this study, we developed and characterized Folate Functionalized Nanostructured Lipid Carriers (FF-NLCs) for the targeted delivery of Paclitaxel in A549 lung adenocarcinoma cells. FF-NLCs prepared by hot homogenization followed by probe sonication method. Physicochemical characterization of FF-NLCs showed a size of 175.3 ± 1.2 nm, PDI of 0.415 ± 0.12 and Zeta potential 5.02 ± 0.4 mV respectively. Entrapment efficiency was found to be 76.24 ± 1.6%, while drug loading 26.2 ± 1.2%, respectively. In-vitro cytotoxicity studies on A549 lung adenocarcinoma cells revealed superior anti-cancer effects of FF-NLCs, with growth inhibition increasing from 18.7% at 10 µg/ml to 46.1% at 80 µg/ml, compared to Pacli-NLCs (15.5% to 26.0%) and ADR (7.6% to 23.7%). Fluorescence-based cell uptake studies confirmed enhanced internalization of FF-NLCs via receptor-mediated endocytosis, supporting their superior targeting ability. In vivo anticancer evaluation highlighted tumour suppression trends, with FF-NLCs demonstrating the greatest reduction in tumour volume (13.15 ± 10.601 mm3), tumour weight (0.29 ± 0.240 g), and tumour incidence (66.67%) compared to Pacli-NLCs (27.60 ± 13.927 mm3, 0.75 ± 0.401 g, 83.33%) and PDS (35.90 ± 18.169 mm3, 0.77 ± 0.398 g, 83.33%). Although tumour volume initially declined, progression was observed at later stages, emphasizing the need for optimizing nanoparticle stability, sustained drug release, and resistance mitigation strategies. Overall, FF-NLCs exhibit superior therapeutic potential, enabling a 1.25-fold increase in lung carcinoma treatment efficacy over conventional drug solutions.