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<p>In recent years, the application of lipid emulsions in drug delivery has gained significant interest among researchers. Pazopanib is a USFDA-approved second-generation potent VEGF receptor inhibitor, acting against angiogenesis to treat various cancers. However, severe hepatic metabolism and low oral bioavailability limit its clinical applications. This study thereby aims to develop and optimize pazopanib incorporated lipid emulsion for treating non-small cell lung cancer by parenteral administration. The nanoemulsion was developed, optimized, and analyzed for its physicochemical characteristics such as droplet size, zeta potential, polydispersity index, drug assay, % drug entrapment, and morphology. The QbD/DoE tools were utilized to achieve the desired CQAs, including maximum entrapment (&gt; 90%) and droplet size (&lt; 200&#xa0;nm). The average droplet size, PDI, and zeta potential were found to be 158.5&#xa0;nm, 0.230, and − 51.9 mV, respectively. The in vitro release demonstrated a biphasic profile, with 22.41% drug release at 0.5&#xa0;h and a cumulative release of 97.28% at 24&#xa0;h. The lipid emulsion was subjected to stability studies, where it demonstrated stable behavior for up to 3 months under accelerated and long-term stability conditions. The efficacy of the developed formulations was further evaluated in vitro using A549 lung cancer cell lines, showing an improved effectiveness of pazopanib-loaded lipid emulsion with enhanced cell absorption and anticancer activity. The formulation significantly reduced IC<sub>50</sub> (3.9 µM) and induced 46.4% apoptosis in the cancer cells relative to the free drug. These promising results suggest the potential of the developed therapeutic system for treating lung cancer.</p> Graphical Abstract <p></p>

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Development and Optimization of Lipid Emulsion Based Therapeutic System Targeting Vascular Endothelial Growth Factor Receptor for Non-small Cell Lung Cancer Treatment

  • 期刊论文

  • 发表日期：

    2026年3月17日

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  • Sonali Singh,
  • Kanan Panchal,
  • Vishal Babasaheb Galave,
  • Ashutosh Mahale,
  • Onkar Prakash Kulkarni,
  • Akash Chaurasiya

摘要

In recent years, the application of lipid emulsions in drug delivery has gained significant interest among researchers. Pazopanib is a USFDA-approved second-generation potent VEGF receptor inhibitor, acting against angiogenesis to treat various cancers. However, severe hepatic metabolism and low oral bioavailability limit its clinical applications. This study thereby aims to develop and optimize pazopanib incorporated lipid emulsion for treating non-small cell lung cancer by parenteral administration. The nanoemulsion was developed, optimized, and analyzed for its physicochemical characteristics such as droplet size, zeta potential, polydispersity index, drug assay, % drug entrapment, and morphology. The QbD/DoE tools were utilized to achieve the desired CQAs, including maximum entrapment (> 90%) and droplet size (< 200 nm). The average droplet size, PDI, and zeta potential were found to be 158.5 nm, 0.230, and − 51.9 mV, respectively. The in vitro release demonstrated a biphasic profile, with 22.41% drug release at 0.5 h and a cumulative release of 97.28% at 24 h. The lipid emulsion was subjected to stability studies, where it demonstrated stable behavior for up to 3 months under accelerated and long-term stability conditions. The efficacy of the developed formulations was further evaluated in vitro using A549 lung cancer cell lines, showing an improved effectiveness of pazopanib-loaded lipid emulsion with enhanced cell absorption and anticancer activity. The formulation significantly reduced IC50 (3.9 µM) and induced 46.4% apoptosis in the cancer cells relative to the free drug. These promising results suggest the potential of the developed therapeutic system for treating lung cancer.

Graphical Abstract