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

Abstract

Aim: 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.

Materials & methods: 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 in vitro characterization, Ex vivo and in vivo biodistribution studies. Moreover, female Wistar rats were used in this study.

Results: 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.

Conclusion: This study showed a promising targeted strategy for effective and safer breast cancer treatment.