Development of PLGA-SPC3 functionalized gefitinib mesoporous silica nano-scaffolds for breast cancer targeting: biodistribution and cytotoxicity analysis

The exploration of novel carriers for cancer treatments is on the rise, as drugs are often hindered by ineffective delivery. In the present study, Mesoporous silica nano scaffolds were developed by a novel heat assisted hydrolysis (HAH) technique, and were functionalized using PLGA. These carriers were further loaded with nanosized Gefitinib (GTB). The surface properties of MSNs (GTB-PEG-PLGA-MSN) were enhanced using 1-oleoyl-2-hydroxy-sn-glycero-3-phosphocholine (SPC3). The MSNs were characterized for pore volume, particle size, zeta potential (ZP), surface area, entrapment efficiency (%EE), and drug content. The <i>in vitro</i> drug release kinetics, cytotoxicity analysis, and <i>in vivo</i> biodistribution studies were performed in optimized MSN using Albino Wistar rats. The result shows an increase in surface area, pore volume, %EE, and drug loading in MSN. <i>In vitro</i> cytotoxicity of optimized F5-GTB-PEG-PLGA-SPC3-MSN demonstrated a higher antitumor activity (43.84 ± 0.63%, <i>p <</i> 0.05) in comparison to free drug. A higher GTB was detected in the liver (29,415 ± 126 ng) indicating significant biodistribution (<i>p</i> > 0.05). The <i>in vitro</i> studies in the MCF-7 cell line signify an increase in cell viability demonstrating its efficacy in breast cancer. Optimized F5-GTB-PEG-PLGA-SPC3-MSN offers improved cellular uptake, biodistribution, and higher antitumor suppression with less toxicity. To conclude, the HAH technique produced stable MSNs, and PLGA-SPC3 functionalized MSN nano scaffolds could be an ideal carrier for cancer drug delivery.