Synthesis And In Vitro Evaluation of Radiolabeled Quercetin-Loaded Polymeric Nanoparticles

Project no. 32843 · Status: Kapanmış (Yayın bekleniyor) · 2025

Summary

<p>Breast&nbsp;cancer&nbsp;is&nbsp;the&nbsp;leading&nbsp;cause&nbsp;of&nbsp;cancer&nbsp;mortality&nbsp;among&nbsp;women&nbsp;worldwide.&nbsp;While&nbsp;numerous&nbsp; treatment&nbsp;options&nbsp;exist,&nbsp;the&nbsp;development&nbsp;of&nbsp;drug&nbsp;delivery&nbsp;systems&nbsp;is&nbsp;crucial&nbsp;due&nbsp;to&nbsp;the&nbsp;high&nbsp;toxicity&nbsp;of&nbsp;these&nbsp;treatments&nbsp;to&nbsp;healthy&nbsp;tissues.&nbsp;Nanotechnology&nbsp;based&nbsp;drug&nbsp;delivery&nbsp;systems,&nbsp;particularly&nbsp;PLGA&nbsp;(polylactic-co-glycolic&nbsp;acid)&nbsp;polymeric&nbsp;nanoparticles,&nbsp;stand&nbsp;out&nbsp;due&nbsp;to&nbsp;their&nbsp;biocompatibility&nbsp;and&nbsp;biodegradability.&nbsp;Quercetin,&nbsp;a&nbsp;molecule&nbsp;with&nbsp;limited&nbsp;bioavailability,&nbsp;is&nbsp;a&nbsp;component&nbsp;with&nbsp;potential&nbsp;effects&nbsp;on&nbsp;cancer&nbsp;cells.&nbsp;</p><p>In&nbsp;this&nbsp;thesis,&nbsp;quercetin&nbsp;loaded&nbsp;PLGA&nbsp;nanoparticles&nbsp;were&nbsp;synthesized&nbsp;and&nbsp;radiolabeled&nbsp;with&nbsp;Tc-99m.&nbsp;The&nbsp;nanoparticles&nbsp;were&nbsp;synthesized&nbsp;using&nbsp;a&nbsp;single&nbsp;emulsion&nbsp;solvent&nbsp;evaporation&nbsp;method.&nbsp;Characterization&nbsp;studies&nbsp;of&nbsp;the&nbsp;nanoparticles&nbsp;were&nbsp;performed&nbsp;using&nbsp;Dynamic&nbsp;Light&nbsp;Scattering&nbsp;(DLS),&nbsp;Zeta&nbsp;Potential,&nbsp;Scanning&nbsp;Electron&nbsp;Microscopy&nbsp;(SEM)&nbsp;and&nbsp;Energy&nbsp;Dispersive&nbsp;X-ray&nbsp;Fluorescence&nbsp;Spectrometry&nbsp;(EDX)&nbsp;analyses.&nbsp;Tc-99m&nbsp;radiolabeling&nbsp;of&nbsp;quercetin&nbsp;loaded&nbsp;PLGA&nbsp;nanoparticles&nbsp;was&nbsp;carried&nbsp;out&nbsp;by&nbsp;the&nbsp;SnCl2&nbsp;reduction&nbsp;method.&nbsp;Quality&nbsp;control&nbsp;studies&nbsp;of&nbsp;radiolabeled&nbsp;nanoparticles&nbsp;were&nbsp;performed&nbsp;using&nbsp;thin&nbsp;layer&nbsp;radiochromatography&nbsp;(TLRC).&nbsp;</p><p>The&nbsp;average&nbsp;size&nbsp;of&nbsp;quercetin&nbsp;loaded&nbsp;PLGA&nbsp;nanoparticles&nbsp;was&nbsp;found&nbsp;to&nbsp;be&nbsp;191&nbsp;±5&nbsp;nm&nbsp;and&nbsp;polydispersity&nbsp;index&nbsp;was&nbsp;0.049.&nbsp;SEM&nbsp;analysis&nbsp;revealed&nbsp;that&nbsp;the&nbsp;nanoparticles&nbsp;were&nbsp;synthesized&nbsp;as&nbsp;morphologically&nbsp;spherical&nbsp;and&nbsp;approximately&nbsp;143&nbsp;±21&nbsp;nm&nbsp;in&nbsp;size.&nbsp;The&nbsp;loading&nbsp;efficiency&nbsp;of&nbsp;quercetin&nbsp;compound&nbsp;onto&nbsp;PLGA&nbsp;nanoparticles&nbsp;was&nbsp;found&nbsp;to&nbsp;be&nbsp;40&nbsp;±&nbsp;2&nbsp;%.&nbsp;To&nbsp;evaluate&nbsp;the&nbsp;drug&nbsp;release&nbsp;profile&nbsp;of&nbsp;the&nbsp;synthesized&nbsp;quercetin&nbsp;loaded&nbsp;PLGA&nbsp;nanoparticles,&nbsp;experiments&nbsp;were&nbsp;carried&nbsp;out&nbsp;at&nbsp;pH&nbsp;4&nbsp;and&nbsp;pH&nbsp;7.&nbsp;After&nbsp;48&nbsp;hours,&nbsp;the&nbsp;drug&nbsp;release&nbsp;was&nbsp;66.19%&nbsp;at&nbsp;pH&nbsp;4,&nbsp;whereas&nbsp;it&nbsp;was&nbsp;54.10%&nbsp;at&nbsp;pH&nbsp;7.</p><p>The&nbsp;bioactivity&nbsp;of&nbsp;quercetin&nbsp;loaded&nbsp;PLGA&nbsp;nanoparticles&nbsp;was&nbsp;investigated&nbsp;in&nbsp;vitro&nbsp;on&nbsp;MCF-7&nbsp;and&nbsp;MDA-MB-231&nbsp;breast&nbsp;cancer&nbsp;cell&nbsp;lines.&nbsp;Cytotoxicity&nbsp;analyses&nbsp;revealed&nbsp;that&nbsp;the&nbsp;nanoparticles&nbsp;were&nbsp;more&nbsp;effective&nbsp;on&nbsp;the&nbsp;MCF-7&nbsp;cell&nbsp;line.&nbsp;Incorporation&nbsp;studies&nbsp;have&nbsp;shown&nbsp;that&nbsp;radiolabeled&nbsp;quercetin-loaded&nbsp;PLGA&nbsp;nanoparticles&nbsp;with&nbsp;Tc-99m&nbsp;exhibit&nbsp;higher&nbsp;uptake&nbsp;than&nbsp;free&nbsp;Tc-99m&nbsp;in&nbsp;the&nbsp;MDA-MB-231&nbsp;and&nbsp;MCF-7&nbsp;cell&nbsp;lines.</p><p><strong>Keywords:</strong>&nbsp;Quercetin,&nbsp;Polymer&nbsp;Nanoparticles,&nbsp;Technetium-99m,&nbsp;Radiolabeling,&nbsp;Breast&nbsp;Cancer,&nbsp;Cell&nbsp;Culture,&nbsp;Nanotechnology</p>

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