Preparation and characterization of quercetin-loaded folic acid TPGS micelles against MCF-7 breast cancer cell line

Breast cancer is one of the common cancers in the world and possibility of this disease among women is higher. In recent years, variety of nanoparticles have been discovered and synthesized in such a way to increase the therapeutic efficiency of drugs through targeted area of tumor cells without cau...

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Main Author: Ibharm, Siti Fatimah
Format: Thesis
Language:English
Published: 2022
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Online Access:http://eprints.utm.my/id/eprint/101612/1/SitiFatimahIbharmMSBME2022.pdf
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spelling my-utm-ep.1016122023-07-03T02:37:43Z Preparation and characterization of quercetin-loaded folic acid TPGS micelles against MCF-7 breast cancer cell line 2022 Ibharm, Siti Fatimah Q Science (General) TP Chemical technology Breast cancer is one of the common cancers in the world and possibility of this disease among women is higher. In recent years, variety of nanoparticles have been discovered and synthesized in such a way to increase the therapeutic efficiency of drugs through targeted area of tumor cells without causing any harm towards healthy tissues. Quercetin is a polyphenolic compound that exists in plants, fruits, and vegetables and has showed numerous promising health benefits. However, therapeutic applications of quercetin are limited due to its low water solubility and poor bioavailability. The main objectives of this study were to synthesize quercetin loaded folic acid d-α-tocopheryl polyethylene glycol succinate (TPGS) polymeric micelles (QUE-FA-TPGS-PMs), to characterize the physicochemical properties of QUE-FA-TPGS-PMs and to analyze the in vitro cytotoxicity of QUE-FA-TPGS-PMs against MCF-7 breast cancer cells. The TPGS micelles containing quercetin were prepared by thin film hydration method and were characterized for their particle size, polydispersity (PDI), encapsulation efficiency (EE), drug loading (DL), critical micelle concentration (CMC), in vitro drug release, and in vitro cytotoxicity. Particle size and polydispersity were analyzed using a zetasizer while surface morphology was determined by transmission electron microscopy (TEM). The EE and DL were determined by ultraviolet-visible (UV-Vis) spectrophotometry while the in vitro drug release studies of micelles were carried out by dialysis bag diffusion method. The in vitro cytotoxicity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay where the cell viability was measured after 24, 48 and 72 h of incubations. It was observed that the average size of both QUE-FA-TPGS-PMs were between 118.53 nm and 651.55 nm. This indicates that these PMs can escape reticuloendothelial system (RES) and have longer circulation in blood. The PDI values were recorded between 0.23 and 0.67 revealed that these PMs were stable. From the TEM results, it can be observed that the QUE-FA-TPGSPMs were in a spherical shape. The QUE-FA-TPGS-10.0 displayed high EE of 99.80% with low CMC of 0.008%. The lower value of CMC indicates greater stability upon dilution. After 96 h, drug release from the QUE-FA-TPGS-10.0 reached 39.42% maximum cumulative percentage of quercetin release. This slower release of quercetin indicates the QUE-FA-TPGS-10.0 was able to be sustainably released. The QUE-FA-TPGS-10.0-PMs exhibited the lowest cell viability of 23.6% against MCF-7 cells after 72 h of incubation. From the findings, it can be concluded that quercetin was successfully loaded inside PMs. These QUE-FA-TPGS-PMs were able to specifically target MCF-7 cells, delivered quercetin inside MCF-7 cells and cause cytotoxicity, thus can supports their role as a new targeted drug delivery system against MCF-7 breast cancer cells. 2022 Thesis http://eprints.utm.my/id/eprint/101612/ http://eprints.utm.my/id/eprint/101612/1/SitiFatimahIbharmMSBME2022.pdf application/pdf en public http://dms.library.utm.my:8080/vital/access/manager/Repository/vital:149048 masters Universiti Teknologi Malaysia, Faculty of Engineering - School of Biomedical Engineering & Health Sciences Faculty of Engineering - School of Biomedical Engineering & Health Sciences
institution Universiti Teknologi Malaysia
collection UTM Institutional Repository
language English
topic Q Science (General)
TP Chemical technology
spellingShingle Q Science (General)
TP Chemical technology
Ibharm, Siti Fatimah
Preparation and characterization of quercetin-loaded folic acid TPGS micelles against MCF-7 breast cancer cell line
description Breast cancer is one of the common cancers in the world and possibility of this disease among women is higher. In recent years, variety of nanoparticles have been discovered and synthesized in such a way to increase the therapeutic efficiency of drugs through targeted area of tumor cells without causing any harm towards healthy tissues. Quercetin is a polyphenolic compound that exists in plants, fruits, and vegetables and has showed numerous promising health benefits. However, therapeutic applications of quercetin are limited due to its low water solubility and poor bioavailability. The main objectives of this study were to synthesize quercetin loaded folic acid d-α-tocopheryl polyethylene glycol succinate (TPGS) polymeric micelles (QUE-FA-TPGS-PMs), to characterize the physicochemical properties of QUE-FA-TPGS-PMs and to analyze the in vitro cytotoxicity of QUE-FA-TPGS-PMs against MCF-7 breast cancer cells. The TPGS micelles containing quercetin were prepared by thin film hydration method and were characterized for their particle size, polydispersity (PDI), encapsulation efficiency (EE), drug loading (DL), critical micelle concentration (CMC), in vitro drug release, and in vitro cytotoxicity. Particle size and polydispersity were analyzed using a zetasizer while surface morphology was determined by transmission electron microscopy (TEM). The EE and DL were determined by ultraviolet-visible (UV-Vis) spectrophotometry while the in vitro drug release studies of micelles were carried out by dialysis bag diffusion method. The in vitro cytotoxicity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay where the cell viability was measured after 24, 48 and 72 h of incubations. It was observed that the average size of both QUE-FA-TPGS-PMs were between 118.53 nm and 651.55 nm. This indicates that these PMs can escape reticuloendothelial system (RES) and have longer circulation in blood. The PDI values were recorded between 0.23 and 0.67 revealed that these PMs were stable. From the TEM results, it can be observed that the QUE-FA-TPGSPMs were in a spherical shape. The QUE-FA-TPGS-10.0 displayed high EE of 99.80% with low CMC of 0.008%. The lower value of CMC indicates greater stability upon dilution. After 96 h, drug release from the QUE-FA-TPGS-10.0 reached 39.42% maximum cumulative percentage of quercetin release. This slower release of quercetin indicates the QUE-FA-TPGS-10.0 was able to be sustainably released. The QUE-FA-TPGS-10.0-PMs exhibited the lowest cell viability of 23.6% against MCF-7 cells after 72 h of incubation. From the findings, it can be concluded that quercetin was successfully loaded inside PMs. These QUE-FA-TPGS-PMs were able to specifically target MCF-7 cells, delivered quercetin inside MCF-7 cells and cause cytotoxicity, thus can supports their role as a new targeted drug delivery system against MCF-7 breast cancer cells.
format Thesis
qualification_level Master's degree
author Ibharm, Siti Fatimah
author_facet Ibharm, Siti Fatimah
author_sort Ibharm, Siti Fatimah
title Preparation and characterization of quercetin-loaded folic acid TPGS micelles against MCF-7 breast cancer cell line
title_short Preparation and characterization of quercetin-loaded folic acid TPGS micelles against MCF-7 breast cancer cell line
title_full Preparation and characterization of quercetin-loaded folic acid TPGS micelles against MCF-7 breast cancer cell line
title_fullStr Preparation and characterization of quercetin-loaded folic acid TPGS micelles against MCF-7 breast cancer cell line
title_full_unstemmed Preparation and characterization of quercetin-loaded folic acid TPGS micelles against MCF-7 breast cancer cell line
title_sort preparation and characterization of quercetin-loaded folic acid tpgs micelles against mcf-7 breast cancer cell line
granting_institution Universiti Teknologi Malaysia, Faculty of Engineering - School of Biomedical Engineering & Health Sciences
granting_department Faculty of Engineering - School of Biomedical Engineering & Health Sciences
publishDate 2022
url http://eprints.utm.my/id/eprint/101612/1/SitiFatimahIbharmMSBME2022.pdf
_version_ 1776100738119761920