Folate receptor-targeted PLGA-PEG nanoparticles for enhancing the activity of genistein in ovarian cancer

AbstractGenistein (GEN), a natural isoflavone possesses a wide range of pharmacological properties and nutraceutical applications. GEN has been studied for its anticancer activity against different types of cancers, but its use in clinical practice is limited due to its low water solubility, rapid m...

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Main Authors: Arjun Patra, Swaha Satpathy, Pradeep K. Naik, Mohsin Kazi, Muhammad Delwar Hussain
Format: Article
Language:English
Published: Taylor & Francis Group 2022-12-01
Series:Artificial Cells, Nanomedicine, and Biotechnology
Subjects:
Online Access:https://www.tandfonline.com/doi/10.1080/21691401.2022.2118758
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author Arjun Patra
Swaha Satpathy
Pradeep K. Naik
Mohsin Kazi
Muhammad Delwar Hussain
author_facet Arjun Patra
Swaha Satpathy
Pradeep K. Naik
Mohsin Kazi
Muhammad Delwar Hussain
author_sort Arjun Patra
collection DOAJ
description AbstractGenistein (GEN), a natural isoflavone possesses a wide range of pharmacological properties and nutraceutical applications. GEN has been studied for its anticancer activity against different types of cancers, but its use in clinical practice is limited due to its low water solubility, rapid metabolism and excretion, lack of cancer cell targeting and poor bioavailability. In the present study, we investigated folate receptor-targeted and PEGylated poly(lactide-co-glycolide) nanoparticles (PLGA-PEG-FA NPs) containing GEN for targeted delivery to ovarian cancer cells. PLGA-PEG and PLGA-PEG-FA polymer conjugates were synthesized and characterized. Nano-precipitation method was employed for the fabrication of NPs of PLGA, PLGA-PEG and PLGA-PEG-FA containing GEN. GEN containing PLGA-PEG and PLGA-PEG-FA NPs prepared were small (104.17 ± 1.61 and 125.41 ± 3.11 nm, respectively) and exhibited sustained release of GEN for around six days. Folate-decorated PLGA-PEG NPs showed increased cellular uptake in comparison to non-targeted PLGA-PEG NPs. The GEN containing PLGA-PEG-FA NPs showed superior anticancer activity than non-targeted PLGA and PLGA-PEG NPs in folate receptor-overexpressing ovarian cancer cell line, SKOV-3. The IC50 of GEN, GEN encapsulated NPs of PLGA, PLGA-PEG and PLGA-PEG-FA were 51.48, 26.70, 23.43 and 11.98 µg/ml, respectively. Folate-targeted PLGA nanoparticles could be developed for potential target-specific delivery of GEN in the treatment of ovarian cancer.
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spelling doaj.art-5b125760da3b40dd86a9fd4e536e205f2022-12-22T04:24:24ZengTaylor & Francis GroupArtificial Cells, Nanomedicine, and Biotechnology2169-14012169-141X2022-12-0150122823910.1080/21691401.2022.2118758Folate receptor-targeted PLGA-PEG nanoparticles for enhancing the activity of genistein in ovarian cancerArjun Patra0Swaha Satpathy1Pradeep K. Naik2Mohsin Kazi3Muhammad Delwar Hussain4Department of Pharmaceutical & Biomedical Sciences, College of Pharmacy, California Health Sciences University, Clovis, CA, USADepartment of Pharmaceutical & Biomedical Sciences, College of Pharmacy, California Health Sciences University, Clovis, CA, USADepartment of Biotechnology and Bioinformatics, Sambalpur University, Sambalpur, IndiaDepartment of Pharmaceutics, College of Pharmacy, POBOX-2457, King Saud University, Riyadh, Saudi ArabiaDepartment of Pharmaceutical & Biomedical Sciences, College of Pharmacy, California Health Sciences University, Clovis, CA, USAAbstractGenistein (GEN), a natural isoflavone possesses a wide range of pharmacological properties and nutraceutical applications. GEN has been studied for its anticancer activity against different types of cancers, but its use in clinical practice is limited due to its low water solubility, rapid metabolism and excretion, lack of cancer cell targeting and poor bioavailability. In the present study, we investigated folate receptor-targeted and PEGylated poly(lactide-co-glycolide) nanoparticles (PLGA-PEG-FA NPs) containing GEN for targeted delivery to ovarian cancer cells. PLGA-PEG and PLGA-PEG-FA polymer conjugates were synthesized and characterized. Nano-precipitation method was employed for the fabrication of NPs of PLGA, PLGA-PEG and PLGA-PEG-FA containing GEN. GEN containing PLGA-PEG and PLGA-PEG-FA NPs prepared were small (104.17 ± 1.61 and 125.41 ± 3.11 nm, respectively) and exhibited sustained release of GEN for around six days. Folate-decorated PLGA-PEG NPs showed increased cellular uptake in comparison to non-targeted PLGA-PEG NPs. The GEN containing PLGA-PEG-FA NPs showed superior anticancer activity than non-targeted PLGA and PLGA-PEG NPs in folate receptor-overexpressing ovarian cancer cell line, SKOV-3. The IC50 of GEN, GEN encapsulated NPs of PLGA, PLGA-PEG and PLGA-PEG-FA were 51.48, 26.70, 23.43 and 11.98 µg/ml, respectively. Folate-targeted PLGA nanoparticles could be developed for potential target-specific delivery of GEN in the treatment of ovarian cancer.https://www.tandfonline.com/doi/10.1080/21691401.2022.2118758Genisteinovarian cancerfolate receptor targetingPLGAcellular internalization
spellingShingle Arjun Patra
Swaha Satpathy
Pradeep K. Naik
Mohsin Kazi
Muhammad Delwar Hussain
Folate receptor-targeted PLGA-PEG nanoparticles for enhancing the activity of genistein in ovarian cancer
Artificial Cells, Nanomedicine, and Biotechnology
Genistein
ovarian cancer
folate receptor targeting
PLGA
cellular internalization
title Folate receptor-targeted PLGA-PEG nanoparticles for enhancing the activity of genistein in ovarian cancer
title_full Folate receptor-targeted PLGA-PEG nanoparticles for enhancing the activity of genistein in ovarian cancer
title_fullStr Folate receptor-targeted PLGA-PEG nanoparticles for enhancing the activity of genistein in ovarian cancer
title_full_unstemmed Folate receptor-targeted PLGA-PEG nanoparticles for enhancing the activity of genistein in ovarian cancer
title_short Folate receptor-targeted PLGA-PEG nanoparticles for enhancing the activity of genistein in ovarian cancer
title_sort folate receptor targeted plga peg nanoparticles for enhancing the activity of genistein in ovarian cancer
topic Genistein
ovarian cancer
folate receptor targeting
PLGA
cellular internalization
url https://www.tandfonline.com/doi/10.1080/21691401.2022.2118758
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