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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Taylor & Francis Group
2022-12-01
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Series: | Artificial Cells, Nanomedicine, and Biotechnology |
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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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issn | 2169-1401 2169-141X |
language | English |
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publishDate | 2022-12-01 |
publisher | Taylor & Francis Group |
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series | Artificial Cells, Nanomedicine, and Biotechnology |
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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