Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles
Fisetin (FST), a potent anticancer phytoconstituent, exhibits poor aqueous solubility and hence poor bioavailability. The aim of the present study is to improve the oral bioavailability of FST by encapsulating into PLGA NPs (poly-lactide-co-glycolic acid nanoparticles) as a complex of HPβCD (hydroxy...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2017-01-01
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| Series: | Drug Delivery |
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| Online Access: | http://dx.doi.org/10.1080/10717544.2016.1245366 |
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| author | Amrita Kadari Sagarika Gudem Hitesh Kulhari Murali Mohan Bhandi Roshan M. Borkar Venkata Ramana Murthy Kolapalli Ramakrishna Sistla |
| author_facet | Amrita Kadari Sagarika Gudem Hitesh Kulhari Murali Mohan Bhandi Roshan M. Borkar Venkata Ramana Murthy Kolapalli Ramakrishna Sistla |
| author_sort | Amrita Kadari |
| collection | DOAJ |
| description | Fisetin (FST), a potent anticancer phytoconstituent, exhibits poor aqueous solubility and hence poor bioavailability. The aim of the present study is to improve the oral bioavailability of FST by encapsulating into PLGA NPs (poly-lactide-co-glycolic acid nanoparticles) as a complex of HPβCD (hydroxyl propyl beta cyclodextrin) and to assess its anti-cancer activity against breast cancer cells. FST-HPβCD inclusion complex (FHIC) was prepared and the supramolecular complex formation was characterized by FTIR, DSC, PXRD and 1H NMR. FHIC encapsulated PLGA nanoparticles (FHIC-PNP) were prepared and were studied for in vitro anticancer activity, cellular uptake, apoptosis and reactive oxygen species generation in MCF-7 human breast cancer cells. Comparative bioavailability of FST was determined after oral administration in C57BL6 mice as pure FST and FHIC-PNP. The results revealed that FHIC-PNP not only enhanced the anti-cancer activity and apoptosis of FST against MCF-7 cells but also improved its oral bioavailability, as demonstrated by increased peak plasma concentration and total drug absorbed. |
| first_indexed | 2024-12-22T00:50:03Z |
| format | Article |
| id | doaj.art-a0431b8071df454495c3ca95f48956a6 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-22T00:50:03Z |
| publishDate | 2017-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-a0431b8071df454495c3ca95f48956a62022-12-21T18:44:28ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642017-01-0124122423210.1080/10717544.2016.12453661245366Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticlesAmrita Kadari0Sagarika Gudem1Hitesh Kulhari2Murali Mohan Bhandi3Roshan M. Borkar4Venkata Ramana Murthy Kolapalli5Ramakrishna Sistla6Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical TechnologyMedicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical TechnologyMedicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical TechnologyNational Centre for Mass Spectrometry, Indian Institute of Chemical TechnologyNational Centre for Mass Spectrometry, Indian Institute of Chemical TechnologyA.U. College of Pharmaceutical Sciences, Andhra UniversityMedicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical TechnologyFisetin (FST), a potent anticancer phytoconstituent, exhibits poor aqueous solubility and hence poor bioavailability. The aim of the present study is to improve the oral bioavailability of FST by encapsulating into PLGA NPs (poly-lactide-co-glycolic acid nanoparticles) as a complex of HPβCD (hydroxyl propyl beta cyclodextrin) and to assess its anti-cancer activity against breast cancer cells. FST-HPβCD inclusion complex (FHIC) was prepared and the supramolecular complex formation was characterized by FTIR, DSC, PXRD and 1H NMR. FHIC encapsulated PLGA nanoparticles (FHIC-PNP) were prepared and were studied for in vitro anticancer activity, cellular uptake, apoptosis and reactive oxygen species generation in MCF-7 human breast cancer cells. Comparative bioavailability of FST was determined after oral administration in C57BL6 mice as pure FST and FHIC-PNP. The results revealed that FHIC-PNP not only enhanced the anti-cancer activity and apoptosis of FST against MCF-7 cells but also improved its oral bioavailability, as demonstrated by increased peak plasma concentration and total drug absorbed.http://dx.doi.org/10.1080/10717544.2016.1245366fisetinhyroxypropyl β-cyclodextrininclusion complexplga nanoparticlesanticancer activityoral bioavailability |
| spellingShingle | Amrita Kadari Sagarika Gudem Hitesh Kulhari Murali Mohan Bhandi Roshan M. Borkar Venkata Ramana Murthy Kolapalli Ramakrishna Sistla Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles Drug Delivery fisetin hyroxypropyl β-cyclodextrin inclusion complex plga nanoparticles anticancer activity oral bioavailability |
| title | Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles |
| title_full | Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles |
| title_fullStr | Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles |
| title_full_unstemmed | Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles |
| title_short | Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles |
| title_sort | enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with hpβcd in polymeric nanoparticles |
| topic | fisetin hyroxypropyl β-cyclodextrin inclusion complex plga nanoparticles anticancer activity oral bioavailability |
| url | http://dx.doi.org/10.1080/10717544.2016.1245366 |
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