Development and evaluation of luteolin loaded pegylated bilosome: optimization, in vitro characterization, and cytotoxicity study
The present research was aimed to develop luteolin (LL) loaded pegylated bilosomes (PG-BLs) for oral delivery. The luteolin bilosomes (BLs) were prepared by the thin-film hydration method and further optimized by the Box–Behnken design (four-factors at three-levels). The prepared LL-BLs were evaluat...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2021-01-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/10717544.2021.2008055 |
| _version_ | 1819279602245173248 |
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| author | Ameeduzzafar Zafar Nabil K. Alruwaili Syed Sarim Imam Omar Awad Alsaidan Mohd Yasir Mohammed M. Ghoneim Sultan Alshehri Md. Khalid Anwer Alanood S. Almurshedi Abdullah S. Alanazi |
| author_facet | Ameeduzzafar Zafar Nabil K. Alruwaili Syed Sarim Imam Omar Awad Alsaidan Mohd Yasir Mohammed M. Ghoneim Sultan Alshehri Md. Khalid Anwer Alanood S. Almurshedi Abdullah S. Alanazi |
| author_sort | Ameeduzzafar Zafar |
| collection | DOAJ |
| description | The present research was aimed to develop luteolin (LL) loaded pegylated bilosomes (PG-BLs) for oral delivery. The luteolin bilosomes (BLs) were prepared by the thin-film hydration method and further optimized by the Box–Behnken design (four-factors at three-levels). The prepared LL-BLs were evaluated for vesicle size (VS), PDI, zeta potential (ZP), and entrapment efficiency to select the optimized formulation. The optimized formulation was further assessed for surface morphology, drug release, gut permeation, antioxidant, and antimicrobial study. The cytotoxicity study was conducted on breast cancer cell lines (MDA-MB-231 and MCF7). The optimized formulation LL-PG-BLs-opt exhibited a VS of 252.24 ± 3.54 nm, PDI of 0.24, ZP of −32 mV with an encapsulation efficiency of 75.05 ± 0.65%. TEM study revealed spherical shape vesicles without aggregation. The DSC and XRD results revealed that LL was encapsulated into a PG-BLs matrix. LL-PG-BLs-opt exhibited a biphasic release pattern as well as significantly high permeation (p<.05) was achieved vis-a-vis LL-BL-opt and LL dispersion. The antioxidant activity result revealed 70.31 ± 3.22%, 83.76 ± 2.56%, and 96.87 ± 2.11% from LL-dispersion, LL-BLs-opt, and LL-PG-BLs-opt, respectively. Furthermore, LL-PG-BLs-opt exhibited high cell viability on both cell lines than LL-BL-opt and pure LL. The IC50 value was found to be 390 µM and 510 µM against MCF7 and MDA-MB-231 cancer cells, respectively. The antimicrobial activity result exhibited LL-PG-BLs-opt had better antibacterial activity than pure LL against Staphylococcus aureus and Escherichia coli. Hence, PG-BLs might provide an efficient nano oral delivery for the management of the different diseases. |
| first_indexed | 2024-12-24T00:30:31Z |
| format | Article |
| id | doaj.art-8da2e3bfcd574daa861aa28d14fc7502 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-24T00:30:31Z |
| publishDate | 2021-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-8da2e3bfcd574daa861aa28d14fc75022022-12-21T17:24:17ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642021-01-012812562257310.1080/10717544.2021.20080552008055Development and evaluation of luteolin loaded pegylated bilosome: optimization, in vitro characterization, and cytotoxicity studyAmeeduzzafar Zafar0Nabil K. Alruwaili1Syed Sarim Imam2Omar Awad Alsaidan3Mohd Yasir4Mohammed M. Ghoneim5Sultan Alshehri6Md. Khalid Anwer7Alanood S. Almurshedi8Abdullah S. Alanazi9Department of Pharmaceutics, College of Pharmacy, Jouf UniversityDepartment of Pharmaceutics, College of Pharmacy, Jouf UniversityDepartment of Pharmaceutics, College of Pharmacy, King Saud UniversityDepartment of Pharmaceutics, College of Pharmacy, Jouf UniversityDepartment of Pharmacy, College of Health Sciences, Arsi UniversityDepartment of Pharmacy Practice, College of Pharmacy, AlMaarefa UniversityDepartment of Pharmaceutics, College of Pharmacy, King Saud UniversityDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz UniversityDepartment of Pharmaceutics, College of Pharmacy, King Saud UniversityDepartment of Clinical Pharmacy, College of Pharmacy, Jouf UniversityThe present research was aimed to develop luteolin (LL) loaded pegylated bilosomes (PG-BLs) for oral delivery. The luteolin bilosomes (BLs) were prepared by the thin-film hydration method and further optimized by the Box–Behnken design (four-factors at three-levels). The prepared LL-BLs were evaluated for vesicle size (VS), PDI, zeta potential (ZP), and entrapment efficiency to select the optimized formulation. The optimized formulation was further assessed for surface morphology, drug release, gut permeation, antioxidant, and antimicrobial study. The cytotoxicity study was conducted on breast cancer cell lines (MDA-MB-231 and MCF7). The optimized formulation LL-PG-BLs-opt exhibited a VS of 252.24 ± 3.54 nm, PDI of 0.24, ZP of −32 mV with an encapsulation efficiency of 75.05 ± 0.65%. TEM study revealed spherical shape vesicles without aggregation. The DSC and XRD results revealed that LL was encapsulated into a PG-BLs matrix. LL-PG-BLs-opt exhibited a biphasic release pattern as well as significantly high permeation (p<.05) was achieved vis-a-vis LL-BL-opt and LL dispersion. The antioxidant activity result revealed 70.31 ± 3.22%, 83.76 ± 2.56%, and 96.87 ± 2.11% from LL-dispersion, LL-BLs-opt, and LL-PG-BLs-opt, respectively. Furthermore, LL-PG-BLs-opt exhibited high cell viability on both cell lines than LL-BL-opt and pure LL. The IC50 value was found to be 390 µM and 510 µM against MCF7 and MDA-MB-231 cancer cells, respectively. The antimicrobial activity result exhibited LL-PG-BLs-opt had better antibacterial activity than pure LL against Staphylococcus aureus and Escherichia coli. Hence, PG-BLs might provide an efficient nano oral delivery for the management of the different diseases.http://dx.doi.org/10.1080/10717544.2021.2008055bilosomesbreast cancerbox–behnken’s designluteolinpegylated |
| spellingShingle | Ameeduzzafar Zafar Nabil K. Alruwaili Syed Sarim Imam Omar Awad Alsaidan Mohd Yasir Mohammed M. Ghoneim Sultan Alshehri Md. Khalid Anwer Alanood S. Almurshedi Abdullah S. Alanazi Development and evaluation of luteolin loaded pegylated bilosome: optimization, in vitro characterization, and cytotoxicity study Drug Delivery bilosomes breast cancer box–behnken’s design luteolin pegylated |
| title | Development and evaluation of luteolin loaded pegylated bilosome: optimization, in vitro characterization, and cytotoxicity study |
| title_full | Development and evaluation of luteolin loaded pegylated bilosome: optimization, in vitro characterization, and cytotoxicity study |
| title_fullStr | Development and evaluation of luteolin loaded pegylated bilosome: optimization, in vitro characterization, and cytotoxicity study |
| title_full_unstemmed | Development and evaluation of luteolin loaded pegylated bilosome: optimization, in vitro characterization, and cytotoxicity study |
| title_short | Development and evaluation of luteolin loaded pegylated bilosome: optimization, in vitro characterization, and cytotoxicity study |
| title_sort | development and evaluation of luteolin loaded pegylated bilosome optimization in vitro characterization and cytotoxicity study |
| topic | bilosomes breast cancer box–behnken’s design luteolin pegylated |
| url | http://dx.doi.org/10.1080/10717544.2021.2008055 |
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