Optimization, formulation, and characterization of multiavonoids-loaded flavanosome by bulk or sequential technique
This study involves adaptation of bulk or sequential technique to load multiple flavonoids in a single phytosome, which can be termed as "flavonosome". Three widely established and therapeutically valuable flavonoids, such as quercetin (Q), kaempferol (K), and apigenin (A), were quantified...
| Autores principales: | , , , , |
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| Formato: | Artículo |
| Lenguaje: | English |
| Publicado: |
Dove Medical Press
2016
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| Acceso en línea: | http://psasir.upm.edu.my/id/eprint/53459/1/Optimization%2C%20formulation%2C%20and%20characterization.pdf |
| _version_ | 1825930856819064832 |
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| author | Karthivashan, Govindarajan Masarudin, Mas Jaffri Kura, Aminu Umar Abas, Faridah Fakurazi, Sharida |
| author_facet | Karthivashan, Govindarajan Masarudin, Mas Jaffri Kura, Aminu Umar Abas, Faridah Fakurazi, Sharida |
| author_sort | Karthivashan, Govindarajan |
| collection | UPM |
| description | This study involves adaptation of bulk or sequential technique to load multiple flavonoids in a single phytosome, which can be termed as "flavonosome". Three widely established and therapeutically valuable flavonoids, such as quercetin (Q), kaempferol (K), and apigenin (A), were quantified in the ethyl acetate fraction of Moringa oleifera leaves extract and were commercially obtained and incorporated in a single flavonosome (QKA-phosphatidylcholine) through four different methods of synthesis - bulk (M1) and serialized (M2) co-sonication and bulk (M3) and sequential (M4) co-loading. The study also established an optimal formulation method based on screening the synthesized flavonosomes with respect to their size, charge, polydispersity index, morphology, drug-carrier interaction, antioxidant potential through in vitro 1,1-diphenyl-2-picrylhydrazyl kinetics, and cytotoxicity evaluation against human hepatoma cell line (HepaRG). Furthermore, entrapment and loading efficiency of flavonoids in the optimal flavonosome have been identified. Among the four synthesis methods, sequential loading technique has been optimized as the best method for the synthesis of QKA-phosphatidylcholine flavonosome, which revealed an average diameter of 375.93±33.61 nm, with a zeta potential of -39.07±3.55 mV, and the entrapment efficiency was >98% for all the flavonoids, whereas the drug-loading capacity of Q, K, and A was 31.63%±0.17%, 34.51%±2.07%, and 31.79%±0.01%, respectively. The in vitro 1,1-diphenyl-2-picrylhydrazyl kinetics of the flavonoids indirectly depicts the release kinetic behavior of the flavonoids from the carrier. The QKA-loaded flavonosome had no indication of toxicity toward human hepatoma cell line as shown by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide result, wherein even at the higher concentration of 200 µg/mL, the flavonosomes exert >85% of cell viability. These results suggest that sequential loading technique may be a promising nanodrug delivery system for loading multiflavonoids in a single entity with sustained activity as an antioxidant, hepatoprotective, and hepatosupplement candidate. |
| first_indexed | 2024-03-06T09:17:55Z |
| format | Article |
| id | upm.eprints-53459 |
| institution | Universiti Putra Malaysia |
| language | English |
| last_indexed | 2024-03-06T09:17:55Z |
| publishDate | 2016 |
| publisher | Dove Medical Press |
| record_format | dspace |
| spelling | upm.eprints-534592017-11-01T03:03:34Z http://psasir.upm.edu.my/id/eprint/53459/ Optimization, formulation, and characterization of multiavonoids-loaded flavanosome by bulk or sequential technique Karthivashan, Govindarajan Masarudin, Mas Jaffri Kura, Aminu Umar Abas, Faridah Fakurazi, Sharida This study involves adaptation of bulk or sequential technique to load multiple flavonoids in a single phytosome, which can be termed as "flavonosome". Three widely established and therapeutically valuable flavonoids, such as quercetin (Q), kaempferol (K), and apigenin (A), were quantified in the ethyl acetate fraction of Moringa oleifera leaves extract and were commercially obtained and incorporated in a single flavonosome (QKA-phosphatidylcholine) through four different methods of synthesis - bulk (M1) and serialized (M2) co-sonication and bulk (M3) and sequential (M4) co-loading. The study also established an optimal formulation method based on screening the synthesized flavonosomes with respect to their size, charge, polydispersity index, morphology, drug-carrier interaction, antioxidant potential through in vitro 1,1-diphenyl-2-picrylhydrazyl kinetics, and cytotoxicity evaluation against human hepatoma cell line (HepaRG). Furthermore, entrapment and loading efficiency of flavonoids in the optimal flavonosome have been identified. Among the four synthesis methods, sequential loading technique has been optimized as the best method for the synthesis of QKA-phosphatidylcholine flavonosome, which revealed an average diameter of 375.93±33.61 nm, with a zeta potential of -39.07±3.55 mV, and the entrapment efficiency was >98% for all the flavonoids, whereas the drug-loading capacity of Q, K, and A was 31.63%±0.17%, 34.51%±2.07%, and 31.79%±0.01%, respectively. The in vitro 1,1-diphenyl-2-picrylhydrazyl kinetics of the flavonoids indirectly depicts the release kinetic behavior of the flavonoids from the carrier. The QKA-loaded flavonosome had no indication of toxicity toward human hepatoma cell line as shown by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide result, wherein even at the higher concentration of 200 µg/mL, the flavonosomes exert >85% of cell viability. These results suggest that sequential loading technique may be a promising nanodrug delivery system for loading multiflavonoids in a single entity with sustained activity as an antioxidant, hepatoprotective, and hepatosupplement candidate. Dove Medical Press 2016 Article PeerReviewed application/pdf en http://psasir.upm.edu.my/id/eprint/53459/1/Optimization%2C%20formulation%2C%20and%20characterization.pdf Karthivashan, Govindarajan and Masarudin, Mas Jaffri and Kura, Aminu Umar and Abas, Faridah and Fakurazi, Sharida (2016) Optimization, formulation, and characterization of multiavonoids-loaded flavanosome by bulk or sequential technique. International Journal of Nanomedicine, 2016 (11). pp. 3417-3434. ISSN 1176-9114; ESSN: 1178-2013 https://www.dovepress.com/optimization-formulation-and-characterization-of-multiflavonoids-loade-peer-reviewed-article-IJN 10.2147/IJN.S112045 |
| spellingShingle | Karthivashan, Govindarajan Masarudin, Mas Jaffri Kura, Aminu Umar Abas, Faridah Fakurazi, Sharida Optimization, formulation, and characterization of multiavonoids-loaded flavanosome by bulk or sequential technique |
| title | Optimization, formulation, and characterization of multiavonoids-loaded flavanosome by bulk or sequential technique |
| title_full | Optimization, formulation, and characterization of multiavonoids-loaded flavanosome by bulk or sequential technique |
| title_fullStr | Optimization, formulation, and characterization of multiavonoids-loaded flavanosome by bulk or sequential technique |
| title_full_unstemmed | Optimization, formulation, and characterization of multiavonoids-loaded flavanosome by bulk or sequential technique |
| title_short | Optimization, formulation, and characterization of multiavonoids-loaded flavanosome by bulk or sequential technique |
| title_sort | optimization formulation and characterization of multiavonoids loaded flavanosome by bulk or sequential technique |
| url | http://psasir.upm.edu.my/id/eprint/53459/1/Optimization%2C%20formulation%2C%20and%20characterization.pdf |
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