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...

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Váldodahkkit: Karthivashan, Govindarajan, Masarudin, Mas Jaffri, Kura, Aminu Umar, Abas, Faridah, Fakurazi, Sharida
Materiálatiipa: Artihkal
Giella:English
Almmustuhtton: Dove Medical Press 2016
Liŋkkat:http://psasir.upm.edu.my/id/eprint/53459/1/Optimization%2C%20formulation%2C%20and%20characterization.pdf
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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.
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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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AT kuraaminuumar optimizationformulationandcharacterizationofmultiavonoidsloadedflavanosomebybulkorsequentialtechnique
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