Synthesis of Pore-Size-Tunable Mesoporous Silica Nanoparticles by Simultaneous Sol-Gel and Radical Polymerization to Enhance Silibinin Dissolution

Background: Silibinin (SBN), a major active constituent of milk thistle seeds, exhibits numerous pharmacological activities. However, its oral bioavailability is low due to poor water solubility. This study aimed to develop a new synthetic approach for tuning the pore characteristics of mesoporous s...

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Autores principales: Mina Shafiee, Samirasadat Abolmaali, Mozhgan Abedanzadeh, Mehdi Abedi, Alimohammad Tamaddon
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Publicado: Shiraz University of Medical Sciences 2021
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spelling oai:doaj.org-article:696c4e0c89ee4d7e98aafcd8f135e3292021-11-09T06:23:38ZSynthesis of Pore-Size-Tunable Mesoporous Silica Nanoparticles by Simultaneous Sol-Gel and Radical Polymerization to Enhance Silibinin Dissolution0253-07161735-368810.30476/ijms.2020.86173.1595https://doaj.org/article/696c4e0c89ee4d7e98aafcd8f135e3292021-11-01T00:00:00Zhttps://ijms.sums.ac.ir/article_47281_1a28e4112937aeb09abd160730afd346.pdfhttps://doaj.org/toc/0253-0716https://doaj.org/toc/1735-3688Background: Silibinin (SBN), a major active constituent of milk thistle seeds, exhibits numerous pharmacological activities. However, its oral bioavailability is low due to poor water solubility. This study aimed to develop a new synthetic approach for tuning the pore characteristics of mesoporous silica nanoparticles (MSNs) intended for the oral delivery of SBN. In addition, the effects of the pore diameter of MSNs on the loading capacity and the release profile of SBN were investigated.Methods: The present study was performed at Shiraz University of Medical Sciences, Shiraz, Iran, in 2019. This synthesis method shares the features of the simultaneous free-radical polymerization of methyl methacrylate and the sol-gel reaction of the silica precursor at the n-heptane/water interface. SBN was loaded onto MSNs, the in vitro release was determined, and the radical scavenging activities were compared between various pH values using the analysis of variance. Results: According to the Brunauer–Emmett–Teller protocol, the pore sizes were well-tuned in the range of 2 to 7 nm with a large specific surface area (600–1200 m2/g). Dynamic light scattering results showed that different volume ratios of n-heptane/water resulted in different sizes, ranging from 25 to 100 nm. Interestingly, high SBN loading (13% w/w) and the sustained release of the total drug over 12 hours were achieved in the phosphate buffer (pH=6.8). Moreover, the antioxidant activity of SBN was well preserved in acidic gastric pH.Conclusion: Well-tuned pores of MSNs provided a proper substrate, and thus, enhanced SBN loading and oral dissolution and preserved its antioxidant activity. Nevertheless, further in vitro and in vivo investigations are needed.Mina ShafieeSamirasadat AbolmaaliMozhgan AbedanzadehMehdi AbediAlimohammad TamaddonShiraz University of Medical Sciencesarticlenanoparticlessilicon dioxidepolymerizationsilybinantioxidantsMedicine (General)R5-920ENIranian Journal of Medical Sciences, Vol 46, Iss 6, Pp 475-486 (2021)
institution DOAJ
collection DOAJ
language EN
topic nanoparticles
silicon dioxide
polymerization
silybin
antioxidants
Medicine (General)
R5-920
spellingShingle nanoparticles
silicon dioxide
polymerization
silybin
antioxidants
Medicine (General)
R5-920
Mina Shafiee
Samirasadat Abolmaali
Mozhgan Abedanzadeh
Mehdi Abedi
Alimohammad Tamaddon
Synthesis of Pore-Size-Tunable Mesoporous Silica Nanoparticles by Simultaneous Sol-Gel and Radical Polymerization to Enhance Silibinin Dissolution
description Background: Silibinin (SBN), a major active constituent of milk thistle seeds, exhibits numerous pharmacological activities. However, its oral bioavailability is low due to poor water solubility. This study aimed to develop a new synthetic approach for tuning the pore characteristics of mesoporous silica nanoparticles (MSNs) intended for the oral delivery of SBN. In addition, the effects of the pore diameter of MSNs on the loading capacity and the release profile of SBN were investigated.Methods: The present study was performed at Shiraz University of Medical Sciences, Shiraz, Iran, in 2019. This synthesis method shares the features of the simultaneous free-radical polymerization of methyl methacrylate and the sol-gel reaction of the silica precursor at the n-heptane/water interface. SBN was loaded onto MSNs, the in vitro release was determined, and the radical scavenging activities were compared between various pH values using the analysis of variance. Results: According to the Brunauer–Emmett–Teller protocol, the pore sizes were well-tuned in the range of 2 to 7 nm with a large specific surface area (600–1200 m2/g). Dynamic light scattering results showed that different volume ratios of n-heptane/water resulted in different sizes, ranging from 25 to 100 nm. Interestingly, high SBN loading (13% w/w) and the sustained release of the total drug over 12 hours were achieved in the phosphate buffer (pH=6.8). Moreover, the antioxidant activity of SBN was well preserved in acidic gastric pH.Conclusion: Well-tuned pores of MSNs provided a proper substrate, and thus, enhanced SBN loading and oral dissolution and preserved its antioxidant activity. Nevertheless, further in vitro and in vivo investigations are needed.
format article
author Mina Shafiee
Samirasadat Abolmaali
Mozhgan Abedanzadeh
Mehdi Abedi
Alimohammad Tamaddon
author_facet Mina Shafiee
Samirasadat Abolmaali
Mozhgan Abedanzadeh
Mehdi Abedi
Alimohammad Tamaddon
author_sort Mina Shafiee
title Synthesis of Pore-Size-Tunable Mesoporous Silica Nanoparticles by Simultaneous Sol-Gel and Radical Polymerization to Enhance Silibinin Dissolution
title_short Synthesis of Pore-Size-Tunable Mesoporous Silica Nanoparticles by Simultaneous Sol-Gel and Radical Polymerization to Enhance Silibinin Dissolution
title_full Synthesis of Pore-Size-Tunable Mesoporous Silica Nanoparticles by Simultaneous Sol-Gel and Radical Polymerization to Enhance Silibinin Dissolution
title_fullStr Synthesis of Pore-Size-Tunable Mesoporous Silica Nanoparticles by Simultaneous Sol-Gel and Radical Polymerization to Enhance Silibinin Dissolution
title_full_unstemmed Synthesis of Pore-Size-Tunable Mesoporous Silica Nanoparticles by Simultaneous Sol-Gel and Radical Polymerization to Enhance Silibinin Dissolution
title_sort synthesis of pore-size-tunable mesoporous silica nanoparticles by simultaneous sol-gel and radical polymerization to enhance silibinin dissolution
publisher Shiraz University of Medical Sciences
publishDate 2021
url https://doaj.org/article/696c4e0c89ee4d7e98aafcd8f135e329
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