TY - JOUR ID - 47281 TI - Synthesis of Pore-Size-Tunable Mesoporous Silica Nanoparticles by Simultaneous Sol-Gel and Radical Polymerization to Enhance Silibinin Dissolution JO - Iranian Journal of Medical Sciences JA - IJMS LA - en SN - 0253-0716 AU - Shafiee, Mina AU - Abolmaali, Samirasadat AU - Abedanzadeh, Mozhgan AU - Abedi, Mehdi AU - Tamaddon, Alimohammad AD - Department of Pharmaceutical Nanotechnology, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran AD - Center for Nanotechnology in Drug Delivery, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran Y1 - 2021 PY - 2021 VL - 46 IS - 6 SP - 475 EP - 486 KW - Nanoparticles KW - Silicon dioxide KW - Polymerization KW - Silybin KW - Antioxidants DO - 10.30476/ijms.2020.86173.1595 N2 - 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. UR - https://ijms.sums.ac.ir/article_47281.html L1 - https://ijms.sums.ac.ir/article_47281_347d30f7a1ffadd5a9a1e120f6ae0b07.pdf ER -