Resveratrol Encapsulation and Release from Pristine and Functionalized Mesoporous Silica Carriers

Pharmaceutics

Cristian Matei¹  Daniela Berger¹  Mihaela Deaconu¹  Simona Ioniţă¹  Daniel Lincu¹  Ana-Maria Brezoiu¹  Laila Ziko²  Nada K. Sedky²  Raul-Augustin Mitran³ 

[1] Faculty of Applied Chemistry and Material Science, University “Politehnica” of Bucharest, 1–7 Polizu Street, 011061 Bucharest, Romania;School of Life and Medical Sciences, University of Hertfordshire, hosted by Global Academic Foundation, New Administrative Capital, Cairo 11865, Egypt;“Ilie Murgulescu” Institute of Physical Chemistry, Romanian Academy, 202 Splaiul Indepedenței, 060021 Bucharest, Romania;

关键词: mesoporous silica;    resveratrol;    drug delivery;    kinetics;    functionalization;    cell cycle analysis;   

DOI  :  10.3390/pharmaceutics14010203

来源: DOAJ

【 摘 要 】

Resveratrol, a naturally occurring polyphenol, has attracted significant attention due to its antioxidant, cardioprotective and anticancer potential. However, its low aqueous solubility limits resveratrol bioavailability and use. In this work, different mesoporous silica matrices were used to encapsulate the polyphenol and to increase its dissolution rate. Pristine MCM-41, MCM-48, SBA-15, SBA-16, FDU-12 and MCF silica were obtained. The influence of SBA-15 functionalized with aminopropyl, isocyanate, phenyl, mercaptopropyl, and propionic acid moieties on resveratrol loading and release profiles was also assessed. The cytotoxic effects were evaluated for mesoporous carriers and resveratrol-loaded samples against human lung cancer (A549), breast cancer (MDA-MB-231) and human skin fibroblast (HSF) cell lines. The effect on apoptosis and cell cycle were assayed for selected resveratrol-loaded carriers. The polyphenol molecules are encapsulated only inside the mesopores, mostly in amorphous state. All materials containing either pristine or functionalized silica carriers increased polyphenol dissolution rate. The influence of the physico-chemical properties of the mesoporous carriers and resveratrol–loaded supports on the kinetic parameters was identified. Resv@SBA-15-SH and Resv@SBA-15-NCO samples exhibited the highest anticancer effect against A549 cells (IC₅₀ values were 26.06 and 36.5 µg/mL, respectively) and against MDA-MB-231 (IC₅₀ values were 35.56 and 19.30 µg/mL, respectively), which highlights their potential use against cancer.

【 授权许可】

Unknown