Polymeric micelles containing resveratrol: development, characterization, cytotoxicity on tumor cells and antimicrobial activity

Abstract

Antimicrobial and antitumor activities of resveratrol, a compound found mainly in grapes, have already been demonstrated. However, its low bioavailability is a limiting factor for therapeutic application. Polymeric micelles can be an approach to solve this problem since they can encapsulate hydrophobic substances. We developed and characterized micellar formulations containing resveratrol and evaluated their cytotoxic and antimicrobial effects. The formulations were prepared by the cold dispersion method with different concentrations of F127 (5 or 10% w/w) and resveratrol (500 or 5000 µM). The formulations were characterized according to size, polydispersity index, pH, encapsulation rate and in vitro release. Cytotoxic effect was evaluated on a bladder cancer cell line and antimicrobial effect was evaluated on E. coli, S. aureus and C. albicans. One of the formulations (10% w/w of F127 and 5000 µM of resveratrol) was a monodispersed solution with high encapsulation rate, thus it was chosen for the cytotoxicity and antimicrobial assays. MS-10+RES-3 was able to preserve the antimicrobial and cytotoxic activity of resveratrol. This is the first study that evaluated antimicrobial potential and cytotoxicity of micelles containing resveratrol on bladder cancer cells and the results showed that micellar nanostructures could ensure the maintenance of the biological activity of resveratrol.

Interplay between Systemic Glycemia and Neuroprotective Activity of Resveratrol in Modulating Astrocyte SIRT1 Response to Neuroinflammation

“…Other beneficial effects of oral RSV administration within the CNS are discussed in detail elsewhere [42,43,48,49]. Improvement of the bioavailability of RSV as a dietary supplement is achieved by opsonization of the RSV molecule with lipophilic particles [51], by its nanoencapsulation within liposomes or micelles, increasing its intestinal absorption [181,182], by modification of the RSV molecular structure (e.g., hydroxylation or metoxylation of its aromatic rings) [183], or by its intrathecal administration, leading to increased penetration through the BBB into the CSF [175].…”

Nanophytomedicine: A promising practical approach in phytotherapy

“…Micellar formulations enhance the permeation and uptake of RSV both in vitro and in vivo, specifically in corneal permeation (Li, Zhang, et al, 2020). Micelles containing RSV have improved RSV bioavailability and maintained the antimicrobial and cytotoxic activity of RSV‐containing pluronic F127 (F127)‐micelles against bladder cancer cells (Almeida et al, 2020). Trans‐RSV is a polyphenol with broad therapeutic utility but has poor bioavailability and limited distribution across the blood–brain barrier.…”

Resveratrol effects in bladder cancer: A mini review

“…The activity of RSV loaded in nanoformulation, aiming its use in blader cancer, was investigated only by Almeida et al (2020 ). The authors showed that polymeric micelles were able to preserve the cytotoxic activity of free resveratrol in RT4 and T24 cells.…”