What is it about?
Flavonoids are natural compounds present in fruits and plants that help to reduce inflammation, but when taken as they are, they tend to reach the tissues poorly because they are degraded or poorly absorbed. This systematic review brought together 24 studies (in vitro and in animals) that tested encapsulating flavonoids within nanoparticles (polymers, liposomes, inorganic particles, etc.) to protect and release them in a controlled manner. In many models, nanoparticle formulations clearly reduced the levels of key proinflammatory cytokines-such as TNF-α, IL-1β, IL-6 and IL-18-and in several cases the effect was greater than that of the free flavonoid. However, results vary according to flavonoid, nanoparticle type, size, charge and experimental model, and in some studies there was no significant difference between formulation and free compound. Overall, the work suggests that nanomedicine can improve the delivery and anti-inflammatory action of flavonoids, but further studies are still needed to optimize formulations and evaluate safety and efficacy in humans.
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Why is it important?
This work brings together two promising trends: natural bioactive compounds (flavonoids) and nanoscale delivery systems. Its importance lies in that it demonstrates, with preclinical evidence, that encapsulating flavonoids can overcome the main limitation of these compounds-their low bioavailability-and enhance their ability to downregulate central mediators of inflammation (TNF-α, IL-1β, IL-6). This opens the door to safer, plant-based adjuvant therapies for chronic inflammatory diseases (e.g. colitis, respiratory conditions, renal damage, cardiovascular pathologies), provided that design (type of nanocarrier, sustained release, stability) and clinical translation (pharmacokinetics, toxicity, dosage) challenges are resolved. In addition, the review identifies specific variables (encapsulation, size, zeta potential, release percentage) that formulators should prioritize, which can accelerate the optimization of new therapeutic formulations.
Perspectives
As a nanomedicine researcher, I am excited about two things about this body of work. First, the real potential of using relatively simple materials (PLGA, proteins such as fibroin, liposomes) to transform natural compounds into more effective therapeutic agents. Second, the abundance of preclinical data already pointing to the reduction of IL-1β, IL-6 and TNF-α, cytokines that we know drive many chronic diseases. That said, my practical perspective is clear: we need to move toward better standardized studies that compare formulations in a systematic manner (same dose, same cytokine readouts, and pharmacokinetic parameters), and prioritize medium-term safety and biodistribution studies before any human trials. For groups designing formulations, I recommend: (1) always report encapsulation efficiency, 24-h release, and zeta-potential; (2) include controls with free flavonoid and empty nanoparticle; and (3) publish bioavailability and toxicity data. I am available to collaborate on studies that integrate physicochemical characterization with biological assays and to help design protocols that accelerate responsible clinical translation of these formulations. Please visit: https://sites.google.com/view/nanomedicine/home
Christian Chapa
Universidad Autonoma de Ciudad Juarez
Read the Original
This page is a summary of: Nanoparticle-Mediated Delivery of Flavonoids: Impact on Proinflammatory Cytokine Production: A Systematic Review, Biomolecules, July 2023, MDPI AG,
DOI: 10.3390/biom13071158.
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