Transdermal Delivery of Phloretin by Gallic Acid Microparticles

Abstract

Exposure to ultraviolet (UV) radiation causes harmful effects on the skin, such as inflammatory states and photoaging, which depend strictly on the form, amount, and intensity of UV radiation and the type of individual exposed. Fortunately, the skin is endowed with a number of endogenous antioxidants and enzymes crucial in its response to UV radiation damage. However, the aging process and environmental stress can deprive the epidermis of its endogenous antioxidants. Therefore, natural exogenous antioxidants may be able to reduce the severity of UV-induced skin damage and aging. Several plant foods constitute a natural source of various antioxidants. These include gallic acid and phloretin, used in this work. Specifically, polymeric microspheres, useful for the delivery of phloretin, were made from gallic acid, a molecule that has a singular chemical structure with two different functional groups, carboxylic and hydroxyl, capable of providing polymerizable derivatives after esterification. Phloretin is a dihydrochalcone that possesses many biological and pharmacological properties, such as potent antioxidant activity in free radical removal, inhibition of lipid peroxidation, and antiproliferative effects. The obtained particles were characterized by Fourier transform infrared spectroscopy. Antioxidant activity, swelling behavior, phloretin loading efficiency, and transdermal release were also evaluated. The results obtained indicate that the micrometer-sized particles effectively swell, and release the phloretin encapsulated in them within 24 h, and possess antioxidant efficacy comparable to that of free phloretin solution. Therefore, such microspheres could be a viable strategy for the transdermal release of phloretin and subsequent protection from UV-induced skin damage.

Antimicrobial, Antioxidant, and Anti‐Inflammatory Nanoplatform for Effective Management of Infected Wounds

“…Polyphenolic compounds like Phloretin are widely used in skincare due to their anti‐oxidative characteristics. [ 37 ] Also, Phloretin has been noted for its anti‐inflammatory properties by significantly inhibiting the levels of IL‐6 and TNF‐ α in lipopolysaccharide (LPS)‐stimulated murine Raw 264.7 cells. [ 38 ] In addition, studies have shown that Phloretin exhibits highly potent anti‐inflammatory properties by suppressing TNF‐ α , IL‐6, and IL‐1 β levels in lung tissue.…”

“…Polyphenolic compounds like Phloretin are widely used in skincare due to their anti-oxidative characteristics. [37] Figure 4. Antioxidant activity and anti-inflammation performance of Phloretin, HP, and HPA.…”

Designed Fabrication of Phloretin-Loaded Propylene Glycol Binary Ethosomes: Stability, Skin Permeability and Antioxidant Activity

“…The observed outcome can be ascribed to the presence of hydrophobic PHL, which was encased within nanoparticles possessing hydrophilic surfaces. This encapsulation facilitated the improved dispersion of PHL in water, hence enhancing the interaction between PHL and free radicals [ 56 ]. Ethosomes without the addition of PG have lower antioxidant potentials due to the presence of less carrier-coated PHL.…”

Gallic Acid-Based Hydrogels for Phloretin Intestinal Release: A Promising Strategy to Reduce Oxidative Stress in Chronic Diabetes

“…The phloretin concentration in the different solutions was monitored by the use of UV-Vis spectrophotometry at 288 nm. The data were calculated in terms of drug release percentage [ 27 ].…”