PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery

Abstract

The in vitro biochemical evaluation of the applicability of polymers carrying active substances (micelles and conjugates) was carried out. Previously designed amphiphilic graft copolymers with retinol or 4-n-butylresorcinol functionalized polymethacrylate backbone and poly(ethylene glycol) (PEG) side chains that included Janus-type heterografted copolymers containing both PEG and poly(ε-caprolactone) (PCL) side chains were applied as micellar carriers. The polymer self-assemblies were convenient to encapsulate arbutin (ARB) as the selected active substances. Moreover, the conjugates of PEG graft copolymers with ferulic acid (FA) or lipoic acid (LA) were also investigated. The permeability of released active substances through a membrane mimicking skin was evaluated by conducting transdermal tests in Franz diffusion cells. The biological response to new carriers with active substances was tested across cell lines, including normal human dermal fibroblasts (NHDF), human epidermal keratinocyte (HaCaT), as well as cancer melanoma (Me45) and metastatic human melanoma (451-Lu), for comparison. These polymer systems were safe and non-cytotoxic at the tested concentrations for healthy skin cell lines according to the MTT test. Cytometric evaluation of cell cycles as well as cell death defined by Annexin-V apoptosis assays and senescence tests showed no significant changes under action of the delivery systems, as compared to the control cells. In vitro tests confirmed the biochemical potential of these antioxidant carriers as beneficial components in cosmetic products, especially applied in the form of masks and eye pads.

Revisiting the Cytotoxicity of Cationic Polyelectrolytes as a Principal Component in Layer-by-Layer Assembly Fabrication

“…The intensity of the accumulation of formazan crystals in the cytoplasm corresponds to the level of mitochondrial respiration, which is an indicator of cell viability. The amount of formazan formed inside the cells is proportional to the number of physiological active cells [ 26 ]. Neutral red is a weak cationic dye that easily penetrates cell membranes through non-diffusive, intercellular accumulation in lysosomes [ 27 ].…”

Development and evaluation of niacinamide transdermal formulation by artificial membrane permeability

“…The Strat-M® membrane (polyethersulfone and polyolefin membrane [synthetic lipid posttreatment]; diameter [ϕ] 25 mm and thickness 300 μm) and donor chamber were assembled, and the receptor chamber was filled with 8 mL of PBS (pH 7.4) using a magnetic stirrer ( Hajjar et al, 2018 , Odrobińska et al, 2020 ). All samples (NAC concentration of 10.0 mg/mL [1 mL]) was added to the donor chamber.…”

One Stone Two Birds: An Upconversion Nanosensor for Sensitive Detection of Fluoroquinolones in Aquatic Products Based on Chelation Recognition

“…So far, sensing methods for upconversion nanosensors are mostly based on immune recognition strategies, but there are a series of problems in the process of immune recognition based on bioactive molecules: (1) The structure of the immune recognition molecule is not easily maintained and can be damaged during storage and reaction phases; (2) The complex structure of immune recognition molecules renders batch-to-batch variation, thus difficult to control. , Optical sensors based on molecular imprinting have achieved some success in target identification. However, this strategy is often overloaded with functional monomers in order to make the equilibrium favorable for the generation of adducts, which inevitably results in the appearance of noncharacteristic binding sites, and make the system less capable of binding substrates .…”