Nanovesicle-based formulations for photoprotection: a safety and efficacy approach.

Vesicular nanosystems are versatile and they are able to encapsulate actives with different solubilities, such as lipophilic and hydrophilic compounds. The most well-known vesicular nanosystems are liposomes and niosomes, the last one is formed by non-ionic surfactants. In the present work, we developed photoprotective niosomes containing sunscreens (octyl methoxycinnamate, diethylamino hydroxybenzoyl hexyl benzoate and phenylbenzimidazole sulfonic acid), non-ionic surfactants, cholesterol and stearylamine (positive-charged lipid). Studies based on dynamic light scattering techniques, entrapment efficiency and morphology by transmission electron microscopy were performed to characterize the niosomes. In addition, rheology, pH, in vitro sun protection factor (SPF) efficacy and toxicity and in vivo and in vitro safety were determined for the niosome formulations F-N1 and F-N2. The mean sizes of N1 and N2 were 168 ± 5 nm and 192 ± 8 nm, respectively, and their morphologies were spherical, unilamellar and with an entrapment efficiency of more than 45% for each sunscreen. Both formulations, F-N1 and F-N2 presented characteristics of pseudoplastic non-Newtonian fluids, showing declining viscosity with increasing shear rate applied. SPF values were considered satisfactory, 34 ± 8 for formulation F-N1 and 34 ± 5 for F-N2. The formulations did not present toxicity when tested in macrophages and the pH was compatible with skin, which minimizes allergies. The in vitro safety assay showed lipophilic sunscreens greater affinity for the epidermis, since this layer contains natural lipids. In vivo safety assay suggests that the increased skin retention of N2 is directly correlated with the positive charge of stearylamine. Stable photoprotective niosomes were obtained and were shown to be promising nanostructures to be used against solar radiation.

Photoprotection assessment of olive (Olea europaea L.) leaves extract standardized to oleuropein: In vitro and in silico approach for improved sunscreens.

Olive leaves contain higher amount of polyphenols than olive oil and represent a waste product from olive harvest and pruning of olive trees. The most abundant compound in olive leaves is oleuropein. Benefits of the topical application of olive leaves extract were previously reported, but little information is available on its photoprotective potential and the result of the association of this extract with organic UV filters in topical sunscreen formulations. The olive leaves extract photoprotective potential is less explored for both oral and topical photoprotection in comparison with other plants extracts and polyphenols, such as Polypodium leucotomos extract and resveratrol. There are increasing efforts towards developing more efficient sunscreens and a photoprotection assessement along with a better understanding of the photochemistry of naturally occurring sunscreens could aid the design of new and improved commercial sunscreen formulations. This study was designed to investigate the photoprotective potential of olive leaves extract standardized for oleuropein performing a set of in vitro and in silico tools as an innovative approach, highlighting yeast assays, in vitro Sun Protection Factor (SPF) and molecular modelling studies of UV absorption. This study supports the use of olive leaves extract for photoprotection, as an effective photoprotective, anti-mutagenic and antioxidant active, also showing a synergistic effect in association with UV filters with an improvement on in vitro SPF of sunscreen formulations.

Niosomes as Nano-Delivery Systems in the Pharmaceutical Field.

Nanosystems used in the pharmaceutical field aim to guarantee a controlled release and efficacy boost with dose reduction of the drug. The same active ingredient could be vehiculated in different concentrations in distinct nanosystems. Among these nanostructures, the vesicular ones present a versatile delivery system that could be applied to encapsulate lipophilic, amphiphilic, and hydrophilic compounds. Liposomes are the most well-known vesicular nanosystems; however, there are others, such as niosomes, that are composed of nonionic surfactants that are polymeric or conventional. Niosomes could be prepared using the thin film hydration method, in which the active ingredient is solubilized in organic solvent with the surfactant or in aqueous solution depending on its polarity. In addition, co-surfactants could be used to improve stabilization and vesicle integrity because they occupy regions in the interface where the mainly surfactant could not reach. Vesicular nanosystems could be characterized by different techniques, such as microscopy, dynamic light scattering, nuclear magnetic resonance, and others. These nanostructures could be applied to drugs (administered by different routes) or to gene and cosmetic delivery systems.

Nanosystems in Photoprotection.

The ultraviolet (UV) radiation is responsible for stimulating acute responses in the human skin, those including positive responses like vitamin D synthesis along with negative ones such as erythema. The chronic effects of UV radiation include photoaging and cancer. Sunscreens are classified as organic and inorganic and the safety of the products containing them is related to the evaluation of the effects of these actives on the skin (irritation and sensitization) and also the possibility of cutaneous permeation that may cause the product to permeate into the bloodstream, possibly generating systemic toxicity. Nanotechnology plays an important role in overcoming the obstacles related to sunscreens. In this context, there are the nanosystems that have been widely used as vehicles to sunscreens. The use of nanosystems aims to reduce phototoxicity and cutaneous permeation of sunscreens and also to act in improving the photostability, the sun protection factor (SPF) and the protection spectrum of sunscreens. The most studied nanosystems in photoprotection are: liposomes, nanoparticles (lipid, polymeric and inorganic), cyclodextrins and nanoemulsions.

Molecular modeling studies of the structural, electronic, and UV absorption properties of benzophenone derivatives.

Benzophenone derivatives (BZP), an important class of organic UV filters, are widely used in sunscreen products due to their ability to absorb in the UVA and UVB ranges. The structural, electronic, and spectral properties of BZP derivatives have been studied by density functional theory (DFT) and time-dependent DFT (TD-DFT) methods. DFT/B3LYP with the 6-31G(d) basis set is an accurate method for optimizing the geometry of BZPs. The absorption maxima obtained from the TD-DFT calculations in a vacuum were in agreement with the experimental absorption bands and showed that the main electronic transitions in the UVA/UVB range present π → π* character, the major transition being HOMO → LUMO. The oscillator strength seems to increase in the presence of disubstitution at the para position. For protic substituents, the position appears to be related to the absorption band. Absorption in the UVB range occurs in the presence of para substitution, whereas ortho substitution leads to absorption in the UVA spectral region. The obtained results provide some features for BZP derivatives that can be useful for customizing absorption properties (wavelengths and intensities) and designing new BZP derivatives as sunscreens.