Microemulsions and nanoemulsions are lipid-based pharmaceutical systems with a high potential to increase the permeation of drugs through the skin. Although being isotropic dispersions of two nonmiscible liquids (oil and water), significant differences are encountered between microemulsions and nanoemulsions. Microemulsions are thermodynamically stable o/w emulsions of mean droplet size approximately 100–400 nm, whereas nanoemulsions are thermodynamically unstable o/w emulsions of mean droplet size approximately 1 to 100 nm. Their inner oil phase allows the solubilization of lipophilic drugs, achieving high encapsulation rates, which are instrumental for drug delivery. In this review, the importance of these systems, the key differences regarding their composition and production processes are discussed. While most of the micro/nanoemulsions on the market are held by the cosmetic industry to enhance the activity of drugs used in skincare products, the development of novel pharmaceutical formulations designed for the topical, dermal and transdermal administration of therapeutic drugs is being considered. The delivery of poorly water-soluble molecules through the skin has shown some advantages over the oral route, since drugs escape from first-pass metabolism; particularly for the treatment of cutaneous diseases, topical delivery should be the preferential route in order to reduce the number of drugs used and potential side-effects, while directing the drugs to the site of action. Thus, nanoemulsions and microemulsions represent versatile options for the delivery of drugs through lipophilic barriers, and many synthetic and natural compounds have been formulated using these delivery systems, aiming to improve stability, delivery and bioactivity. Detailed information is provided concerning the most relevant recent scientific publications reporting the potential of these delivery systems to increase the skin permeability of drugs with anti-inflammatory, sun-protection, anticarcinogenic and/or wound-healing activities. The main marketed skincare products using emulsion-based systems are also presented and discussed.
Skin aging is described as dermatologic changes either naturally occurring over the course of years or as the result of the exposure to environmental factors (e.g., chemical products, pollution, infrared and ultraviolet radiations). The production of collagen and elastin, the main structural proteins responsible for skin strength and elasticity, is reduced during aging, while their role in skin rejuvenation can trigger a wrinkle reversing effect. Elasticity loss, wrinkles, dry skin, and thinning are some of the signs that can be associated with skin aging. To overcome skin aging, many strategies using natural and synthetic ingredients are being developed aiming to reduce the signs of aging and/or to treat age-related skin problems (e.g., spots, hyper- or hypopigmentation). Among the different approaches in tissue regeneration, the use of nanomaterials loaded with cosmeceuticals (e.g., phytochemicals, vitamins, hyaluronic acid, and growth factors) has become an interesting alternative. Based on their bioactivities and using different nanoformulations as efficient delivery systems, several cosmeceutical and pharmaceutical products are now available on the market aiming to mitigate the signs of aged skin. This manuscript discusses the state of the art of nanomaterials commonly used for topical administration of active ingredients formulated in nanopharmaceuticals and nanocosmeceuticals for skin anti-aging.
Glyphosate-based herbicide has been the first choice for weed management worldwide since the 1970s, mainly due to its efficacy and reported low toxicity, which contributed to its high acceptance. Many of the recent studies focus solely on the persistence of pesticides in soils, air, water or food products, or even on the degree of exposure of animals, since their potential hazards to human health have raised concerns. Given the unaware exposure of the general population to pesticides, and the absence of a significant number of studies on occupational hazards, new glyphosate-induced toxicity data obtained for both residual and acute doses should be analyzed and systematized. Additionally, recent studies also highlight the persistence and toxicity of both glyphosate metabolites and surfactants present in herbicide formulations. To renew or ban the use of glyphosate, recently published studies must be taken into account, aiming to define new levels of safety for exposure to herbicide, its metabolites, and the toxic excipients of its formulations. This review aims to provide an overview of recent publications (2010–present) on in vitro and in vivo studies aimed at verifying the animal toxicity induced by glyphosate, its metabolite aminomethylphosphonic acid (AMPA) and glyphosate-based formulations, evaluated in various experimental models. Apart from glyphosate-induced toxicity, recent data concerning the role of surfactants in the toxicity of glyphosate-based formulations are discussed.
1 December 2018 in International Journal of Pharmaceutics
Oleanolic (OA) and ursolic (UA) acids are recognized triterpenoids with anti-cancer properties, showing cell-specific activity that can be enhanced when loaded into polymeric nanoparticles. The cytotoxic activity of OA and UA was assessed by Alamar Blue assay in three different cell lines, i.e., HepG2 (Human hepatoma cell line), Caco-2 (Human epithelial colorectal adenocarcinoma cell line) and Y-79 (Human retinoblastoma cell line). The natural and synthetic mixtures of these compounds were tested as free and loaded in polymeric nanoparticles in a concentration range from 2 to 32 µmol/L. The highest tested concentrations of the free triterpene mixtures produced statistically significant cell viability reduction in HepG2 and Caco-2 cells, compared to the control (untreated cells). When loaded in the developed PLGA nanoparticles, no differences were recorded for the tested concentrations in the same cell lines. However, in the Y-79 cell line, a decrease on cell viability was observed when testing the lowest concentration of both free triterpene mixtures, and after their loading into PLGA nanoparticles.