Natural bioactives are mixtures of compounds extracted from plants with physicochemical properties that are usually not favorable for penetrating the skin’s complex barrier. Nanoparticles have important advantages both in dermatology and cosmetology: improved solubility and stability of encapsulated phytocompounds, controlled and sustained skin delivery, and enhanced skin permeation, leading to an improved bioavailability. This review focuses on two generations of lipid-based nanoparticles: solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). An extensive overview on the recent studies on SLNs and NLCs entrapping essential oils, oils, herbal extracts, and phytocompounds for topical applications is presented, emphasizing their composition, physicochemical characterization, efficacy, and methodologies used to evaluate them. This review also summarizes topical systems containing natural bioactives incorporated into SLNs and NLCs, commercially available products and registered patents in the field. SLNs and NLCs turn out to be effective nanocarriers for skin applications, offering significantly improved encapsulation efficiency, stability, and bioactives delivery. However, their full potential is underexplored. Future applications should study the encapsulation potential of new natural bioactives and show more specialized solutions that address specific requirements; an improved product performance and a pleasant sensory profile could lead to increased customer compliance with the product use.
1 February 2017 in Drug Design, Development and Therapy
Striae distensae are a frequent skin condition associated with pregnancy, weight change or lack of skin elasticity. The aim of this research was to obtain a topical product containing herbal active ingredients with documented antioxidant and anti-inflammatory activity (Punica granatum seed oil and Croton lechleri resin extract) and demonstrate its positive effect on prevention and treatment of striae distensae. First, the cream base formulation was optimized through experimental design. Secondly, the cream containing the two active ingredients was investigated in an interventional nonrandomized clinical trial. The clinical outcome was assessed through biophysical parameters and ultrasonographic evaluation. The state of the skin was evaluated by biophysical measurements and ultrasonography at the beginning of the study and after 3 and 6 weeks. The experimental design was successfully used to set the best ranges for the technological and formulation factors to obtain a cosmetic formulation with optimal characteristics. The study of clinical efficacy on the optimal formulation revealed an increase in the dermis thickness, hydration and elasticity values in both groups after 6 weeks of cream application. The new oil-in-water cream containing P. granatum seed oil and C. lechleri resin extract can be helpful in the prevention or improving of skin changes associated with striae.
Winery industry by-products have a great reuse potential in the pharmaceutical and cosmetic fields due to their bioactive compounds. This study investigates the phytochemical profile and the bioactivity of Vitis vinifera variety Fetească neagră tendrils extract (TE) and leaves extract (LE), intended to be used in oral hygiene products recommended in periodontal disease. The evaluation of the phenolic content was performed by colorimetric analysis. Liquid chromatography coupled with mass spectrometry was used to determine the chemical profile of the two extracts obtained from V. vinifera. Moreover, the antioxidant activity of the extracts was determined by spectrophotometric methods, as well as on human gingival fibroblasts (HGF) cell line. The cytocompatibility and cytoprotective effect against nicotine-induced cytotoxicity were tested, as well as the anti-inflammatory and antimicrobial effects. The TE showed higher total polyphenolic content, rich in rutin, compared to the leaves extract that displayed important amounts of isoquercitrin. The antioxidant effect was confirmed by both non-cellular and cellular tests. The cytocompatibility of the extracts was confirmed at a wide range of concentrations. The cytoprotective effect was demonstrated in HGF exposed to cytotoxic doses of nicotine; 300 µg/mL of both tested extracts decreased nicotine toxicity by approximately 20%. When challenged with E. coli polysaccharides, in HGF cells co-exposed to TE and LE, a reduction in the release of proinflammatory cytokines (IL-8, IL-6 and IL-1β) was observed. The extracts were both able to reduce the levels of reactive oxygen species and inflammatory cytokines, and had notable antimicrobial effects on pathogenic bacteria associated with periodontitis.
The current study aimed to develop carbomer based hydrogel dressings, incorporating ethanolic extracts of Rosmarinus officinalis aerial parts, Achillea millefolium and Calendula officinalis flowers. The pharmaceutical properties of the obtained hydrogels, as well as their texture and antimicrobial activity, were further evaluated. Five wound dressing formulations based on carbopol were prepared. The addition of the ethanolic extracts to the formulation slightly lowered the pH of the hydrogels, as expected. The Rosmarinus officinalis aerial parts extract loaded hydrogel proved to be the firmest one. In terms of consistency and viscosity, the behavior of the five hydrogels was relatively similar. Based on the texture analysis, the texture of the hydrogels has been affected to some extent by the addition of the ethanolic extracts, decreasing their consistency, firmness, and adhesiveness. The hydrogel loaded with Rosmarinus officinalis aerial parts extract and the one incorporating the blend of extracts (mixture of the three above-mentioned extracts) proved to have a good antimicrobial activity. The studied hydrogel formulations could serve as a basis for the development of novel wound dressing materials, although more extended in vivo studies would be needed in order to support current results.
The need to develop wound healing preparations is a pressing challenge given the limitations of the current treatment and the rising prevalence of impaired healing wounds. Although herbal extracts have been used for many years to treat skin disorders, due to their wound healing, anti-inflammatory, antimicrobial, and antioxidant effects, their efficacy can be questionable because of their poor bioavailability and stability issues. Nanotechnology offers an opportunity to revolutionize wound healing therapies by including herbal compounds in nanosystems. Particularly, vesicular nanosystems exhibit beneficial properties, such as biocompatibility, targeted and sustained delivery capacity, and increased phytocompounds’ bioavailability and protection, conferring them a great potential for future applications in wound care. This review summarizes the beneficial effects of phytocompounds in wound healing and emphasizes the advantages of their entrapment in vesicular nanosystems. Different types of lipid nanocarriers are presented (liposomes, niosomes, transferosomes, ethosomes, cubosomes, and their derivates’ systems), highlighting their applications as carriers for phytocompounds in wound care, with the presentation of the state-of-art in this field. The methods of preparation, characterization, and evaluation are also described, underlining the properties that ensure good in vitro and in vivo performance. Finally, future directions of topical systems in which vesicle-bearing herbal extracts or phytocompounds can be incorporated are pointed out, as their development is emerging as a promising strategy.
1 June 2017 in European Journal of Pharmaceutical Sciences