Linoleic, oleic, palmitoleic, palmitic, and stearic fatty acids (FAs) are commonly used in dermatological formulations. They differ by their structure, presence in the skin, and mode of application in pharmaceuticals and cosmetics compounding. These FAs are also known as chemical penetration enhancers, but their mechanisms of penetration enhancement and effect on barrier characteristics of the skin require additional study. In this study, the authors conducted an ex vivo analysis of the distribution of lipid components in the epidermis and dermis of human skin after applying individual FAs. The goal was to elucidate possible mechanisms of penetration enhancement and FA effects on barrier characteristics of the skin. FA penetration studies were conducted ex vivo on human skin and time-of-flight secondary ion mass spectrometry (TOF-SIMS) bioimaging analysis was performed to visualize and analyze distribution of FAs in skin sections. The current study demonstrated that TOF-SIMS imaging was effective in visualizing the distribution of linoleic, oleic, palmitoleic, palmitic, and stearic acid in the human skin ex vivo after the skin penetration experiment of individual FAs. The integration of the obtained TOF-SIMS images allowed a semiquantitative comparison of the effects induced by individual FA applications on the human skin ex vivo. FAs showed varying abilities to penetrate the skin and disorder the FAs within the skin, based on their structures and physicochemical properties. Linoleic acid penetrated the skin and changed the distribution of all the analyzed FAs. Skin treatment with palmitoleic or oleic acid increased the amounts of singular FAs in the skin. Penetration of saturated FAs was low, but it increased the detected amounts of linoleic acid in both skin layers. The results indicate that application of FAs on the skin surface induce redistribution of native FAs not only in the stratum corneum layer of epidermis but also in the lipid content of full epidermis and dermis layers. The results indicate that topically applied pharmaceutical products should be evaluated for potential chemical penetration enhancement and lipid component redistribution effects during formulation.
Fatty acids classified as chemical penetration enhancers (CPEs) might cause the fluidization and perturbation of stratum corneum (SC) lipid matrix. The penetration of oleic, linoleic, lauric and capric acids into human skin was studied by time-of-flight secondary ion mass spectrometry (TOF-SIMS) imaging and related to fatty acids enhancing effect on lipophilic model drug tolnaftate penetration into human epidermis and dermis ex vivo. Fatty acid enhancing effect on tolnaftate penetration into human skin was evaluated using Bronaugh-type flow-through diffusion cells. After in vitro penetration studies visualization and spatial localization of fatty acid molecules in human skin were performed using TOF-SIMS. Penetration of oleic, linoleic, lauric and capric acids into human skin was compared to the control skin sections by ion images and intensity profiles. Only oleic acid significantly (P<0.05) enhanced tolnaftate penetration into epidermis (enhancing ratio equal to 1.867). CPE might have no effect on model drug penetration enhancement, but might penetrate itself into the skin.
Natural oils are commonly used in topical pharmaceutical formulations as emulsifiers, stabilizers or solubility enhancers. They are presented as safe and inert components, mainly used for formulation purposes. It is confirmed that natural oils can affect the skin penetration of various substances. Fatty acids are mainly responsible for this effect. Current understanding lacks reliable scientific data on penetration of natural oils into the skin and their skin penetration enhancement potential. In the current study, fatty acid content analysis was used to determine the principal fatty acids in soybean, olive, avocado, sea-buckthorn pulp, raspberry seed and coconut oils. Time of flight secondary ion mass spectrometry bioimaging was used to determine the distribution of these fatty acids in human skin ex vivo after application of the oils. Skin penetration enhancement ratios were determined for a perspective antioxidant compound dihydroquercetin. The results demonstrated skin penetration of fatty acids from all oils tested. Only soybean and olive oils significantly increased the skin distribution of dihydroquercetin and can be used as skin penetration enhancers. However, no correlation can be determined between the fatty acids’ composition and skin penetration enhancement using currently available methodological approaches. This indicates that potential chemical penetration enhancement should be evaluated during formulation of topically applied products containing natural oils.
The paradigm of how we manage allergic rhinitis is shifting with a growing understanding that it is a complex process, requiring a coordinated effort from healthcare providers and patients. Pharmacists are key members of these integrated care pathways resolving medication-related problems, optimizing regimens, improving adherence and recommending therapies while establishing liaisons between patients and physicians. Community pharmacists are the most accessible healthcare professionals to the public and allergic rhinitis is one of the most common diseases managed by pharmacists. Allergic Rhinitis and its Impact on Asthma (ARIA) guidelines developed over the past 20 years have improved the care of allergic rhinitis patients through an evidence-based, integrated care approach. In this paper, we propose an integrated approach to allergic rhinitis management in community pharmacy following the 2019 ARIA in the pharmacy guidelines.
An electrospun hydrophilic non-water-soluble biocompatible polylactic acid (PLA) nonwoven material was used as a delivery system for propolis ethanolic extract (PEE) and silver nanoparticles (AgNPs) that are known for their established antiseptic and antimicrobial activity. Combination of PEE and AgNPs in a single product should provide efficient antimicrobial protection and improved wound healing. Evaluations of PEE and AgNPs on morphology of electrospun materials, release kinetics of AgNPs and phenolic compounds, antibacterial properties, and cytotoxicity of electrospun PLA materials were performed. The presence of PEE or/and AgNPs resulted in denser mats formed by thicker PLA fibers. The average diameter of PLA microfibers was nm. The average diameter of microfibers increased to and nm when 10 wt% and 20 wt% ethanol were added, respectively. Addition of 10 wt% or 20 wt% PEE increased the diameter to and nm, respectively. Suspension of AgNPs also caused the formation of thicker microfibers with nm diameter. Electrospun PLA microfibers with PEE maintained viability of HaCaT cells. Testing of antimicrobial activity confirmed the ability of AgNPs containing PLA electrospun materials to inhibit the growth of microorganisms.