Permeation Protection by Waterproofing Mucosal Membranes

The permeability of the oral or nasal mucosa is higher than that of the skin. Mucosa permeabilitydepends mainly on the thickness and keratinization degree of the tissues. Their permeabilitybarrier is conditioned by the presence of certain lipids. This work has the main aim of reinforcing thebarrier effect of oral mucosa with a series of formulations to reduce permeation. Transmembranewater loss of different formulations was evaluated, and three of them were selected to be tested onthe sublingual mucosa permeation of drugs. Caffeine, ibuprofen, dexamethasone, and ivermectinwere applied on porcine skin, mucosa, and modified mucosa in order to compare the effectiveness ofthe formulations. A similar permeation profile was obtained in the different membranes: caffeine> ibuprofen~dexamethasone > ivermectin. The most efficient formulation was a liposomal formulationcomposed of lipids that are present in the skin stratum corneum. Impermeability providedby this formulation was notable mainly for the low-molecular-weight compounds, decreasing theirpermeability coefficient by between 40 and 80%. The reinforcement of the barrier function of mucosaprovides a reduction or prevention of the permeation of different actives, which could be extrapolatedto toxic compounds such as viruses, contaminants, toxins, etc.</p

Enzymatic Synthesis of Phloretin alpha-Glucosides Using a Sucrose Phosphorylase Mutant and its Effect on Solubility, Antioxidant Properties and Skin Absorption

Glycosylation of polyphenols may increase their aqueous solubility, stability, bioavailability and pharmacological activity. Herein, we used a mutant of sucrose phosphorylase from Thermoanaerobacterium thermosaccharolyticum engineered to accept large polyphenols (variant TtSPP_R134A) to produce phloretin glucosides. The reaction was performed using 10% (v/v) acetone as cosolvent. The selective formation of a monoglucoside or a diglucoside (53% and 73% maximum conversion percentage, respectively) can be kinetically controlled. MS and 2D-NMR determined that the monoglucoside was phloretin 4¿-O-¿-D-glucopyranoside and the diglucoside phloretin-4¿-O-[¿-D-glucopyranosyl-(1¿3)-O-¿-D-glucopyranoside], a novel compound. The molecular features that determine the specificity of this enzyme for 4¿-OH phenolic group were analysed by induced-fit docking analysis of each putative derivative, using the crystal structure of TtSPP and changing the mutated residue. The mono- and diglucoside were, respectively, 71- and 1200-fold more soluble in water than phloretin at room temperature. The a-glucosylation decreased the antioxidant capacity of phloretin, measured by DPPH and ABTS assays; however, this loss was moderate and the activity could be recovered upon deglycosylation in vivo. Since phloretin attracts a great interest in dermocosmetic applications, we analyzed the percutaneous absorption of glucosides and the aglycon employing a pig skin model. Although the three compounds were detected in all skin layers (except the fluid receptor), the diglucoside was present mainly on superficial layers

In Vitro DVS Approach to Evaluate Skin Reparation

The stratum corneum (SC), the most superficial layer of the skin, is directly responsible for the skin’s barrier function. The intercellular lipids in the SC play an important role in the regulation of the skin’s water-holding capacity. The modification of the intercellular lipid organization and composition may impair these properties. The aim of the present study is to describe a new in vitro approach of the repairing capacity evaluation of lipid formulations on skin with the use of absorption and desorption curves. The formulations were applied on lipid-extracted SC, and the possible SC reparation was assessed with the use of a thermogravimetric balance (DVS). Moisture absorption/desorption experiments proved to be adequate for the evaluation of the repairing capacity of formulations applied on damaged skin. Besides, freeze-substitution transmission electron microscopy (FSTEM) images showed some lipid bilayers, indicating a lipid bilayer reconstitution due to the applied formulations.We acknowledge support by the CSIC Open Access Publication Initiative through its Unit of Information Resources for Research (URICI).The authors wish to thank the Spanish National Projects (Ministerio de Educación y Ciencia) CTQ-2013-449-98-P for their financial support. The authors are indebted to the Skin Efficacy Service (SES-IQAC) for allowing the use of their non-invasive instrument techniques. The authors are grateful to Montserrat Rigol Muxart and Núria Solanes Batlló from the Department of Cardiology (Institut d’Investigacions Biomèdiques August Pi i Sunyer (IDIBAPS) Hospital Clínic, Universitat de Barcelona, Spain) for supplying porcine skin biopsies

Composiciones y uso extracto de lípidos internos de la lana en la preparación de productos para el tratamiento y cuidado de la piel

Referencia OEPM: P9901541.-- Fecha de solicitud: 09/07/1999.-- Titular: Consejo Superior de Investigaciones Científicas (CSIC).Composiciones y uso extracto de lípidos internos de la lana en la preparación de productos para el tratamiento y cuidado de la piel. Se describe el uso de extractos de los lípidos internos de las fibras de lana, con un contenido en ceramidas de al menos un 15% en peso, para preparar composiciones, farmacéuticas o cosméticas para el tratamiento y cuidado de la piel. Los extractos objeto de la invención manifiestan excelentes cualidades para mejorar de manera sostenida y prolongada el efecto de barrera de la piel contra las agresiones externas, así como una buena capacidad para mantener el grado de hidratación de la misma. Dichas cualidades son incluso superiores a las que se obtienen con composiciones lipídicas que contienen ceramida III, que imitan la propia del stratum corneum de la piel humana.Peer reviewe

Ethnic hair: Thermoanalytical and spectroscopic differences

Abstract Background The aim of this study is to characterize and detect the possible differences among the hair of three different ethnicities: African, Asiatic and Caucasian. Materials and Methods The differences in water adsorption/desorption behaviour of hairs were studied using a thermogravimetric balance and compared with the analysis of the lipid distribution and order using synchrotron‐based Fourier transform infrared microspectroscopy. Besides, the thermal thermogravimetry (TG) and differential scanning calorimetry (DSC) analyses on human hair were executed. Results Differences in the diffusion coefficients were evidenced. African hair exhibited increased permeability. Caucasian hair displayed a higher water absorption capability with increasing humidity but with a slow diffusion rate. The Asian fibre appeared to be more resistant to hydration changes. The spectroscopic analysis showed notable differences in the cuticle lipids. The African cuticle exhibited more lipids with a lower order bilayer. The outmost layer of Caucasian fibres contained more ordered lipids, and the Asian fibres show a very low level of lipids on the cuticle region. The DSC results indicate no difference in the thermal stability and TG showed higher water content in the Caucasian fibre and a possible lower cysteine disulphide bond content in the African hair matrix. Conclusion The triple approach demonstrated the permeability differences among the ethnic fibres and their correlation with the properties of their cuticle lipids. These differences could have particular relevance to the hair care cosmetic market.The authors wish to thank the 2009 SGR 2012 (AGAUR) for providing support. FTIR microspectroscopy was performed on the MIRAS beamline at the ALBA Synchrotron in collaboration with ALBA staff. Additionally, the authors acknowledge the Service of Dermocosmetic Assessment for its collaboration and the technical support provided by Isabel Yuste.Peer reviewe

Modelos de piel basados en membranas artificiales con lanolina

La presente invención se refiere a un modelo artificial de piel capaz de simular el comportamiento de la piel natural a nivel de permeación y penetración de compuestos. Este modelo está formado por una membrana polimérica de distinta naturaleza sobre la que se deposita una capa de lanolina. Este modelo artificial de piel es útil para ensayos de permeación y absorción de principios activos farmacológicos o cosméticosPeer reviewedConsejo Superior de Investigaciones Científicas (España)A1 Solicitud de patente con informe sobre el estado de la técnic

Keratin Proteins and Peptides from Wool, for Hair Restoration

6 páginas.-- et al.Human hair is composed mainly of keratin (80% w/w), an -helical protein with high cystine content, and a small amount of lipids. From a cosmetic point of view, it is the cuticle that gives hair a healthy or unhealthy look. Most beauty care products and treatments primarily affect the cuticle layers. Permanent waving, straightening or relaxing and bleaching during hair coloring processes are major causes of hair damage. The complex protein chemistry and the way the molecules assemble together give rise to the unique tensile properties of hair fibres. An important indicator of hair health and strength is its resistance to fracture breakage. Conventional hair treatments can modify hair structure and compromise some of the natural properties of the hair. The deterioration of the hair properties can be noticed in the form of poor manageability, dryness, brittleness, loss of shine and decrease strength (fiber breakage). There is a growing consumer trend in natural actives that can address these negative issues and have the potential to maintain youthful hair. It has been well known for some time, for example, that proteins and protein hydrolysates, are very beneficial to the hair, imparting increased moisturisation, enhancing softness and flexibility.Peer reviewe