A Synthetic Model of the Mucosa for Oral Penetration Studies.

The main objective of this study is the evaluation of the use of a synthetic membrane, Nuclepore, as a model for permeation studies through sublingual mucosa. The permeability of two types of membranes, porcine sublingual oral mucosa and a synthetic Nuclepore membrane, to water was compared. Moreover, the water permeability of membranes modified with waterproofing formulations was measured to study their ability to protect against the penetration of viruses, toxins, etc. A relatively high correlation (R2 0.88) was obtained between the transmucosal water loss (TMWL) values of the artificial membrane and the mucosa. These results support the possible use of this synthetic membrane in the screening of the water permeability of formulations. In addition, studies of the permeation of different actives, drugs, and biocides through the two membranes were carried out, and these results were compared with their skin permeation data. The synthetic membrane does not seem to discern between compounds in terms of permeability. However, the permeation of caffeine through intact or modified membranes incorporating waterproofing formulations presents similar permeation profiles through the synthetic membrane and mucosa. The results from these assays should lend support to the use of this synthetic membrane when screening formulations to be applied in oral penetration studies.

Permeation Protection by Waterproofing Mucosal Membranes.

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

Application of Lavender-Oil Microcapsules to Functionalized PET Fibers.

Surface treatments for textile substrates have received significant attention from researchers around the world. Ozone and plasma treatments trigger a series of surface alterations in textile substrates that can improve the anchoring of other molecules or particles on these substrates. This work aims to evaluate the effect of ozone and plasma treatments on the impregnation of polymeric microcapsules containing lavender oil in polyester fabrics (PES). Microcapsules with walls of chitosan and gum arabic were prepared by complex coacervation and impregnated in PES, plasma-treated PES, and ozone-treated PES by padding. The microcapsules were characterized for their size and morphology and the surface-treated PES was evaluated by FTIR, TGA, SEM, and lavender release. The microcapsules were spherical in shape, with smooth surfaces. The FTIR analyses of the textile substrates with microcapsules showed bands referring to the polymers of the microcapsules, but not to the lavender; this was most likely because the smooth surface of the outer wall did not retain the lavender. The mass loss and the degradation temperatures measured by TGA were similar for all the ozone-treated and plasma-treated polyester samples. In the SEM images, spherical microcapsules and the impregnation of the microcapsules of larger sizes were perceived. Through the lavender release, it was observed that the plasma and ozone treatments interfered both with the amount of lavender delivered and with the control of the delivery.

Formation and Characterization of Oregano Essential Oil Nanocapsules Applied onto Polyester Textile.

Oregano essential oil was encapsulated in poly-ϵ-caprolactone nanoparticles by a nanoprecipitation method using glycerin as a moisturizer. Nanocapsule characterization was performed by measuring the particle size, colloidal stability and encapsulation efficiency using dynamic light scattering, UV-Vis spectrophotometry and scanning electron microscopy (SEM). The nanoparticles had a mean particle size of 235 nm with a monomodal distribution. In addition, a low polydispersity index was obtained, as well as a negative zeta potential of -36.3 mV and an encapsulation efficiency of 75.54%. Nanocapsules were applied to polyester textiles through bath exhaustion and foulard processing. Citric acid and a resin were applied as crosslinking agents to improve the nanocapsules' adhesion to the fabric. The adsorption, desorption, moisture content and essential oil extraction were evaluated to determine the affinity between the nanocapsules and the polyester. The adsorption was higher when the citric acid and the resin were applied. When standard oregano nanocapsules were used, almost all of the impregnated nanoparticles were removed when washed with water. The moisture content was evaluated for treated and non-treated textiles. There was a significant increase in the moisture content of the treated polyester compared to the non-treated polyester, which indicates that the polyester hydrophilicity increased with an important absorption of the essential oil nanocapsules; this can improve fabric comfort and probably promote antibacterial properties.

Lipid distribution on ethnic hairs by Fourier transform infrared synchrotron spectroscopy.

BACKGROUND: A synchrotron-based Fourier transform infrared micro-spectrometer (µ-FTIR) allows the spatial determination of lipids across the different layers of ethnic hairs and differentiates between the lipid order arrangement and quantity. MATERIALS AND METHODS: The three ethnic fibers were delipidized, the lipid extracts were characterized, and the delipidized fibers were studied by dynamic vapor sorption experiments (DVS) and FTIR-synchrotron techniques. RESULTS: The average spectra from the different hair regions exhibited the most intense CH2 sym peaks on the medulla, followed by those from the cuticle and cortex for all hairs of different ethnicities. Differences in the lipid fraction of the three hair types have been observed, and they can explain some barrier properties. African virgin hair was demonstrated to have more lipids mainly in the medulla, which implies an important hydrophobicity with low hysteresis between absorption and desorption water vapor processes. In addition, these lipids are highly disordered, mainly in the cuticle, which can be related to its high water vapor diffusion. Asian and Caucasian virgin hairs presented a similar lipid order in all regions, with similar diffusion coefficients. Results indicate that the higher order of the lipid bilayer hinders water permeation kinetics in some way. CONCLUSION: The differences in the presence and organization of the lipids in the different regions of the African hair can account for its differentiation with regards to moisturization and swelling from the other types of fibers.

Increased Comfort of Polyester Fabrics.

The hydrophilicity of fibers is directly related to the comfort of a fabric and represents one of the most important aspects of a textile. Therefore, polyester (PES) modification has focused on an increase in moisture content and a subsequent improvement of the user's experience. Based on the glycerol hygroscopic properties, the main objective has been the enhancement of the hydrophilicity of polyester by glycerol treatments. Furthermore, microwave irradiation and alkaline treatment have been applied, in order to increase glycerol adhesion. Treated PES samples were characterized by performing moisture content, negative ion, water diffusion and water vapor resistance analyses. The effect of different treatment conditions such as bath ratio (1/10 or 1/15), temperature (40, 60 or 100 °C), time (2 or 5 min) and microwave radiation intensity (300 or 500 W) was evaluated. The moisture content of treated PES results indicated that by decreasing the bath ratio and increasing the time and temperature the moisture gain can reach almost 14%, which can be easily related to increases in the weight of the fiber. The treatment with alkali was done and led to the highest moisture increase. Treatment with 500 W microwave irradiation led to higher glycerol retention after rinsing. Different experimental conditions were applied to the glycerol-treated PES fabrics, and a clear improvement in moisture content was obtained increasing the comfort. The results were compared with the ones obtained for cotton and wool, where the moisture is higher than non treated PES.

Lanolin-Based Synthetic Membranes for Transdermal Permeation and Penetration Drug Delivery Assays.

Due to the high similarity in composition and structure between lanolin and human SC lipids, we will work with two models from wool wax. Two types of lanolin were evaluated: one extracted with water and surfactants (WEL) and the other extracted with organic solvents (SEL). Skin permeation and skin penetration studies were performed with two active compounds to study the feasibility of the use of lanolin-based synthetic membranes as models of mammalian skin. Diclofenac sodium and lidocaine were selected as the active compounds considering that they have different chemical natures and different lipophilicities. In the permeation assay with SEL, a better correlation was obtained with the less permeable compound diclofenac sodium. This assay suggests the feasibility of using artificial membranes with SEL as a model for percutaneous absorption studies, even though the lipophilic barrier should be improved. Penetration profiles of the APIs through the SEL and WEL membranes indicated that the two membranes diminish penetration and can be considered good membrane surrogates for skin permeability studies. However, the WEL membranes, with a pH value similar to that of the skin surface, promoted a higher degree of diminution of the permeability of the two drugs, similar to those found for the skin.

Ethnic hair: Thermoanalytical and spectroscopic differences.

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.

Effect of propylene glycol on the skin penetration of drugs.

Propylene glycol (PG) has been used in formulations as a co-solvent and/or to enhance drug permeation through the skin from topical preparations. Two skin in vitro permeation approaches are used to determine the effect of PG on drug penetration. The in vitro Skin-PAMPA was performed using 24 actives applied in aqueous buffer or PG. PG modulates permeability by increasing or diminishing it in the compounds with poor or high permeability, respectively. Percutaneous absorption using pigskin on Franz diffusion cells was performed on seven actives and their commercial formulations. The commercial formulations evaluated tend to have a lower permeability than their corresponding PG solutions but maintain the compound distribution in the different strata: stratum corneum, epidermis and dermis. The results indicate the enhancer properties of PG for all compounds, especially for the hydrophilic ones. Additionally, the Synchrotron-Based Fourier Transform Infrared microspectroscopy technique is applied to study the penetration of PG and the molecular changes that the vehicle may promote in the different skin layers. Results showed an increase of the areas under the curve indicating the higher amount of lipids in the deeper layers and altering the lipidic order of the bilayer structure to a more disordered lipid structure.

Selective modification of skin barrier lipids.

The molecular organization of stratum corneum (SC) lipids is important for maintaining the barrier properties of the skin. The majority of intercellular lipids are in a solid state at normal humidity (RH) and ambient temperature; however, several studies indicate that a small fraction exist in a fluid state. In a previous work, a preferential solubilization of fluid skin lipids by acetone (Ac) was envisaged. A different change in the skin permeability related to the different lipid structures of the extracted lipids was suggested. To increase the knowledge of the specific role of different lipids on skin structure, a selective lipid modification is proposed. This study assess the effect of Ac on skin barrier lipids in-depth. Synchrotron based Fourier-transform infrared microspectroscopy (FTIR), which is used to study SC lipid organization, revealed a more ordered lipid organization after Ac treatment. In vitro experiments using Franz cells, which were selected to follow the SC barrier function capability, demonstrated that Ac-treated skin retained caffeine and ibuprofen on the SC with very low permeation of both compounds into the deeper skin layers. In vitro transepidermal water loss (TEWL) measurements revealed the ability of Ac to induce a less water permeated skin. Although an important lipid fraction has been removed, Ac skin treatment brings to a skin where the remaining lipids promote an improved barrier function. These results could lead to a better understanding of the role of different lipid components in skin structure.

External lipid function in ethnic hairs.

OBJECTIVE: The main aim of this study is to characterize the external lipids of different ethnic hairs and to study the contribution of the exogenous lipids on their physicochemical properties. METHODS: On the extraction procedure, sebaceous lipids from the exterior of the fiber are removed. The influence of those free lipids on the hair properties, such as contact angle, mechanical characteristics, and sorption of water, will be evaluated to determine permeation characteristics of the keratin fibers. Relationship with lipid order was also determined by infrared spectroscopy (IR). RESULTS: Lipid extraction indicates the greatest amount of total lipids for African hair. Caucasian lipid extracts present the higher melting point and phase transition temperatures. This could be related to higher hydration and lower diffusion coefficient of the Caucasian fibers. A decrease in moisture was found in the lipid-extracted fibers. This diminution of the maximum water regain in all cases could be due to a higher water desorption. IR results indicate that Caucasian and moreover African native fibers present the most quantity of lipids, and the similar frequency of all fibers indicates a lamellar/orthorhombic order arrangement. CONCLUSION: The hexane/tert-butanol extraction was demonstrated to modify not only cuticular but also cortex lipids. Exogenous lipid depletion in all fibers indicates a less water content and higher water desorption. However, lipid depleted Caucasian fibers presents an increase in the lipid order which could be related to the different saturation of the lipid extract and its improvement in breaking tenacity.

Lipid loses and barrier function modifications of the brown-to-white hair transition.

BACKGROUND: The main objective of this study was to determine the lipid profile of brown and white Caucasian hair fibres and the effects of lipids on the properties of fibres. MATERIALS AND METHODS: To determine the structures of white and brown hair lipid bilayers, cross sections of fibres of both hair types were examined using synchrotron-based µ-FTIR mapping. Dynamic vapour sorption (DVS) analyses were also performed to determine the differences in the barrier function of both fibres. RESULTS: Spatial identification of lipids showed that a great amount of lipids was present in the medulla of fibres of both hair types, but important differences were also observed between cuticles of the different fibres. The cuticle of a white hair fibre showed a significant decrease in its lipid content, but did not show differences in the lateral packing order with respect to the cuticle of a brown hair fibre. The cortex and medulla of the white hair fibre also exhibited a significant decrease in its lipid content but with a higher lateral packing order than brown hair. Using DVS analysis, it was found that the water dynamics of white hair fibres differed from those of brown hair fibres, showing a decrease in their total capacity to absorb water and an increase in the velocity of the exchange of water with the environment. CONCLUSION: The results of both techniques demonstrated a high correlation between the characteristics of the lipids located in the cuticle and the water dynamics of the fibres.

Vehiculation of Active Principles as a Way to Create Smart and Biofunctional Textiles.

In some specific fields of application (e.g., cosmetics, pharmacy), textile substrates need to incorporate sensible molecules (active principles) that can be affected if they are sprayed freely on the surface of fabrics. The effect is not controlled and sometimes this application is consequently neglected. Microencapsulation and functionalization using biocompatible vehicles and polymers has recently been demonstrated as an interesting way to avoid these problems. The use of defined structures (polymers) that protect the active principle allows controlled drug delivery and regulation of the dosing in every specific case. Many authors have studied the use of three different methodologies to incorporate active principles into textile substrates, and assessed their quantitative behavior. Citronella oil, as a natural insect repellent, has been vehicularized with two different protective substances; cyclodextrine (CD), which forms complexes with it, and microcapsules of gelatin-arabic gum. The retention capability of the complexes and microcapsules has been assessed using an in vitro experiment. Structural characteristics have been evaluated using thermogravimetric methods and microscopy. The results show very interesting long-term capability of dosing and promising applications for home use and on clothes in environmental conditions with the need to fight against insects. Ethyl hexyl methoxycinnamate (EHMC) and gallic acid (GA) have both been vehicularized using two liposomic-based structures: Internal wool lipids (IWL) and phosphatidylcholine (PC). They were applied on polyamide and cotton substrates and the delivery assessed. The amount of active principle in the different layers of skin was determined in vitro using a Franz-cell diffusion chamber. The results show many new possibilities for application in skin therapeutics. Biofunctional devices with controlled functionality can be built using textile substrates and vehicles. As has been demonstrated, their behavior can be assessed using in vitro methods that make extrapolation to their final applications possible.

Lanolin-Based Synthetic Membranes as Percutaneous Absorption Models for Transdermal Drug Delivery.

BACKGROUND: The major in vitro permeation studies are currently performed in Franz-type diffusion cells because of their simplicity, cost effectiveness and because the experimental conditions can be easily controlled. Apart from the skin, Franz-type diffusion cells can be used with synthetic membranes. Nevertheless, they do not emulate the nature of the lipidic matrix, which is responsible for the topical barrier function. OBJECTIVE: This paper offers two new approaches combining different synthetic membranes (Strat-M® and Nucleopore®) with lanolin, which provides lipidic components similar to the lipidic matrix. METHODS: The molecular structure of lanolin was studied in membranes by attenuated total reflectance infrared spectroscopy (ATR-IR). The water permeability and absorption of lidocaine, diclofenac sodium and betamethasone dipropionate were also studied and compared against free-lanolin membranes and skin. RESULTS: The results showed an increasing barrier function after lanolin application in both membranes, resulting in a decrease in water permeability. Observing the IR spectra, the lateral packaging of the lipid in the synthetic membranes seems to emulate the orthorhombic disposition from the stratum corneum. Moreover, the three substances applied to the lanolin-containing membranes have a similar absorption to that of the skin. CONCLUSIONS: In conclusion, combining synthetic membranes with lanolin may be a useful approach to mimic topical actives’ absorption.

Solvent-Extracted Wool Wax: Thermotropic Properties and Skin Efficacy.

BACKGROUND/AIMS: Wool wax is a soft, yellow, waxy substance that is secreted by the sebaceous glands of sheep. The purpose of wool wax is to waterproof and protect the wool. Chemically, wool wax is a complex mixture of esters, fatty acids, and alcohols. Wool waxes with different prop-erties can be obtained by following different extraction methodologies. METHODS: Two differently extracted wool waxes are compared in this study. Their effectiveness in mimicking the properties of skin lipids is evaluated. In addition, the lipid compositions and thermotropic behaviours of the 2 differently extracted wool waxes were evaluated. RESULTS: The solvent-extracted wool wax was found to have a significantly higher polar lipid content than that of the water-extracted wool wax. This increase in the polar character of the solvent-extracted wool wax was also demonstrated by increased values of transition and degradation temperatures in the differential scanning calorimetry and thermogravimetric analyses, respectively. In addition, solvent-extracted wool wax demonstrated the ability to reinforce stratum corneum lipids, which led to improved skin barrier function. CONCLUSIONS: The suitability of the solvent-extracted wool wax for application in the preparation of cosmetics and dermatological products was demonstrated.

Skin barrier modification with organic solvents.

The primary barrier to body water loss and influx of exogenous substances resides in the stratum corneum (SC). The barrier function of the SC is provided by patterned lipid lamellae localized to the extracellular spaces between corneocytes. SC lipids are intimately involved in maintaining the barrier function. It is generally accepted that solvents induce cutaneous barrier disruption. The main aim of this work is the evaluation of the different capability of two solvent systems on inducing changes in the SC barrier function. SC lipid modifications will be evaluated by lipid analysis, water sorption/desorption experiments, confocal-Raman visualization and FSTEM images. The amount of SC lipids extracted by chloroform/methanol was significantly higher than those extracted by acetone. DSC results indicate that acetone extract has lower temperature phase transitions than chloroform/methanol extract. The evaluation of the kinetics of the moisture uptake and loss demonstrated that when SC is treated with chloroform/methanol the resultant sample reach equilibrium in shorter times indicating a deterioration of the SC tissue with higher permeability. Instead, acetone treatment led to a SC sample with a decreased permeability thus with an improved SC barrier function. Confocal-Raman and FSTEM images demonstrated the absence of the lipids on SC previously treated with chloroform/methanol. However, they were still present when the SC was treated with acetone. Results obtained with all the different techniques used were consistent. The results obtained increases the knowledge of the interaction lipid-solvent, being this useful for understanding the mechanism of reparation of damaged skin.

Mass transport model through the skin by microencapsulation system.

Skin drug delivery can be subdivided into topical and transdermal administration. Transdermal administration can take advantage of chemical and physical strategies that can improve skin permeability and allow drug penetration. In this study, the development of a skin penetration profile was carried out by an in vitro technique for a microencapsulated system of ibuprofen. Release experiments were performed using percutaneous absorption tests to determine the evolution of the principle present in each of the different skin compartments as a function of time. A general kinetic model for a microencapsulated structure as a mass transport system through the skin was applied: [Formula: see text] This model could predict the penetration profile of encapsulated substances through skin from biofunctional textiles as well as estimate the dosage profile of the active principle. The apparent diffusion coefficients found were 1.20 × 10(-7 )cm/s for the stratum corneum and higher for the rest of the skin 6.67 × 10(-6 )cm/s.

Skin delivery of antioxidant surfactants based on gallic acid and hydroxytyrosol.

OBJECTIVES: The aim of this study has been to investigate the dermal absorption profile of the antioxidant compounds gallic acid and hydroxytyrosol as well as their derivatives, hexanoate (hexyl gallate and hydroxytyrosol hexanoate) and octanoate (octyl gallate and octanoate derivative) alkyl esters (antioxidant surfactants). Previously, the scavenging capacity of these compounds, expressed as efficient dose ED50, has also determined. METHODS: The percutaneous absorption of these compounds was obtained by an in vitro methodology using porcine skin biopsies on Franz static diffusion cells. The antiradical activity of compounds was determined using the 1,1-diphenyl-2-picrylhydrazyl free radical method. KEY FINDINGS: The percutaneous penetration results show the presence of antioxidants in all layers of the skin. The content of the cutaneously absorbed compound is higher for the antioxidant surfactants (ester derivatives). This particular behaviour could be due to the higher hydrophobicity of these compounds and the presence of surface activity in the antioxidant surfactants. CONCLUSIONS: These new antioxidant surfactants display optimum properties, which may be useful in the preparation of emulsified systems in cosmetic and pharmaceutical formulations because of their suitable surface activity and because they can protect the skin from oxidative damage.

Antioxidative effects and percutaneous absorption of five polyphenols.

A new strategy was designed to evaluate the antioxidant effectiveness of five topically applied polyphenols following skin penetration profiles. The antioxidants were the following polyphenol derivatives: epicatechin, resveratrol, rutin, quercetin, and trolox, which was used as the reference antioxidant. The hydrophilic/lipophilic character of these compounds was evaluated, and their antioxidant activity was measured by the DPPH method. The percutaneous absorption of these polyphenols was obtained by an in vitro methodology using porcine skin biopsies. This methodology involves the quantification of the antioxidants present in each specific skin layer to evaluate antioxidant effectiveness. The antioxidant activity in each skin layer was also determined by the DPPH method. The results indicated that lipophilic antioxidants (epicatechin, resveratrol, quercetin, and trolox) penetrated deeper into the skin layers, whereas a more hydrophilic compound, rutin, remained on the skin surface. The antioxidant evaluation of each skin compartment suggested that resveratrol and rutin were the most effective topically applied compounds in view of their antioxidant activity and their skin penetration profile.

Textiles with gallic acid microspheres: in vitro release characteristics.

Abstract The aim of this study was to demonstrate the skin penetration of an antioxidant, gallic acid (GA), encapsulated in poly-ε-caprolactone (PCL) microspheres and applied onto textile fabrics, by a specific in vitro percutaneous absorption methodology. Two techniques (particle size distribution and FTIR) were used to characterise the microspheres obtained. The amount of GA-loaded microspheres present in the biofunctional textiles was established before their use as a textile drug delivery system. More absorption and desorption of microspheres with GA for the polyamide fabric were found in comparison with cotton fabric. The percutaneous absorption results indicated that the skin penetration of GA released from PCL-microspheres that were applied directly to the skin was higher than when GA was embedded within biofunctional textiles, in conclusion, an interesting reservoir effect may be promoted when biofunctional textiles were used.