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.

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.

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.

Assessment of Finite and Infinite Dose In Vitro Experiments in Transdermal Drug Delivery.

Penetration, usually with finite dosing, provides data about the total active amount in the skin and permeation, being the most used methodology, usually with infinite dosing, leads to data about pharmacokinetic parameters. The main objective of this work is to assess if results from permeation, most of them at finite dose, may be equivalent to those from penetration usually at infinite dose. The transdermal behavior of four drugs with different physicochemical properties (diclofenac sodium, ibuprofen, lidocaine, and caffeine) was studied using penetration/finite and kinetic permeation/infinite dose systems using vertical Franz diffusion cells to determine the relationships between permeation and penetration profiles. Good correlation of these two in vitro assays is difficult to find; the influence of their dosage and the proportion of different ionized/unionized compounds due to the pH of the skin layers was demonstrated. Finite and infinite dose regimens have different applications in transdermal delivery. Each approach presents its own advantages and challenges. Pharmaceutical industries are not always clear about the method and the dose to use to determine transdermal drug delivery. Being aware that this study presents results for four actives with different physicochemical properties, it can be concluded that the permeation/infinite results could not be always extrapolated to those of penetration/finite. Differences in hydrophilicity and ionization of drugs can significantly influence the lack of equivalence between the two methodologies. Further investigations in this field are still needed to study the correlation of the two methodologies and the main properties of the drugs that should be taken into account.

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.

Prediction of the skin permeability of topical drugs using in silico and in vitro models.

The main challenge of topically applied drugs is to overcome the skin barrier to reach the site of action at the concentration needed for efficacy. In the research of new topical drugs, design of molecules with optimized properties for skin penetration is a key factor and assays for its characterization are needed. A group of 20 representative topical molecules of clinical use were studied in two in silico models (Potts & Guy and Barratt), and an in vitro assay with artificial membrane (Skin-PAMPA). A subset of 9 drugs were also evaluated in the Franz cells assay, formulated in a solvent and in a marketed formulation. Each assay allowed us to grade compounds according to their permeability value. Globally good alignments were found for the studied compounds when comparing models, although discrepancies for some compounds such as tazarotene, tacrolimus, ketoconazole and metronidazole were observed. Overall, the studied in silico and the in vitro models are useful tools to support selection and characterization of research compounds in terms of skin permeability.

In vitro penetration through the skin layers of topically applied glucocorticoids.

Corticoids are actives widely used in the treatment of skin diseases. This work aims to study the penetration of 3 corticoids (betamethasone, clobetasol, and flurandrenolide), their relationship with their Log D values and the effects of the vehicles. The 3 compounds were applied on a Franz-type diffusion cell in propylene glycol solution and their respective commercial creams and ointments. The active amounts found in the stratum corneum, epidermal, and dermal layers of the skin were investigated. Their diffusions were greatly affected by the formulation; moreover higher amounts of substance in the epidermis and dermis were detected in ointments than in creams. The enhancement effect of propylene glycol was also observed. The differences between the 3 substances could be related to their lipophilicity, molecular structure, and molecular weight. The more hydrophobic compounds (clobetasol and betamethasone) are present in higher amounts in the epidermis and dermis, while the hydrophilic compound (flurandrenolide) is mostly present in the receptor fluid.

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.