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.

Approach to design space from retrospective quality data.

CONTEXT: Nowadays, the entire manufacturing process is based on the current GMPs, which emphasize the reproducibility of the process, and companies have a lot of recorded data about their processes. OBJECTIVE: The establishment of the design space (DS) from retrospective data for a wet compression process. MATERIALS AND METHODS: A design of experiments (DoE) with historical data from 4 years of industrial production has been carried out using the experimental factors as the results of the previous risk analysis and eight key parameters (quality specifications) that encompassed process and quality control data. RESULTS: Software Statgraphics 5.0 was applied, and data were processed to obtain eight DS as well as their safe and working ranges. DISCUSSION AND CONCLUSION: Experience shows that it is possible to determine DS retrospectively, being the greatest difficulty in handling and processing of high amounts of data; however, the practicality of this study is very interesting as it let have the DS with minimal investment in experiments since actual production batch data are processed statistically.

Damaged hair retrieval with ceramide-rich liposomes.

Lipids from human hair consist mainly of cholesterol esters, free fatty acids, cholesterol, ceramides, and cholesterol sulfate. They are structured as lipid bilayers in the cell membrane complex (CMC) and make a large contribution to diffusion, cell cohesion, and mechanical strength. The loss of these lipids could impair the integrity of the hair, leading to deterioration in its tensile properties. Internal wool lipids (IWL) resemble those of the membranes of other keratinic tissues such as human hair or stratum corneum. The application of IWL structured as liposomes on pretreated hair samples has been demonstrated to restore the natural properties of the fibers. This study seeks to apply IWL liposomes to untreated hair fibers and to hair fibers subjected to chemical treatment. Differences in the lipidic composition of all chemically treated hairs were found with respect to the untreated ones. Lipid recovery of damaged hair due to the application of IWL liposomes was corroborated by lipid analysis of the hair. A high resistance to break of hair samples post-treated with IWL liposomes was observed. An increase in hydrogen bonds and electrostatic forces and an improvement in the cohesion between matrix and filaments were detected, probably because of some lipid recovery.

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.

The role of SeDeM for characterizing the active substance and polyvinyilpyrrolidone eliminating metastable forms in an oral lyophilizate-A preformulation study.

A preformulation study of an oral lyophilisate with cetirizine dihydrochloride (CTZ) as active ingredient, mannitol and PVP K30 as bulking agents is presented. CTZ shown a humidity content of 0.150% and a spontaneous hygroscopicity of 0.200% (both determined by SeDeM diagram), demonstrating an adequate stability behavior in solid form. A design of experiments (DoE) performed with both mannitol and PVP K30, followed by a simple factorial design (32) has determined the optimum combination of excipients and CTZ, and showed that a higher proportion of PVP K30 was able to prevent metastable forms generated by mannitol.

Adsolubilisation of organic compounds onto collagen fibres.

Adsolubilisation has been defined as the incorporation to solid-water interfaces of molecules that do not adsorb spontaneously to such interfaces, but can be incorporated through an interaction with an adsorbing surfactant molecule. The aim of this work was to study the adsolubilisation of organic molecules with different hydrophobicity on collagen fibres. Hide powder collagen was treated under mild acidic aqueous conditions with an anionic surfactant, sodium dodecylbenzene sulphonate. Thereafter, five different organic molecules, i.e., benzyl alcohol, 2-naphtol, pararosaniline, hexamethylpararosaniline and nonylphenol with 10 mol ethylene oxide were separately applied to the treated collagen in order to study adsolubilisation as a function of their hydrophobicity. It was found that under acidic conditions all molecules were scarcely adsorbed or not adsorbed by the native hide powder collagen. However, all organic molecules, except benzyl alcohol, were adsolubilised if the hide powder collagen was previously treated with the anionic surfactant. The hydrophobicity of the molecules plays an important role in the adsolubilisation phenomenon with the result that the higher the hydrophobicity (nonylphenol with 10 mol ethylene oxide), the higher the adsolubilisation.

On the generation and outcome of 3-(N-phenylamino)propane-1,2-diol derivatives in deodorized model oils related to toxic oil syndrome.

Toxic Oil Syndrome (TOS) was a massive food-born intoxication that occurred in Spain in 1981 and affected more than 20,000 people. TOS was attributed to the ingestion of rapeseed oil that had been adulterated with aniline, illegally refined, and delivered for human consumption. Two chemical species derived from aniline have been identified in oil batches: fatty acid anilides, qualified as biomarkers of the adulterated oil, and fatty acid esters of 3-(N-phenylamino)propane-1,2-diol (PAP), considered toxic oil biomarkers. These esters were generated by chemical processes during oil refining, specifically in the deodorization step, which involves treatment of the oil at high temperatures under vacuum to remove volatile contaminants. Since PAP derivatives are strongly associated with TOS, their formation and putative interconversion in a toxic oil model has been studied. The main results obtained are (i) only triglycerides and aniline are required to produce PAP esters, thus eliminating the possibility that unknown activators present in the deodorization tank were required for toxification of the oil; (ii) PAP and PAP mono- and diesters are chemically interrelated, as are anilides and PAP esters to an even higher degree. In addition to the reaction of aniline with triglycerides, anilides can be also formed via attack of PAP esters by aniline. However, the most important source of anilides during deodorization seems to be the thermal decomposition of PAP esters. Overall, these results suggest that the generation and outcome of PAP derivatives during deodorization is a complex scenario whereby PAP esters are not only generated from different reactions but decompose to produce anilides, among other compounds. In addition to providing a rapeseed oil model that reproduces the composition of case oils with respect to anilides and PAP derivatives, the results presented herein further support the hypothesis imputing PAP diesters or their metabolites for the intoxication episode.