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Lipid Matrix (lipid + matrix)

Distribution by Scientific Domains

Chemistry	50%
Medical Sciences	33%

Selected Abstracts

pH-induced alterations in stratum corneum properties

INTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 3 2003
K. P. Ananthapadmanabhan
Synopsis Skin-cleansing compositions based on alkyl carboxylates (soaps) have a higher irritation potential than those based on syndet surfactants such as alkyl isethionates or alkyl ether sulphates. Contributing factors include inherent differences in the irritation potential of soaps and syndet surfactants, pH-induced changes in surfactant solution chemistry, and the direct effects of pH on the physical properties of the stratum corneum (SC). Past work has not directly addressed the effect of solution pH on the SC itself and its potential role in cleanser-induced skin irritation. In the current work, alterations to SC properties induced by buffered pH solutions and two strongly ionizable surfactants, sodium dodecyl sulphate and sodium lauryl ether sulphate, at different pH values are measured. By utilizing optical coherence tomography (OCT) and infrared (IR) spectroscopy we have directly measured physical changes in SC proteins and lipids. Our results indicate that SC swelling, which reflects alterations to SC structural proteins, is increased significantly at pH 10, compared to pH 4 and 6.5. The transition temperature (Tm) of SC lipids is found to increase at pH 10, compared to pH 4 and 6.5, suggesting a more rigid SC lipid matrix. Surfactants cause a further increase in swelling and lipid rigidity. Some aspects of what these results mean for SC physical properties as well as their implications to potential mechanisms of surfactant-induced skin irritation are discussed. Résumé Les compositions nettoyantes pour la peau à base d'alkyl carboxylates (savons) ont un potentiel irritant supérieur à celles à base de syndet tensioactifs tels que les alkyl isothionates ou les alkyl ether sulfates. Les facteurs en cause comprennent les différences de potentiel irritant inhérentes aux savons et aux syndet tensioactifs, les modifications de la chimie de la solution de tensioactif dues aux pH, et les effets directs du pH sur les propriétés physiques de la couche cornée (CC). Les travaux antérieurs n'ont pas traité directement l'effet du pH de la solution sur la couche cornée elle-même et son rôle potentiel dans l'irritation de la peau due à la solution nettoyante. Dans la présente étude on a mesuré les altérations des propriétés de la CC causées par des solutions à pH tamponné et deux tensioactifs fortement ionisables, le dodecyl sulfate de sodium et le lauryl ether sulfate de sodium, à différentes valeurs de pH. En utilisant la tomographie optique (OCT) et la spectroscopie à infrarouge (IR) on a mesuré directement les modifications physiques des protéines et des lipides de la CC. Nos résultats montrent que le gonflement de la CC, qui traduit des altérations des protéines structurales de la CC, augmente significativement à pH 10, par comparaison au pH 4 et 6.5. On observe que la température de transition (Tm) des lipides de la CC augmente à pH 10, par comparaison au pH 4 et 6.5, suggérant une matrice lipidique de la CC plus rigide. Les tensioactifs provoquent une augmentation plus importante du gonflement et de la rigidité lipidique. On aborde certains aspects de la signification de ces résultats vis-à-vis des propriétés physiques de la couche cornée ainsi que leurs conséquences sur les mécanismes potentiels de l'irritation de la peau causée par les tensioactifs. [source]

An investigation into the mechanism of dissolution rate enhancement of poorly water-soluble drugs from spray chilled gelucire 50/13 microspheres

JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 1 2010
Sheng Qi
Abstract The production and physicochemical characterisation of spray chilled Gelucire 50/13 microspheres is described with a view to improving the dissolution of a poorly water-soluble drug, piroxicam, and understanding the fundamental mechanisms associated with the improved drug release. Thermorheological testing was developed as a fast screening method for predicting the processability of dispersions for spray chilling preparation. Spray chilled piroxicam loaded microspheres were spherical in shape with a median diameter of circa 150,µm. DSC indicated no interaction between piroxicam and lipid matrix, while HSM studies performed in polarized light mode indicated that the spheres contained distinct drug crystals. Polarising light microscopy and small-angle XRD investigations on the hydration behaviour of the lipid and the spray chilled microspheres revealed the formation of liquid crystalline phases depending on the degree of hydration. The dissolution behaviour of the piroxicam loaded microspheres showed significant improvements compared to drug alone. The particle size, drug loading and aging of the microspheres were all found to have an influence on the release behaviour. It was proposed that Gelucire 50/13 microspheres release the entrapped piroxicam via formation of a lyotropic liquid crystalline phase, which allows dissolution of the drug particles in a finely divided, high surface area and well-wetted state. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:262,274, 2010 [source]

An evaluation of mathematical models for predicting skin permeability

JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 1 2008
Guoping Lian
Abstract A number of mathematical models have been proposed for predicting skin permeability, mostly empirical and very few are deterministic. Early empirical models use simple lipophilicity parameters. The recent trend is to use more complicated molecular structure descriptors. There has been much debate on which models best predict skin permeability. This article evaluates various mathematical models using a comprehensive experimental dataset of skin permeability for 124 chemical compounds compiled from various sources. Of the seven models compared, the deterministic model of Mitragotri gives the best prediction. The simple quantitative structure permeability relationships (QSPR) model of Potts and Guy gives the second best prediction. The two models have many features in common. Both assume the lipid matrix as the pathway of transdermal permeation. Both use octanol,water partition coefficient and molecular size. Even the mathematical formulae are similar. All other empirical QSPR models that use more complicated molecular structure descriptors fail to provide satisfactory prediction. The molecular structure descriptors in the more complicated QSPR models are empirically related to skin permeation. The mechanism on how these descriptors affect transdermal permeation is not clear. Mathematically it is an ill-defined approach to use many colinearly related parameters rather than fewer independent parameters in multi-linear regression. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:584,598, 2008 [source]

Liposomes in investigative dermatology

PHOTODERMATOLOGY, PHOTOIMMUNOLOGY & PHOTOMEDICINE, Issue 5 2001
Daniel B. Yarosh
Liposomes are microscopic spheres, usually composed of amphiphilic phospholipids. They may be useful without skin penetration if they simply protect or sequester compounds that would otherwise be unstable in the formulation. Liposomes that remain on the skin surface are useful as light-absorbers, agents to deliver color or sunscreens, or as depots for timed-release. Liposomes that penetrate the stratum corneum have the potential to interact with living tissue. Topically applied liposomes can either mix with the stratum corneum lipid matrix or penetrate the stratum corneum by exploiting the lipid-water interface of the intercellular matrix. There are at least four major routes of entry into the skin: pores, hair follicles, columnular spaces and the lipid:water matrix between squames. A major force driving liposome penetration is the water gradient, and flexible liposomes are best able to exploit these delivery opportunities. Some liposomes release their contents extracellularly. Topical application of photosensitizers may be enhanced by encapsulation in liposomes. Higher and longer-lasting drug concentrations may be produced in localized areas of skin, particularly at disease sites where the stratum corneum and the skin barrier function are disrupted. The liposome membrane should be designed to capture lipophilic drugs in the membrane or hydrophilic drugs in the interior. Other types of liposomes can be engineered to be taken up by cells. Once inside cells, the lysosomal sac and clatherin-coated pit are the dead-end destinations for liposomes unless an escape path has been engineered into the liposome. A novel method has been developed to allow delivery into cells of the skin, by escape from the lysosomal sac. These liposomes have been used to topical deliver active DNA repair enzymes from liposomes into epidermal cells and to enhance DNA repair of UV-irradiated skin. From these studies a tremendous amount has been learned about the relationship of DNA damage and skin cancer. Both mutations and immunosuppression appear to be essential to skin cancer and both are induced by DNA damage. DNA damage produces immediate effects by inducing the expression of cytokines, which means that DNA damage can induce signaling in neighboring, undamaged cells. The repair of only a fraction of the DNA damage has a disproportionate effect on the biological responses, clearly demonstrating that not all DNA damage is equivalent. This technology demonstrates that biologically active proteins can be delivered into the cells of skin, and opens up a new field of correcting or enhancing skin cell metabolism to improve human health. [source]

Invertase-Lipid Biocomposite Films: Preparation, Characterization, and Enzymatic Activity

BIOTECHNOLOGY PROGRESS, Issue 1 2004
Sumant Phadtare
The formation of biocomposite films of the industrially important enzyme invertase and fatty lipids under enzyme-friendly conditions is described. The approach involves a simple beaker-based diffusion protocol wherein invertase diffuses into the cationic lipid octadecylamine during immersion of the lipid film in the enzyme solution. Entrapment of invertase in the octadecylamine film is highly pH-dependent, underlining the role of attractive electrostatic interactions between the enzyme and the lipid in the biocomposite film formation. The kinetics of formation of the enzyme-lipid biocomposites has been studied by quartz crystal microgravimetry (QCM) measurements. The stability of the enzyme in the lipid matrix was confirmed by fluorescence spectroscopy and biocatalytic activity measurements. The biocatalytic activity of the invertase-lipid biocomposite films was comparable to that of the free enzyme in solution and showed marginally higher temperature stability. Particularly exciting was the excellent reuse characteristics of the biocomposite films, indicating potential industrial application of these films. [source]

Giant Vesicles: Preparations and Applications

CHEMBIOCHEM, Issue 7 2010
Peter Walde Prof. Dr.
Abstract There is considerable interest in preparing cell-sized giant unilamellar vesicles from natural or nonnatural amphiphiles because a giant vesicle membrane resembles the self-closed lipid matrix of the plasma membrane of all biological cells. Currently, giant vesicles are applied to investigate certain aspects of biomembranes. Examples include lateral lipid heterogeneities, membrane budding and fission, activities of reconstituted membrane proteins, or membrane permeabilization caused by added chemical compounds. One of the challenging applications of giant vesicles include gene expressions inside the vesicles with the ultimate goal of constructing a dynamic artificial cell-like system that is endowed with all those essential features of living cells that distinguish them from the nonliving form of matter. Although this goal still seems to be far away and currently difficult to reach, it is expected that progress in this and other fields of giant vesicle research strongly depend on whether reliable methods for the reproducible preparation of giant vesicles are available. The key concepts of currently known methods for preparing giant unilamellar vesicles are summarized, and advantages and disadvantages of the main methods are compared and critically discussed. [source]