Enhancement of percutaneous absorption by laurocapram. 1992

T Ogiso, and M Iwaki, and K Bechako, and Y Tsutsumi
Faculty of Pharmaceutical Sciences, Kinki University, Osaka, Japan.

The in vitro treatment of shed snake skin and hairless rat skin with laurocapram resulted in dramatic decreases in the amounts of cholesterol, phospholipids, and ceramides but not triglycerides in the skins. Scanning electron microscopic observations of hairless rat skin treated with laurocapram indicated looseness and cell separation of the stratum corneum probably caused by the extensive extraction of the intercellular lipids. An ESR study demonstrated the increased fluidity of the corneum lipids after laurocapram treatment. The apparent rotational correlation time of 16-doxyl-stearic acid was decreased by 1.6-2 times after treatment with laurocapram. No penetration of laurocapram itself through shed snake skin and hairless rat skin was detected in vitro, except when the reservoir solvent was 60% ethanol or propylene glycol. The enhancer was hardly metabolized during a 48-h incubation with skin homogenate. Pretreatment of shed snake skin with laurocapram increased significantly the penetration of sulfanilamide and indomethacin through the skin. These results indicate that laurocapram penetrating into the stratum corneum interacts with structured lipids in the intercellular channels and releases them, thereby enhancing the penetration of hydrophilic drugs through the channels. Additionally, laurocapram penetrating into the intracellular matrix of the corneum fluidizes the intracellular lipids and causes the reduction of diffusional resistance.

UI MeSH Term Description Entries
D007213 Indomethacin A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. Amuno,Indocid,Indocin,Indomet 140,Indometacin,Indomethacin Hydrochloride,Metindol,Osmosin
D007424 Intracellular Fluid The fluid inside CELLS. Fluid, Intracellular,Fluids, Intracellular,Intracellular Fluids
D008055 Lipids A generic term for fats and lipoids, the alcohol-ether-soluble constituents of protoplasm, which are insoluble in water. They comprise the fats, fatty oils, essential oils, waxes, phospholipids, glycolipids, sulfolipids, aminolipids, chromolipids (lipochromes), and fatty acids. (Grant & Hackh's Chemical Dictionary, 5th ed) Lipid
D008297 Male Males
D008855 Microscopy, Electron, Scanning Microscopy in which the object is examined directly by an electron beam scanning the specimen point-by-point. The image is constructed by detecting the products of specimen interactions that are projected above the plane of the sample, such as backscattered electrons. Although SCANNING TRANSMISSION ELECTRON MICROSCOPY also scans the specimen point by point with the electron beam, the image is constructed by detecting the electrons, or their interaction products that are transmitted through the sample plane, so that is a form of TRANSMISSION ELECTRON MICROSCOPY. Scanning Electron Microscopy,Electron Scanning Microscopy,Electron Microscopies, Scanning,Electron Microscopy, Scanning,Electron Scanning Microscopies,Microscopies, Electron Scanning,Microscopies, Scanning Electron,Microscopy, Electron Scanning,Microscopy, Scanning Electron,Scanning Electron Microscopies,Scanning Microscopies, Electron,Scanning Microscopy, Electron
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D004578 Electron Spin Resonance Spectroscopy A technique applicable to the wide variety of substances which exhibit paramagnetism because of the magnetic moments of unpaired electrons. The spectra are useful for detection and identification, for determination of electron structure, for study of interactions between molecules, and for measurement of nuclear spins and moments. (From McGraw-Hill Encyclopedia of Science and Technology, 7th edition) Electron nuclear double resonance (ENDOR) spectroscopy is a variant of the technique which can give enhanced resolution. Electron spin resonance analysis can now be used in vivo, including imaging applications such as MAGNETIC RESONANCE IMAGING. ENDOR,Electron Nuclear Double Resonance,Electron Paramagnetic Resonance,Paramagnetic Resonance,Electron Spin Resonance,Paramagnetic Resonance, Electron,Resonance, Electron Paramagnetic,Resonance, Electron Spin,Resonance, Paramagnetic
D004817 Epidermis The external, nonvascular layer of the skin. It is made up, from within outward, of five layers of EPITHELIUM: (1) basal layer (stratum basale epidermidis); (2) spinous layer (stratum spinosum epidermidis); (3) granular layer (stratum granulosum epidermidis); (4) clear layer (stratum lucidum epidermidis); and (5) horny layer (stratum corneum epidermidis).
D000077145 Sulfanilamide A short-acting sulfonamide used as an anti-infective agent. It has lower anti-bacterial activity than SULFAMETHOXAZOLE. 4-aminobenzenesulfonamide,Azol Polvo,Sulfanilamide Barium Salt,Sulfanilamide Cadmium Salt,Sulfanilamide Hydrochloride,Sulfanilamide Lithium Salt,Sulfanilamide Magnesium Salt,Sulfanilamide Monohydrate,Sulfanilamide Silver Salt,Sulfanilamide Sodium,Sulfanilamide Sodium Salt,Sulfanilamide Strontium Salt,Sulfanilamide Zinc Salt,Sulphanilamide,4 aminobenzenesulfonamide
D000279 Administration, Cutaneous The application of suitable drug dosage forms to the skin for either local or systemic effects. Cutaneous Drug Administration,Dermal Drug Administration,Drug Administration, Dermal,Percutaneous Administration,Skin Drug Administration,Transcutaneous Administration,Transdermal Administration,Administration, Dermal,Administration, Transcutaneous,Administration, Transdermal,Cutaneous Administration,Cutaneous Administration, Drug,Dermal Administration,Drug Administration, Cutaneous,Skin Administration, Drug,Administration, Cutaneous Drug,Administration, Dermal Drug,Administration, Percutaneous,Administrations, Cutaneous,Administrations, Cutaneous Drug,Administrations, Dermal,Administrations, Dermal Drug,Administrations, Percutaneous,Administrations, Transcutaneous,Administrations, Transdermal,Cutaneous Administrations,Cutaneous Administrations, Drug,Cutaneous Drug Administrations,Dermal Administrations,Dermal Drug Administrations,Drug Administrations, Cutaneous,Drug Administrations, Dermal,Drug Skin Administrations,Percutaneous Administrations,Skin Administrations, Drug,Skin Drug Administrations,Transcutaneous Administrations,Transdermal Administrations

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