Deoxycholate-hydrogels: novel drug carrier systems for topical use.
Na-deoxycholate (Na-DOC) forms a viscous thixotropic gel when in contact with excess buffer systems. The resulting gels have been tested as novel drug carrier systems for topical use. The influence of differing amounts of mannitol, glycerol and xylitol on the viscous modulus (G"/Pa) was evaluated by oscillatory measurements. Na-DOC (0.5%) in phosphate buffered saline (PBS) with 5% mannitol was chosen as an optimised formulation, taking into account viscosity, distribution and appearance. The release rate of the model drug rutin through an artificial membrane was higher than those from hydroxyethylcellulose- (HEC) and sodium polyacrylate (NaC934)-gels; permeation through excised rat skin was also highest for the Na-DOC systems. The results indicate that Na-DOC significantly increases the membrane permeability. The microbial stability was in the same range as HEC- and NaC934-gels, making a preservation necessary. Na-DOC-gels are novel low molecular weight, multifunctional drug carriers, which also act as penetration enhancers. Their thixotropy is an additional advantage for better application to large skin areas, nasal, vaginal and buccal membranes. Therefore, Na-DOC-gels can be considered promising, alternative drug carrier systems for topical pharmaceutical as well as cosmetic use.
Valenta
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Institute of Pharmaceutical Technology, University of Vienna, Althanstrasse 14, A-1090, Vienna, Austria. claudia.valenta@univie.ac.at
Nowack
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E
Bernkop-Schnürch
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A
D000279:Administration, Cutaneous; D000818:Animals; D001419:Bacteria / Q000254:growth & development; D015169:Colony Count, Microbial; D003840:Deoxycholic Acid / Q000737:chemistry* / Q000494:pharmacology; D004058:Diffusion; D004234:Diuretics, Osmotic / Q000737:chemistry; D004337:Drug Carriers; D004355:Drug Stability; D005782:Gels; D008353:Mannitol / Q000737:chemistry; D008567:Membranes, Artificial; D051381:Rats; D012212:Rheology; D012431:Rutin / Q000008:administration & dosage / Q000378:metabolism*; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects; D014783:Viscosity
D004234:Diuretics, Osmotic; D004337:Drug Carriers; D005782:Gels; D008567:Membranes, Artificial; D003840:Deoxycholic Acid; D008353:Mannitol; D012431:Rutin