Influence of 6-ketocholestanol on skin permeation of 5-aminolevulinic acid and evaluation of chemical stability

Journal of Pharmaceutical Sciences
Barbara Gabriele AunerClaudia Valenta

Abstract

The ability of 6-ketocholestanol to increase the skin permeation of the prodrug aminolevulinic acid (5-ALA) was investigated. 6-Ketocholestanol was incorporated together with 5-ALA in four different formulations. Preparations used were a liquid solution/suspension of 5-ALA in buffer, 5-ALA in phospholipid liposomal formulations with and without gelating agent, and finally, a complex cream formulation also including phospholipids. Standard diffusion experiments of 5-ALA using Franz-type diffusion cells and porcine skin were performed. Drug stability was monitored by analyzing the 5-ALA content in the different formulations over time and viewing the preparation for microbial contamination. The analysis of 5-ALA as a nonfluorescent probe was performed after chemical reaction, leading to a fluorescent derivative. The 5-ALA permeation through porcine skin was increased threefold by 6-ketocholestanol in the cream formulation. The chemical stability of 5-ALA in the tested formulations was in the range of about 33 to 72% after an observation period of 28 days. After that time point microbial stability was no longer evident for formulations 2 and 3. Formulation 1 could be observed until day 34, and only formulation 4 showed a microbial ...Continue Reading

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Citations

Apr 9, 2005·International Journal of Pharmaceutics·Barbara G AunerJonathan Hadgraft
Mar 14, 2007·Journal of Photochemistry and Photobiology. B, Biology·Miron KaliszewskiJohan Moan
Oct 6, 2005·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Babette Biruss, Claudia Valenta
Nov 26, 2009·Pharmaceutical Development and Technology·Yousef JavadzadehAli Nokhodchi
Oct 18, 2018·Photochemical & Photobiological Sciences : Official Journal of the European Photochemistry Association and the European Society for Photobiology·Kunal M Tewari, Ian M Eggleston
Jul 20, 2010·The Journal of Pharmacy and Pharmacology·Desmond I J MorrowRyan F Donnelly

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