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Influence of 6-Ketocholestanol on Skin Permeation of 5-Aminolevulinic Acid and Evaluation of Chemical Stability
- Source :
- Journal of Pharmaceutical Sciences. 93:2780-2787
- Publication Year :
- 2004
- Publisher :
- Elsevier BV, 2004.
-
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 stability over the whole observation period of 42 days.
- Subjects :
- 6-ketocholestanol
Liposome
Chromatography
Swine
Chemistry
Stereochemistry
Skin Absorption
Diffusion
Drug Evaluation, Preclinical
Phospholipid
Pharmaceutical Science
Aminolevulinic Acid
In Vitro Techniques
Permeation
Prodrug
Chemical reaction
chemistry.chemical_compound
Drug Stability
Animals
Chemical stability
Ketocholesterols
Subjects
Details
- ISSN :
- 00223549
- Volume :
- 93
- Database :
- OpenAIRE
- Journal :
- Journal of Pharmaceutical Sciences
- Accession number :
- edsair.doi.dedup.....2cd09b5db18c09522fa43d83c641cf38