Ex-vivo absorption study of lysine R-lipoate salt, a new pharmaceutical form of R-ALA
| Autor: | Michela Buccioni, Rosaria Volpini, Michael Alliance Ngouadjeu Ngnintedem, Andrea Spinaci, Gabriella Marucci, Diego Dal Ben, Massimo Ricciutelli, Catia Lambertucci, Aleix Martí Navia, Francesco Amenta |
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| Rok vydání: | 2018 |
| Předmět: |
Male
0301 basic medicine chemistry.chemical_classification Aqueous solution Thioctic Acid Lysine Pharmaceutical Science Salt (chemistry) Biological activity Absorption (skin) In Vitro Techniques Permeability Intestinal absorption 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology Intestinal Absorption Biotin chemistry Biochemistry Oral administration Animals Rats Wistar |
| Zdroj: | European Journal of Pharmaceutical Sciences. 118:200-207 |
| ISSN: | 0928-0987 |
| Popis: | Alpha-lipoic acid (ALA) oral supplements were used in many pathologies associated with increased oxidative stress. Although only R-ALA is considered the biologically active form, R,S-ALA is used in therapeutic applications even showing poor water solubility. The aim of this work was to study the absorption and transport mechanism across the intestinal barrier of new R-ALA stable and water soluble form, consisting in the lysine R-ALA salt, in presence and absence of specific inhibitors of Na+/multivitamin (SMVT) and monocarboxylic acids (MCT). The absorption of a new ALA form was investigated at rat everted sacs in comparison with R-ALA, S-ALA, and R,S-ALA. Results showed that duodenum is the best portion of intestine for ALA forms absorption. The absorption percentage of R-ALA, S-ALA, R,S-ALA, and lysine R-ALA salt was 66%, 43%, 55%, and 70%, respectively. The modest effect of the SMVT inhibitor biotin demonstrated that this transporter system is not principally involved in the absorption of lysine R-lipoate salt across the rat intestinal barrier. On the contrary, the MCT inhibitor octanoic acid significantly reduced the transport of this salt, whit an absorption decrease of R-ALA and lysine R-lipoate salt of 28% and 24%, respectively. Since the highest concentration of these inhibitors did not completely inhibit the absorption of lysine R-lipoate salt, other transport mechanisms probably operate for its intracellular delivery. The new form of ALA, lysine R-lipoate salt, was the most absorbed respect to the other ALA forms demonstrating that this compound is more suitable for oral administration. This new salt could represent a promising candidate for ALA oral supplementation. |
| Databáze: | OpenAIRE |
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