Solubilization and stabilization of lipoic acid trisulfide by creation of various ß-cyclodextrin clathrates.
Biosci Biotechnol Biochem
; 88(6): 601-607, 2024 May 22.
Article
em En
| MEDLINE
| ID: mdl-38569654
ABSTRACT
Lipoic acid trisulfide, a sulfane sulfur-containing trisulfide of α-lipoic acid, holds promise in pharmaceuticals, yet knowledge gaps persist regarding its synthesis, properties, and stability. Here, we synthesized the lipoic acid trisulfide with a purity exceeding 99% from α-lipoic acid on a gram scale and obtained novel ß-cyclodextrin clathrates (84%-95% yield). Differential scanning calorimetry confirmed the inclusion of lipoic acid trisulfide in ß-cyclodextrins. The resulting ß-cyclodextrin clathrates exhibited significant improvements in water solubility and thermal stability. This pioneering study demonstrated a novel approach to the practical preparation of trisulfide and its ß-cyclodextrin clathrates as active ingredients, paving the way for clinical development.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Solubilidade
/
Ácido Tióctico
/
Beta-Ciclodextrinas
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article