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- Title
Solubilization and stabilization of lipoic acid trisulfide by creation of various β-cyclodextrin clathrates.
- Authors
Tomonaga, Shoichiro; Ishimaru, Hiroaki; Isobe, Takahiro; Ohshima, Etsuo; Kitagaki, Shinji
- 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 β - cyclodextrin clathrates (84%-95% yield). Differential scanning calorimetry confirmed the inclusion of lipoic acid trisulfide in β-cyclodextrins. The resulting β-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 β-cyclodextrin clathrates as active ingredients, paving the way for clinical development.
- Subjects
LIPOIC acid; CYCLODEXTRINS; CYCLODEXTRIN derivatives; SOLUBILIZATION; DIFFERENTIAL scanning calorimetry; THERMAL stability
- Publication
Bioscience, Biotechnology & Biochemistry, 2024, Vol 88, Issue 6, p601
- ISSN
0916-8451
- Publication type
Article
- DOI
10.1093/bbb/zbae042