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Insights on the Use of α-Lipoic Acid for Therapeutic Purposes

Insights on the Use of α-Lipoic Acid for Therapeutic Purposes

Bahare Salehi, Yakup Berkay Yılmaz, Gizem Antika, Tugba Boyunegmez Tumer, Mohamad Fawzi Mahomoodally, Devina Lobine, Muhammad Akram, Muhammad Riaz, Esra Capanoglu, Farukh Sharopov, Natália Martins, William C Cho, etc.

Biomolecules. 2019 Aug 9;9(8):356.

PMID: 31405030

Abstract:

α-lipoic acid (ALA, thioctic acid) is an organosulfur component produced from plants, animals, and humans. It has various properties, among them great antioxidant potential and is widely used as a racemic drug for diabetic polyneuropathy-associated pain and paresthesia. Naturally, ALA is located in mitochondria, where it is used as a cofactor for pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase complexes. Despite its various potentials, ALA therapeutic efficacy is relatively low due to its pharmacokinetic profile. Data suggests that ALA has a short half-life and bioavailability (about 30%) triggered by its hepatic degradation, reduced solubility as well as instability in the stomach. However, the use of various innovative formulations has greatly improved ALA bioavailability. The R enantiomer of ALA shows better pharmacokinetic parameters, including increased bioavailability as compared to its S enantiomer. Indeed, the use of amphiphilic matrices has capability to improve ALA bioavailability and intestinal absorption. Also, ALA's liquid formulations are associated with greater plasma concentration and bioavailability as compared to its solidified dosage form. Thus, improved formulations can increase both ALA absorption and bioavailability, leading to a raise in therapeutic efficacy. Interestingly, ALA bioavailability will be dependent on age, while no difference has been found for gender. The present review aims to provide an updated on studies from preclinical to clinical trials assessing ALA's usages in diabetic patients with neuropathy, obesity, central nervous system-related diseases and abnormalities in pregnancy.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1200222	(R)-(+)-α-Lipoic acid		1200-22-2	Price

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