Alpha-lipoic acid in pharmaceutical development: a comprehensive review of its therapeutic potential and molecular mechanisms
DOI:
https://doi.org/10.56782/pps.456Keywords:
alpha-lipoic acid, therapeutic potential, pharmacological activities, pharmacokinetics, pharmaceutical developmentAbstract
Alpha-lipoic acid (ALA), also known as thioctic acid, is a lipid acid with strong biological activity synthesized from octanoic acid in prokaryotic and eukaryotic microorganisms, plants, and animals. It is gaining attention for its potential therapeutic benefits for a wide range of health problems. A comprehensive systematic literature review on ALA has been performed without temporal restrictions, utilizing the PubMed, Scopus, Embase, ScienceDirect, SciELO, and SciVerse databases. Different in vitro, in vivo, and clinical studies have demonstrated numerous potent pharmacological activities of ALA, including antioxidant, anti-inflammatory, antimicrobial, anti-Alzheimer’s, antiepileptic, antiparkinsonian, anxiolytic, effects on schizophrenia, neuroprotective, antidiabetic, antiallergic, anticancer, anti-osteoporosis, cardioprotective, hepatoprotective, anti-obesity, anti-aging, and effects on the reproductive system, etc. Although dietary supplements (tablets, capsules, etc.) containing ALA are available due to their various biological activities, there are no Food and Drug Administration (FDA) or European Medicines Agency (EMA)-approved over-the-counter (OTC) ALA drugs worldwide. Pharmacokinetically, ALA has an oral bioavailability of approximately 30% due to its brief blood half-life, significant presystemic clearance, and hepatic first-pass metabolism. However, the use of different innovative formulations has greatly enhanced ALA bioavailability. The data obtained show that ALA liquid formulations have higher plasma concentrations and therefore bioavailability compared to solid dosage forms. These innovative approaches hold promise for the development of improved ALA-based treatments across a broad spectrum of health conditions.
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