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

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Student Research Committee, School of Medicine, Bam University of Medical Sciences, Bam 44340847, Iran
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Graduate Program of Biomolecular Sciences, Institute of Natural and Applied Sciences, Canakkale Onsekiz Mart University, Canakkale 17020, Turkey
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Department of Molecular Biology and Genetics, Faculty of Arts and Science, Canakkale Onsekiz Mart University, Canakkale 17020, Turkey
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Department of Health Sciences; Faculty of Science, University of Mauritius, Réduit 80837, Mauritius
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Department of Eastern Medicine, Government College University Faisalabad; Faisalabad 38000, Pakistan
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Department of Allied Health Sciences, Sargodha Medical College, University of Sargodha, Sargodha 40100, Pakistan
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Faculty of Chemical & Metallurgical Engineering, Food Engineering Department, Istanbul Technical University, Maslak 34469, Turkey
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Department of Pharmaceutical Technology, Avicenna Tajik State Medical University, Rudaki 139, Dushanbe 734003, Tajikistan
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Faculty of Medicine, University of Porto, Alameda Prof. Hernâni Monteiro, 4200-319 Porto, Portugal
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Institute for Research and Innovation in Health (i3S), University of Porto, 4200-135 Porto, Portugal
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Department of Clinical Oncology, Queen Elizabeth Hospital, 30 Gascoigne Road, Hong Kong
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Zabol Medicinal Plants Research Center, Zabol University of Medical Sciences, Zabol 61615-585, Iran
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Authors to whom correspondence should be addressed.
Biomolecules 2019, 9(8), 356; https://doi.org/10.3390/biom9080356
Received: 27 June 2019 / Revised: 26 July 2019 / Accepted: 26 July 2019 / Published: 9 August 2019
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. View Full-Text
Keywords: α-lipoic acid; bioavailability; formulations; clinical trial; diabetic neuropathy; obesity; schizophrenia; sclerosis; pregnancy α-lipoic acid; bioavailability; formulations; clinical trial; diabetic neuropathy; obesity; schizophrenia; sclerosis; pregnancy
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Salehi, B.; Berkay Yılmaz, Y.; Antika, G.; Boyunegmez Tumer, T.; Fawzi Mahomoodally, M.; Lobine, D.; Akram, M.; Riaz, M.; Capanoglu, E.; Sharopov, F.; Martins, N.; Cho, W.C.; Sharifi-Rad, J. Insights on the Use of α-Lipoic Acid for Therapeutic Purposes. Biomolecules 2019, 9, 356.

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