Alpha-lipoic acid in the treatment of psychiatric and neurological disorders: a systematic review

Sousa, Caren Nádia Soares de; Leite, Cláudio Manuel Gonçalves da Silva; Medeiros, Ingridy da Silva; Vasconcelos, Luna Costa; Cabral, Lucas Manoel da Silva; Patrocínio, Cláudio Felipe Vasconcelos; Patrocínio, Marianna Letícia Vasconcelos; Mouaffak, Fayçal; Kébir, Oussama; Macedo, Danielle; Patrocínio, Manoel Cláudio Azevedo; Vasconcelos, Silvânia Maria Mendes

doi:10.1007/s11011-018-0344-x

Cited by 32 publications

(18 citation statements)

References 57 publications

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“…It has been demonstrated that ALA is effective in relieving some symptoms related to certain diseases, such as diabetes, age-related cardiovascular and neuromuscular defects, antipsychotic drugs-related weight gain and metabolic obesity [29,89,101,102]. Its potential effects on different types of diseases have drawn attention, since the results from studies were promising, namely in the field of neurodegenerative conditions [103]. In addition, the number of clinical trials increased to deepen knowledge on other ALA therapeutic properties and found hopeful effects.…”

Section: α-Lipoic Acid In Clinical Trialsmentioning

confidence: 99%

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

et al. 2019

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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.

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Section: α-Lipoic Acid In Clinical Trialsmentioning

confidence: 99%

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

et al. 2019

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“…LA supplementation significantly reduces TBARS, AOPP, improves TAS levels in healthy subjects, but it showed significant differences in bipolar or schizophrenic patients group [42][43][44] a need for well-designed clinical trials to enhance the clinical evidence of ALA effects [45].…”

Section: Ala In Neurological and Psychiatric Conditionsmentioning

confidence: 99%

Evaluation of Dissolution Profiles of a Newly Developed Solid Oral Immediate-Release Formula Containing Alpha-Lipoic Acid

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et al. 2021

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Alpha-lipoic acid (ALA, thioctic acid), a naturally-occurring essential dithiol compound, has become a common ingredient in many pharmaceutical and food supplement products (FSP), used in oxidative stress-dependent pathologies; oral bioavailability of ALA is limited by pharmacokinetic particularities that reduce its therapeutic efficacy-reduced solubility, lack of gastric stability and hepatic degradation, doubled by formulation hinders. The objectives were to develop a solid oral 600 mg ALA FSP to obtain an optimal pharmaceutical profile compared to a reference listed drug (RLD) with a similarity factor f2 50. A comparative dissolution study was performed; an HPLC method was used for ALA quantification. After planning combinatory simulations (formulation stage), two prototype formulas (#1 and #2) were manufactured and further optimized by adjusting ALA physical characteristics and the excipients quantities (#3 and #4) in order to achieve the Quality Target Product Profile. A misshapen of ALA’s in vitro release was observed for #3 Formula (f2 = 31.6); the optimal profile was obtained for Formula #4 (f2 = 58.5). A simple quantitative formula is not enough to assure good ALA bioavailability; the formulation needs multiple compounding modulations under physicochemical compatibility algorithms, with multiple dissolution profiles testing back-ups. It is essential to ensure a formulation with an in vitro dissolution comparable with the RLD, allowing the compound to reach its target level to assure the optimum claimed antioxidant activity of ALA at the cellular level, even for food supplement formulations.

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“…In a systemic review concerning the use of α-lipoic acid for the treatment of psychiatric and neurological conditions, it revealed that α-lipoic acid improves schizophrenia symptoms with fewer side effects from antipsychotic medication. It also showed the effectiveness in the prevention of Alzheimer’s disease progression and the ability to improve clinical parameters and oxidative imbalance in stroke patients [ 153 ]. In a clinical trial, α-lipoic acid was found to stimulate cAMP production in healthy control and patients of multiple sclerosis [ 154 ].…”

Section: The Potentials Of Antioxidants In Status Epilepticusmentioning

confidence: 99%

Seizure-Induced Oxidative Stress in Status Epilepticus: Is Antioxidant Beneficial?

et al. 2020

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Epilepsy is a common neurological disorder which affects patients physically and mentally and causes a real burden for the patient, family and society both medically and economically. Currently, more than one-third of epilepsy patients are still under unsatisfied control, even with new anticonvulsants. Other measures may be added to those with drug-resistant epilepsy. Excessive neuronal synchronization is the hallmark of epileptic activity and prolonged epileptic discharges such as in status epilepticus can lead to various cellular events and result in neuronal damage or death. Unbalanced oxidative status is one of the early cellular events and a critical factor to determine the fate of neurons in epilepsy. To counteract excessive oxidative damage through exogenous antioxidant supplements or induction of endogenous antioxidative capability may be a reasonable approach for current anticonvulsant therapy. In this article, we will introduce the critical roles of oxidative stress and further discuss the potential use of antioxidants in this devastating disease.

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Alpha-lipoic acid in the treatment of psychiatric and neurological disorders: a systematic review

Cited by 32 publications

References 57 publications

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

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

Evaluation of Dissolution Profiles of a Newly Developed Solid Oral Immediate-Release Formula Containing Alpha-Lipoic Acid

Seizure-Induced Oxidative Stress in Status Epilepticus: Is Antioxidant Beneficial?

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