Alpha-Lipoic Acid and Cyanocobalamin Co-Loaded Nanoemulsions: Development, Characterization, and Evaluation of Stability

Çoban, Özlem Emir; Yıldırım, Sercan; Bakır, Tuğçe

doi:10.1007/s12247-020-09531-4

Cited by 10 publications

(8 citation statements)

References 48 publications

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“…The activity of the ALA molecule is limited by two critical factors: (i) The low stability to oxidation and heat (ii) and the low solubility [80].…”

Section: Pharmacokineticsmentioning

confidence: 99%

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

Pop

Crișan²,

Barca

et al. 2021

Processes

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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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“…The activity of the ALA molecule is limited by two critical factors: (i) The low stability to oxidation and heat (ii) and the low solubility [80].…”

Section: Pharmacokineticsmentioning

confidence: 99%

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

Pop

Crișan²,

Barca

et al. 2021

Processes

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“…The preparation of emulsions includes the low-energy method [ 12 , 24 ], solvent evaporation method [ 25 ], ultrasonic method [ 26 ], electrostatic complexation [ 27 ], high pressure homogenization method [ 28 , 29 ] and others. The emulsions in this study were prepared by a low-energy method.…”

Section: Methodsmentioning

confidence: 99%

Enhancing the stability of lutein emulsions with a water-soluble antioxidant and a oil-soluble antioxidant

Wang¹,

Zhang²,

Yan³

et al. 2023

Heliyon

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“…To treat various neurological disorders, coencapsulation of alpha-lipoic acid (ALA) and cyanocobalamin in NE was performed by Coban et al Castor oil was found to be suitable for encapsulating both ingredients, and optimum NE in terms of globule size, PDI, and zeta potential were obtained by formulations made by magnetic stirring and fine-tuning of the agitation speed, temperature, and pH. NE was found to be suitable, in comparison to the solution form, for extending the stability of both encapsulated molecules along with a desirable release profile [250].…”

Section: Vitamin B 12mentioning

confidence: 99%

Lipid Nanoparticles: An Effective Tool to Improve the Bioavailability of Nutraceuticals

Ashfaq,

Rasul,

Asghar

et al. 2023

IJMS

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Nano-range bioactive colloidal carrier systems are envisaged to overcome the challenges associated with treatments of numerous diseases. Lipid nanoparticles (LNPs), one of the extensively investigated drug delivery systems, not only improve pharmacokinetic parameters, transportation, and chemical stability of encapsulated compounds but also provide efficient targeting and reduce the risk of toxicity. Over the last decades, nature-derived polyphenols, vitamins, antioxidants, dietary supplements, and herbs have received more attention due to their remarkable biological and pharmacological health and medical benefits. However, their poor aqueous solubility, compromised stability, insufficient absorption, and accelerated elimination impede research in the nutraceutical sector. Owing to the possibilities offered by various LNPs, their ability to accommodate both hydrophilic and hydrophobic molecules and the availability of various preparation methods suitable for sensitive molecules, loading natural fragile molecules into LNPs offers a promising solution. The primary objective of this work is to explore the synergy between nature and nanotechnology, encompassing a wide range of research aimed at encapsulating natural therapeutic molecules within LNPs.

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Alpha-Lipoic Acid and Cyanocobalamin Co-Loaded Nanoemulsions: Development, Characterization, and Evaluation of Stability

Cited by 10 publications

References 48 publications

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

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

Enhancing the stability of lutein emulsions with a water-soluble antioxidant and a oil-soluble antioxidant

Lipid Nanoparticles: An Effective Tool to Improve the Bioavailability of Nutraceuticals

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