In vitro and in vivo evaluation of organic solvent-free injectable melatonin nanoformulations

Molska, Alicja; Nyman, Axel Karl Gottfrid; Sofias, Alexandros Marios; Kristiansen, Kåre Andre; Hak, Sjoerd; Widerøe, Marius

doi:10.1016/j.ejpb.2020.05.003

Cited by 19 publications

(10 citation statements)

References 30 publications

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“…Because of its well-recognized low bioavailability, scientific innovations are underway to develop formulations that bypass the gastrointestinal tract, have a longer half-life, and/or leverage nanotechnology [ 261 , 298 , 299 ]. Overall, more research is needed to better understand the bioavailability of various formats and sources of melatonin, as well as innovative developments to optimize its physiological effects [ 200 ].…”

Section: Therapeutic Considerationsmentioning

confidence: 99%

Is Melatonin the “Next Vitamin D”?: A Review of Emerging Science, Clinical Uses, Safety, and Dietary Supplements

Minich

Henning²,

Darley

et al. 2022

Nutrients

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Melatonin has become a popular dietary supplement, most known as a chronobiotic, and for establishing healthy sleep. Research over the last decade into cancer, Alzheimer’s disease, multiple sclerosis, fertility, PCOS, and many other conditions, combined with the COVID-19 pandemic, has led to greater awareness of melatonin because of its ability to act as a potent antioxidant, immune-active agent, and mitochondrial regulator. There are distinct similarities between melatonin and vitamin D in the depth and breadth of their impact on health. Both act as hormones, affect multiple systems through their immune-modulating, anti-inflammatory functions, are found in the skin, and are responsive to sunlight and darkness. In fact, there may be similarities between the widespread concern about vitamin D deficiency as a “sunlight deficiency” and reduced melatonin secretion as a result of “darkness deficiency” from overexposure to artificial blue light. The trend toward greater use of melatonin supplements has resulted in concern about its safety, especially higher doses, long-term use, and application in certain populations (e.g., children). This review aims to evaluate the recent data on melatonin’s mechanisms, its clinical uses beyond sleep, safety concerns, and a thorough summary of therapeutic considerations concerning dietary supplementation, including the different formats available (animal, synthetic, and phytomelatonin), dosing, timing, contraindications, and nutrient combinations.

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Section: Therapeutic Considerationsmentioning

confidence: 99%

Is Melatonin the “Next Vitamin D”?: A Review of Emerging Science, Clinical Uses, Safety, and Dietary Supplements

Minich

Henning²,

Darley

et al. 2022

Nutrients

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show abstract

“…In dogs, after oral administration of melatonin at a dose of 1 mg/kg, the bioavailability was reduced to 17%, indicating a dose-dependent bioavailability [ 155 ]. Due to low bioavailability, research is being conducted to develop preparations bypassing the gastrointestinal tract, with a longer half-life or developed with the use of nanotechnology [ 18 , 156 , 157 , 158 ]. In addition, demonstrating whether plant-derived phytomelatonin is more easily digestible than the synthetic form [ 18 ].…”

Section: Melatonin Bioavailabilitymentioning

confidence: 99%

Melatonin: A Potential Candidate for the Treatment of Experimental and Clinical Perinatal Asphyxia

et al. 2023

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Perinatal asphyxia is considered to be one of the major causes of brain neurodegeneration in full-term newborns. The worst consequence of perinatal asphyxia is neurodegenerative brain damage, also known as hypoxic-ischemic encephalopathy. Hypoxic-ischemic encephalopathy is the leading cause of mortality in term newborns. To date, due to the complex mechanisms of brain damage, no effective or causal treatment has been developed that would ensure complete neuroprotection. Although hypothermia is the standard of care for hypoxic-ischemic encephalopathy, it does not affect all changes associated with encephalopathy. Therefore, there is a need to develop effective treatment strategies, namely research into new agents and therapies. In recent years, it has been pointed out that natural compounds with neuroprotective properties, such as melatonin, can be used in the treatment of hypoxic-ischemic encephalopathy. This natural substance with anti-inflammatory, antioxidant, anti-apoptotic and neurofunctional properties has been shown to have pleiotropic prophylactic or therapeutic effects, mainly against experimental brain neurodegeneration in hypoxic-ischemic neonates. Melatonin is a natural neuroprotective hormone, which makes it promising for the treatment of neurodegeneration after asphyxia. It is supposed that melatonin alone or in combination with hypothermia may improve neurological outcomes in infants with hypoxic-ischemic encephalopathy. Melatonin has been shown to be effective in the last 20 years of research, mainly in animals with perinatal asphyxia but, so far, no clinical trials have been performed on a sufficient number of newborns. In this review, we summarize the advantages and limitations of melatonin research in the treatment of experimental and clinical perinatal asphyxia.

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“…A wide range of potential applications of liposomes is mainly attributed to its ability to incorporate hydrophilic substances in the aqueous compartment, hydrophobic within the lipidic membrane, and amphiphilic molecules in the lipid aqueous interface [40]. Liposomes have been the most popular NCs since they were discovered, and various liposomal formulations are clinically approved [41,42]. A number of techniques have been reported for liposomal preparation, including ethanol injection, reversed-phase evaporation, detergent dialysis, and high-pressure homogenization [43].…”

Section: Liposomes Nps As Carriers Of Melatoninmentioning

confidence: 99%

“…Interestingly, ethanolic liposomes (ethosomes) loaded with melatonin and stored for 120 days showed only 7.6% increase in size, suggesting a stabilizing effect of ethanol in the formulation by providing a net negative charge on the surface and avoiding aggregation [48]. Curiously, an in vitro dialysis set-up of melatonin into liposomes had a desirable and slower release profile compared to free-melatonin dissolved in 10% ethanol [41]. This is probably due to the fact that melatonin diffusion from lipid bilayers is hindered by the aqueous medium, acting as a barrier to the melatonin transport.…”

Section: Liposomes Nps As Carriers Of Melatoninmentioning

confidence: 99%

Melatonin-Loaded Nanocarriers: New Horizons for Therapeutic Applications

et al. 2021

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The use of nanosized particles has emerged to facilitate selective applications in medicine. Drug-delivery systems represent novel opportunities to provide stricter, focused, and fine-tuned therapy, enhancing the therapeutic efficacy of chemical agents at the molecular level while reducing their toxic effects. Melatonin (N-acetyl-5-methoxytriptamine) is a small indoleamine secreted essentially by the pineal gland during darkness, but also produced by most cells in a non-circadian manner from which it is not released into the blood. Although the therapeutic promise of melatonin is indisputable, aspects regarding optimal dosage, biotransformation and metabolism, route and time of administration, and targeted therapy remain to be examined for proper treatment results. Recently, prolonged release of melatonin has shown greater efficacy and safety when combined with a nanostructured formulation. This review summarizes the role of melatonin incorporated into different nanocarriers (e.g., lipid-based vesicles, polymeric vesicles, non-ionic surfactant-based vesicles, charge carriers in graphene, electro spun nanofibers, silica-based carriers, metallic and non-metallic nanocomposites) as drug delivery system platforms or multilevel determinations in various in vivo and in vitro experimental conditions. Melatonin incorporated into nanosized materials exhibits superior effectiveness in multiple diseases and pathological processes than does free melatonin; thus, such information has functional significance for clinical intervention.

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In vitro and in vivo evaluation of organic solvent-free injectable melatonin nanoformulations

Cited by 19 publications

References 30 publications

Is Melatonin the “Next Vitamin D”?: A Review of Emerging Science, Clinical Uses, Safety, and Dietary Supplements

Is Melatonin the “Next Vitamin D”?: A Review of Emerging Science, Clinical Uses, Safety, and Dietary Supplements

Melatonin: A Potential Candidate for the Treatment of Experimental and Clinical Perinatal Asphyxia

Melatonin-Loaded Nanocarriers: New Horizons for Therapeutic Applications

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