Transdermal permeation of selegiline from hydrogel-membrane drug delivery systems

Fang, Jia‐You; Hung, Chi‐Feng; Chi, Chen-Hsien; Chen, Chih-Chieh

doi:10.1016/j.ijpharm.2009.06.025

Cited by 19 publications

(6 citation statements)

References 30 publications

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“…Se-L-M may favor this interaction compared to the D form. According to previous studies involving the skin delivery of enantiomers [38][39][40] , the L form (or S form) of ketorolac, ketoprofen, and selegiline also exhibited greater skin absorption than the D form (or R form).…”

Section: Discussionmentioning

confidence: 92%

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

Lin

Fang²,

Al‐Suwayeh

et al. 2011

Acta Pharmacol Sin

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Aim: To investigate the in vitro and in vivo percutaneous absorption of seleno-L-methionine (Se-L-M), an ultraviolet (UV)-protecting agent, from aqueous solutions. Methods: Aqueous solutions of Se-L-M were prepared in pH 4, 8, and 10.8 buffers. The pH 8 buffer contained 30% glycerol, propylene glycol (PG) and polyethylene glycol (PEG) 400. The in vitro skin permeation of Se-L-M via porcine skin and nude mouse skin was measured and compared using Franz diffusion cells. The in vivo skin tolerance study was performed, which examined transepidermal water loss (TEWL), skin pH and erythema. Results: In the excised porcine skin, the flux was 0.1, 11.4 and 8.2 μg· cm -2 ·h -1 for the pH 4, 8, and 10.8 buffers, respectively. A linear correlation between the flux and skin deposition was determined. According to permeation across skin with different treatments (stripping, delipidation, and ethanol treatments), it was determined that the intracellular route comprised the predominant pathway for Se-L-M permeation from pH 8 buffer. Aqueous solutions of seleno-DL-methionine (Se-DL-M), selenium sulfide and selenium-containing quantum dot nanoparticles were also used as donor systems. The DL form showed a lower flux (7.0 vs 11.4 μg· cm -2 ·h -1 ) and skin uptake (23.4 vs 47.3 μg/g) as compared to the L form, indicating stereoselective permeation of this compound. There was no or only negligible permeation of selenium sulfide and quantum dots into and across the skin. With in vivo topical application for 4 and 8 h, the skin deposition of Se-L-M was about 7 μg/g, and values were comparable to each other. The topical application of Se-L-M for up to 5 d did not caused apparent skin irritation. However, slight inflammation of the dermis was noted according to the histopathological examination. Conclusion: Se-L-M was readily absorbed by the skin in both the in vitro and in vivo experiments. The established profiles of Se-L-M skin absorption will be helpful in developing topical products of this compound.Keywords: seleno-L-methionine; selenium; percutaneous absorption; topical delivery; skin [5] . In humans, a low selenium status is associated with up to a 4-fold increased risk of developing skin cancer [6] . Topical selenium compounds also increase the minimum dose of UV radiation required to cause skin reddening and protect against skin damage caused by UVB [7,8] . Seleno-L-methionine (Se-L-M), the major component of dietary selenium, represents an organic form of selenium which may provide enhanced protection of the skin [9] . Se-L-M also decreases the oxidative stress of neurodegenerative diseases, rheumatoid arthritis, and HIV/AIDS [10,11] . Most ingested selenium, whether in organic or inorganic form, is converted by liver metabolism [3] . In addition, selenium toxicity can produce gastrointestinal problems [12] . Delivery of pharmacologically active compounds via the skin is an attractive alternative to oral dosing for numerous reasons including stable plasma concentrations, bypass of firstpass effects, and reduction of some si...

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Section: Discussionmentioning

confidence: 92%

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

Lin

Fang²,

Al‐Suwayeh

et al. 2011

Acta Pharmacol Sin

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“…Selegiline, a Monoamine oxidase B (MAO-B) inhibitor with neuroprotective and antioxidant effects, is utilized for the oral therapy of Parkinson’s disease, Alzheimer’s disease, depression, narcolepsy and cocaine addiction [64]. Recently, some neurologists have proposed selegiline monotherapy for patients that are in the early stage of Parkinson’s disease [64]. This allowed to delay the treatment with l -dopa, thus avoiding l -dopa side-effects for a certain period.…”

Section: General Overview Of Nes For Nose-to-brain Deliverymentioning

confidence: 99%

Nanoemulsions for “Nose-to-Brain” Drug Delivery

et al. 2019

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The blood–brain barrier (BBB) plays a fundamental role in protecting the brain from toxic substances and therefore also controls and restricts the entry of therapeutic agents. The nasal administration of drugs using the nose-to-brain pathway allows direct drug targeting into the brain, avoiding the first-pass effect and bypassing the BBB. Through the nasal route, the drug can access the brain directly along the trigeminal and olfactory nerves, which are located in the upper part of the nasal cavity. Nanoemulsions are formulations belonging to the field of nanomedicine. They consist of emulsions (commonly oil in water) stabilized by one or more surfactants—and eventually co-surfactants—delivered in droplets of small dimensions (sizes of 100–300 nm or less) with a high surface area. A mucoadhesive polymer such as chitosan can be added to the formulation to impair rapid nasal clearance. Nanoemulsions represent promising formulations to deliver drugs directly into the brain through the intranasal route. Therefore, they can be used as a possible alternative to oral administration, avoiding problems such as low solubility in water, poor bioavailability, enzymatic degradation and slow onset of action. This review focuses the present situation in literature regarding the use of nanoemulsions for nose-to-brain targeting, with particular attention to recent publications. Nasal nanoemulsions appear to be effective, non-invasive and safe drug delivery systems to achieve brain targeting for the treatment of neurological diseases.

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“…Selegiline, an antioxidant and neuroprotective agent, is used for the oral therapeutics of PD, AD, depression, narcolepsy, and cocaine addiction. Of lately, it has been proposed as monotherapy for early stage PD [75] to hold back the treatment with levodopa to avoid its side effects for a substantial period. Other problems with the oral therapy of selegiline are poor drug bioavailability (<10%) due to its poor solubility in water and high presystemic metabolism.…”

Section: Ne For Parkinson's Diseasementioning

confidence: 99%

Intranasal Nanoemulsions for Direct Nose-to-Brain Delivery of Actives for CNS Disorders

et al. 2020

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The treatment of various central nervous system (CNS) diseases has been challenging, despite the rapid development of several novel treatment approaches. The blood–brain barrier (BBB) is one of the major issues in the treatment of CNS diseases, having major role in the protection of the brain but simultaneously constituting the main limiting hurdle for drugs targeting the brain. Nasal drug delivery has gained significant interest for brain targeting over the past decades, wherein the drug is directly delivered to the brain by the trigeminal and olfactory pathway. Various novel and promising formulation approaches have been explored for drug targeting to the brain by nasal administration. Nanoemulsions have the potential to avoid problems, including low solubility, poor bioavailability, slow onset of action, and enzymatic degradation. The present review highlights research scenarios of nanoemulsions for nose-to-brain delivery for the management of CNS ailments classified on the basis of brain disorders and further identifies the areas that remain unexplored. The significance of the total dose delivered to the target region, biodistribution studies, and long-term toxicity studies have been identified as the key areas of future research.

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Transdermal permeation of selegiline from hydrogel-membrane drug delivery systems

Cited by 19 publications

References 30 publications

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

Nanoemulsions for “Nose-to-Brain” Drug Delivery

Intranasal Nanoemulsions for Direct Nose-to-Brain Delivery of Actives for CNS Disorders

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