Eur J Pharm Biopharm: Improving the negative effects of the new Amodafinil microneedle patch on sleep deprivation

Sleep deprivation refers to shortened sleep time and reduced sleep quality due to environmental changes or other force majeure factors, and the inability to meet normal physiological needs in an active or passive state

Sleep deprivation Sleep deprivation leads to fatigue, mood disorders, memory loss, and even cognitive disorders lead to fatigue, mood disorders, memory loss, and even cognitive disorders

Armodafinil, as an oral preparation, is clinically mainly used to treat narcolepsy, patients with depression, idiopathic drowsiness or narcolepsy with excessive daytime sleepiness, and the dosage is often larger

Armodafinil armodafinil dose often large dose often large is not convenient to swallow, nor convenient time to stop the administration is not convenient to swallow, nor facilitate the timely administration stopped

Transdermal administration typically having ease of administration, dosage adjustable, high compliance , etc.

Transdermal administration transdermally ease of administration, dosage adjustable, high compliance for ease of administration, dosage adjustable, high compliance biocompatibility, biodegradability, and excellent release profile can be adjusted dosing capacity biological Compatibility, biodegradability, adjustable release profile and excellent drug delivery ability

Microneedles can create transient microchannels in the skin, promote the effective penetration of polypeptides, antibodies, oligonucleotides and nanoparticles, and may break the barriers to the penetration of high-molecular-weight drugs

A study published in Eur J Pharm Biopharm recently used polyvinylpyrrolidone (PVP) K90 to be dissolved in methanol and dried, and then molded to prepare Armodafinil- loaded microneedles with high mechanical strength and large drug loading.

Armodafinil microneedlesAmodafinil microneedles Higher mechanical strength Higher mechanical strength

The drug release rate of microneedle armodafinil was determined by high performance liquid chromatography, and the results indicated that the drug would be released quickly within 1.

Fast release drugs fast release drugs

Behavioral experiments (water maze experiment, elevated + maze test) showed that there were significant differences in the trajectories of the model group and the healthy group, suggesting that sleep deprivation may reduce the spatial memory ability of mice

Behavioral Experiments Behavioral Experiments

Pharmacokinetic analysis (LC-MS/MS measurement) showed that after the administration of the microneedle patch, the content of armodafinil in the blood of mice increased significantly, and its concentration was equivalent to that of oral armodafinil

Pharmacokinetic analysis Pharmacokinetic analysis

Histopathological observations indicated that nuclear atrophy and hyperchromatism were seen in the model group, suggesting that sleep deprivation mice had brain cell necrosis and severe neuronal damage, suggesting that sleep deprivation may lead to hippocampal CA1 lesions, which were significantly improved after oral administration and microneedle administration

Histopathological observation Histopathological observation

The results of corticosterone measurement showed that after 72 hours of sleep deprivation, compared with the healthy group, the serum corticosterone level of mice in the model group was significantly increased

Corticosterone determination

The detection of brain-derived neurotrophic factor BDNF showed that after 72 hours of sleep deprivation, the expression of BDNF in the hippocampus of mice decreased significantly.

Brain-derived neurotrophic factor BDNF detection Brain-derived neurotrophic factor BDNF detection

Studies have shown that Armodafinil microneedles can significantly improve the cognitive level of sleep deprived rats, thereby reducing various adverse effects of sleep deprivation on mice

Amodafinil microneedle can significantly improve the cognitive level of sleep-deficient rats, thereby reducing the various adverse effects of sleep deprivation on mice.

Literature source:

Zhu, L.

Zhu, L.
, Zhang, S.
, Yu, X.
, Zhu, S.
, Ou, G.
, Li, Q.
, Zhang, Y.
, Wang, L.
, Zhuang, X.
, Du, L.
, & Jin, Y.
(2021).
Application of armodafinil-loaded microneedle patches against the negative influence induced by sleep deprivation.
European journal of pharmaceutics and biopharmaceutics: official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik eV, S0939-6411(21)00264-2 .
Advance online publication.
https://doi.
org/10.
1016/j.
ejpb.
2021.
10.
009

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