Abstract
Antidepressant and cognitive effects of piperine -encapsulated liposomes (PL) were investigated in male Wistar rats. Oral piperine (5 mg/kg body weight/day) and intranasal PL (7.2 µg/day) were randomly assigned to daily administer for 14 days to rats which were subjected to forced swimming, Mor-ris water maze and spontaneous motor behavior tests. PL significantly exhibited anti-depression like activity and cognitive enhancing effects, in comparison to the control groups after the first dose (p < 0.01) and the effects could be maintained throughout the period of study. Quantitative analysis of the brain homogenates by HPLC indicated that piperine, delivered either orally or nasally, distributed to the hippocampus at a higher extent than the cortex and that the time to peak concentration of nasal PL was shorter than for the oral piperine. Intranasal PL was, thus, potential in delivery of piperine, at a low dose, to exert its an-tidepressant and cognitive enhancing activities.
Highlights
Piperine, a major alkaloid of black pepper (Piper nigrum Linn.) and long pepper (Piper longum Linn.), has been used in folk medicine for the treatment of various diseases, including seizure disorders [1,2,3]
(a) Escape latency time (b) Retention time pylene glycol, PEG and water, or the blank liposomes, composed of egg L-α-phosphatidylcholine (EPC), chol, and the vehicle, used in this study were not significantly different from the results obtained from the relevant control groups (p > 0.05 all)
The intranasal dose was proposed by estimation from its oral dose and pharmacokinetic profile reported earlier [8], based on minimal or none first-pass metabolism involvement on nasal absorption
Summary
A major alkaloid of black pepper (Piper nigrum Linn.) and long pepper (Piper longum Linn.), has been used in folk medicine for the treatment of various diseases, including seizure disorders [1,2,3]. Pharmacological studies have shown that piperine possesses various activities including anti-inflammatory and analgesic [4], anticonvulsant [5], anti-ulcer [6], anti-depressant [1], cytoprotection, antioxidant [7] and cognitive enhancing effect [8]. It inhibits monoamine oxidase (MAO) activity [1,3,9] and increases the level of noradrenaline and serotonin in mouse brain [3], indicating its potential neurological benefits. Results from cell survival and the level of brain-derived neurotrophic factor in corticosterone-treated cultured hippocampal neurons confirm similar findings [11], yet the mechanism of actions of piperine on neuronal damage is still unknown
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