Role of mucoadhesive polymers in enhancing delivery of nimodipine microemulsion to brain via intranasal route

Intranasal drug administration is receiving increased attention as a delivery method for bypassing the blood-brain barrier and rapidly targeting therapeutics to the CNS. However, rapid mucociliary clearance in the nasal cavity is a major hurdle. The purpose of this study was to evaluate the effect of mucoadhesive polymers in enhancing the delivery of nimodipine microemulsion to the brain via the intranasal route. The optimized mucoadhesive microemulsion was characterized, and the in vitro drug release and in vivo nasal absorption of drug from the new formulation were evaluated in rats. The optimized formulation consisted of Capmul MCM as oil, Labrasol as surfactant, and Transcutol P as co-surfactant, with a particle size of 250 nm and zeta potential value of -15 mV. In vitro and ex vivo permeation studies showed an initial burst of drug release at 30 min and sustained release up to 6 h, attributable to the presence of free drug entrapped in the mucoadhesive layer. In vivo pharmacokinetic studies in rats showed that the use of the mucoadhesive microemulsion enhanced brain and plasma concentrations of nimodipine. These results suggest that incorporation of a mucoadhesive agent in a microemulsion intranasal delivery system can increase the retention time of the formulation and enhance brain delivery of drugs.

Reduction in aluminum induced oxidative stress by meloxicam in rat brain

Non-steroidal anti-inflammatory drugs [NSAID] have been associated with antioxidant property and have been shown to improve the circulating antioxidant status on daily dosing in different inflammatory conditions. The present study was conducted to investigate the antioxidant role of meloxicam in aluminum induced oxidative stress in rat brain. In the in vivo experiments, Sprague-Dawley rats where randomized into 4 groups receiving daily treatment for 4 weeks: 1] double distilled water i.p., 2] 4.2 mg/kg aluminum i.p. 3] meloxicam [5.0 mg/kg, i.m.] 4] 5.0 mg/kg, meloxicam i.m. + 4.2 mg/kg aluminum i.p. brain homogenates from the above animals were assayed for lipid peroxidation levels as well as superoxide dismutase activity. In the in vitro experiments, brain homogenates from Sprague-Dawley rats were treated with either, aluminum, meloxicam or their combinations and were then assayed as per the in vivo samples. In vivo data showed elevated lipid peroxidation levels in brain homogenate in aluminium-treated group as compared to aluminium + meloxicam treatment which showed a significant decrease in the malonaldehyde levels. Similar results were observed in the in vitro experiments when brain homogenates were treated with either, aluminum, meloxicam or their combinations. Furthermore, no change was observed in superoxide dismutase activity in any treatment group as compared to the control in either experiment. These results indicate that NSAID can be used in Alzheimer management

Sperm membrane modulation by Sapindus mukorossi during sperm maturation / 亚洲男科学杂志(英文版)

<p><b>AIM</b>To observe the alterations in the biochemical and biophysical changes in the sperm membrane during sperm maturation in male rats treated with the water extract of the fruit pericarp of S. mukorossi.</p><p><b>METHODS</b>Adult male Sprague-Dawley rats were gavaged the aqueous extract of the fruit pericarp of S. mukorossi at a dose of 50 mg/kg/d for 45 days. On day 46, the sperm parameters were observed in different sections of the epididymis and the sperm superoxide dismutase and the lipid peroxidation was determined and compared with the controls. The testis and epididymis were routinely prepared for histological examination under the light microscope.</p><p><b>RESULTS</b>No significant differences in the sperm number and morphology were observed between the control and treated groups. However, a significant inhibition (P<0.05-0.01) of sperm motility in the caput, corpus and cauda regions of the epididymis was seen in the treated group. No significant histopathological changes were found in the testis and epididymis. The important finding was that in the treated animals, the spermatozoa showed an abnormal distribution of the superoxide dismutase activity, being minimum in the caput and maximum in the corpus, which was just opposite to that of the controls.</p><p><b>CONCLUSION</b>The study provides a unique observation where the plant extract alters the sperm membrane physiology without change the testicular and epididymal morphology.</p>