Formulation and Evaluation of Niosomes of Benzyl Penicillin.

Benzylpencillin niosomes were formulated using thin film hydration technique. The resultant niosomes were evaluated using surface morphology, particle size and its distribution, encapsulation efficiency, In vitro drug release, in vivo bioavailability and In vitro antimicrobial activity parameters. Both short (3 h) and long term (24 h) stability studies were carried out on the formulations. The lipid-surfactant ratio and the presence of cosurfactant were identified as the key variables that affect performance of the formulations. The niosomes particle sizes were between 1.67μm to 2.22 μm. The encapsulation efficiency was found to be highest in batch A with value of 82.42 %. Batches B and C exhibited slow release, oral stability and good bioavailability in vivo. For In vitro and in vivo studies, batch B containing span 80,Tween 65 and cholesterol was particularly stable and released its drug content in a controlled manner. The Cmax for the batches were higher than that of pure drug which has value of 55.04 mg/ml in vivo. The IZD of the batches were high against the test micro organisms and all the batches exhibited antimicrobial activities greater than the unformulated drug against S. typhi, P. vulgaris and Ps. Aereuginosa.

Pharmacological justification for the ethnomedical use of Clausena anisata root-bark extract in the management of epilepsy.

Various morphological parts of the tropical plant, Clausena anisata (Wild) Hook [family: Rutaceae], have ethnomedical claim for use in the management of epilepsy. This study examined the antiepileptic activity of Clausena anisata root bark, stem bark and leaf ethanolic extracts (i.e. CARE, CASE and CALE respectively) against pentylenetetrazole (PTZ) induced seizures in mice. Phytochemical and acute toxicity tests were performed on the extracts followed by oral administration of graded doses of CASE (500, 750 and 1000 mg/kg), CARE and CALE (400, 600 and 800 mg/kg) to the mice, thirty minutes before the administration of PTZ (90 mg/kg i.p.). The anticonvulsant effect of the extracts and diazepam (4 mg/kg) were compared. CALE was found to possess large amount of saponins, CARE large amounts of tannins and saponins, CASE large amounts of flavonoids, alkaloids and tannins. While CARE at the dose level of 800 mg/kg significantly (p<0.05) delayed the onset of convulsions and afforded 33.33 % protection, neither CALE nor CASE could exert any significant protective effect on PTZ induced convulsions, whereas diazepam totally abolished the episodes of convulsions. This study suggests that the ethanolic root bark extract of Clausena anisata contains bioactive constituents that may be beneficial in petit mal epilepsy and lend pharmacological credence to the ethnomedical claim for the use of the plant in the management of epilepsy. Abbreviations: NMDA= N-methyl-D-aspartate, SCMC= sodium carboxy methyl cellulose, CARE= Clausena anisata root bark ethanolic extract, CASE= Clausena anisata stem bark ethanolic extract, CALE= Clausena anisata leaf ethanolic extract, PTZ= pentylenetetrazole.