The main aim of the study was designed to develop bioadhesive buccal patches of carvedilol (CR) and evaluate for isoprenaline-induced tachycardia. Buccal patches of carvedilol were prepared by using chitosan (CH), sodium salt of carboxy methyl cellulose (NaCMC), and polyvinyl alcohol (PVA) as mucoadhesive polymers. The solvent evaporation method was used for the preparation of buccal patches. The patches were evaluated for their physical characteristics like patch thickness, weight variation, content uniformity, folding endurance, surface pH, residence time, in vitro drug release, and in vivo pharmacodynamic study. The swelling index of the patches was found to be proportional to the polymer concentration, whereas surface pH of all the formulated bioadhesive patches was found to lie between neutral ranges. In-vitro release study shows that 94.75% drug was release in 8 hours from the patch, which containing 2% w/v chitosan. The folding endurance result shows good elasticity in all the patches. Application of buccal patches on buccal mucosa of rabbit shows a significant result in % inhibition of isoprenaline-induced tachycardia. Prepared buccal patches of chitosan, NaCMC, and PVA containing Carvedilol meet the ideal requirement for the delivery of cardiovascular drugs and inhibit the isoprenaline tachycardia.
Paraquat (PQ), a highly popular agricultural herbicide, is a serious occupational hazard with lethality reported at doses as low as 35 mg/kg body weight with intoxication occurring via inhalation or dermal route. The main objective of this study was to determine the median lethal concentration (LCt) of paraquat through whole body exposure in adult male Wistar rats. Aerosolized PQ dissolved in water was delivered in a dose-dependent manner, to fully conscious rats confined in whole body plethysmograph (WBP), in a nebulized form with concentrations ranging from 40-200 mg/kg of air over a 4 h exposure period. Animals were observed up to 24-48 h post-exposure to observe any lethality. LCt estimates (±95% confidence interval) were obtained from the sequential stage-wise experiments using probit analysis. Rat lungs were examined radiologically and histopathologically. Gas chromatography-mass spectrometry (GC-MS) analysis determined the correlation of PQ accumulation in the lungs with the actual exposed dose of PQ. The actual LCt was found to be 218 g·min/m whereas 57.9 ± 2.90 µg/g of PQ accumulated in the lungs of each lifeless animal. All animals exhibited severe respiratory changes and pulmonary abnormalities. This study demonstrated that when compared with the actually exposed dose, the amount of PQ that accumulated in the lungs was very low, but enough to cause death in 50% of animal population and cause pulmonary abnormalities in each of the experimental animal. The PQ exposure carried out in WBP also facilitated the dermal absorption of aerosolized PQ, which replicated the real-life situation in workers operating with PQ.
In recent years the treatment of infectious diseases and immunisation has undergone a revolutionary shift. Not only a large number of disease-specific biological have been developed, but also contortion has been made to deliver these biological effectively. Conventional dosage forms are unable to deliver the drug in accordance with a predetermined rate and release therapeutically effective amount of drug at the site of action. The vesicular systems of niosomes, having bilayer structure assembled by nonionic surfactants are able to enhance the bioavailability of a drug to a predetermined area for a particular time period. In recent years various comprehensive researchs carried over niosome as a drug carrier and proved to be a promising drug carrier, which has potential to reduce the side effects of drugs and increased therapeutic effectiveness in various diseases. This narrative review describes fundamental aspects of niosomes, formulation methods, methods of characterization, recent advances in niosomal drug delivery.
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