Sorbitol based proniosomes to improve the permeability and stability of an oral cephlosporin

In the present study, dry free-flowing proniosomes containing Cefuroxime axetil has been prepared with sorbitol. Span 40, 60 and 80 have been used in different molar ratios with cholesterol and stearylamine. Proniosomes are characterized by SEM, flowability, entrapment efficiency, release study and ex-vivo permeation study. Stability study of proniosomes has been determined at room-temperature. The vesicle size is found to be less than 5µm. Decreased angle of repose indicates the coating of niosomes with sorbitol carrier. Entrapment efficiency of Span 60 is found to be maximum. Both proniosomes and niosomes indicate the similar controlled release profile. Permeation study of cefuroxime axetil, follows the order of Span 60 with bile salt > Span 60 only > Span 40. Upon ageing, proniosomes indicate no change in its physical property and the entrapment efficiency is found to be more than 90%, indicating no leakage or degradation of drug from proniosomes whereas niosomes indicate slight sedimentation and aggregation of particles. These factors indicate the commercial viability and easy scale up of proniosomes

Solid Dispersions: A tool for improving the Solubility and Dissolution of Metronidazole

Metronidazole is a broad spectrum antibiotic. It is sparingly soluble in water but has oral bioavailability of 93-95%. So solid dispersions (SDs) containing metronidazole was prepared in different ratios (1:1, 1:2 and 1:5) and using different carriers like dextrose, citric acid, polyethylene glycol (PEG-4000) and polyvinylpyrrolidone (PVP). Fusion or melting method was used for SD containing dextrose and citric acid and Solvent evaporation method was used for SD containing PVP and PEG-4000. The solubility studies revealed that solubility of metronidazole was enhanced to manifolds. Best result was exhibited when drug carrier ratio is in the order of 1:5>1:2>1:1. Among the different carriers, the solubility and dissolution was increased to maximum in case of PVP and PEG and almost 100 % drug released within 1 hour. The development of solid dispersions was further confirmed by DSC and XRD

Solid Dispersions: A tool for improving the Solubility and Dissolution of Metronidazole

Metronidazole is a broad spectrum antibiotic. It is sparingly soluble in water but has oral bioavailability of 93-95%. So solid dispersions (SDs) containing metronidazole was prepared in different ratios (1:1, 1:2 and 1:5) and using different carriers like dextrose, citric acid, polyethylene glycol (PEG-4000) and polyvinylpyrrolidone (PVP). Fusion or melting method was used for SD containing dextrose and citric acid and Solvent evaporation method was used for SD containing PVP and PEG-4000. The solubility studies revealed that solubility of metronidazole was enhanced to manifolds. Best result was exhibited when drug carrier ratio is in the order of 1:5>1:2>1:1. Among the different carriers, the solubility and dissolution was increased to maximum in case of PVP and PEG and almost 100 % drug released within 1 hour. The development of solid dispersions was further confirmed by DSC and XRD

Formulation of risperidone loaded proniosomes for effective transdermal delivery: An in-vitro and in-vivo study

In the present investigation, proniosomes of risperidone were formulated, optimized and evaluated for effective transdermal delivery in order to overcome the bioavailability issues of orally administered risperidone. The proniosomes were prepared using various sorbitan esters with cholesterol and soya lecithin and were evaluated for in-vitro parameters, ex-vivo permeation and in-vivo performance. Results indicated that the vesicles were spherical in shape, their size ranged from 284.00 nm to 941.40 nm and they had high zeta potential. The entrapment efficiency for spans was higher compared to tweens. DSC and IR studies confirmed the absence of chemical interactions between the risperidone and proniosome components. In-vitro release study showed that formulations with spans exhibit controlled release profile and followed the Higuchi model. No significant change in vesicle size and entrapment efficiency was observed when the proniosomes were stored at 4 ± 1 °C and 25 ± 2 °C for three months. Proniosomes with span 60 showed no signs of erythema or edema and has highest flux across the rat skin (169.851 ± 2.13 μg cmâ2 hâ1). The relative bioavailability was 92% after transdermal administration of proniosomes and the tmax was increased to 8 h. So we conclude that the developed proniosome formulation would be a promising alternative to improve the bioavailability problems of risperidone. Keywords: Risperidone, Proniosomes, Transdermal systems, Atypical antipsychotic, Relative bioavailabilit