Objective Clinical utility of lornoxicam in oral therapy is primarily restricted by the low solubility and gastric adverse effects. This study evaluated the prospective of optimized proniosomal gel to improve the clinical efficacy of lornoxicam and compare with oral therapy. Methods Proniosomes were formulated by coacervation phase separation technique using span 60, lecithin and cholesterol. A four-factor three-level Box-Behnken design was used to evaluate the effect of amount of four independent variables; span 60 (X 1 ), cholesterol (X 2 ), lecithin (X 3 ) and lornoxicam (X 4 ) on response variables; vesicle size (Y 1 ), entrapment efficiency (Y 2 ) and transdermal flux (Y 3 ). The selected proniosomal gel (F19) was characterized, and evaluated for the transdermal efficacy by ex vivo and in vivo experiments. Results Optimization study signifies that amount of formulation components (span 60, cholesterol, lecithin and lornoxicam) influence the vesicle size, entrapment efficiency and/or transdermal flux. Optimized formulation F19 exhibited nano size with high entrapment efficiency, adequate zeta potential, greater transdermal flux and better stability (at refrigerated conditions). The entrapment of lornoxicam in the bilayers of proniosome vesicles was confirmed by differential scanning calorimeter. Release profile of F19 was distinct (p < 0.001) from gel prepared using hydroxypropyl methylcellulose (control) and displayed steady lornoxicam release by Fickian diffusion. Transdermal administration of F19 significantly inhibited the carrageenan induced hindpaw edema in rats as compared to oral lornoxicam group. Conclusions The data observed in this study demonstrated that the developed proniosomal gel (F19) improved the clinical efficacy of lornoxicam as compared to oral therapy.
The objective of this research study was to optimize formulation and process variables affecting characteristic of nanosuspension in bead milling process. In this study, the practically water-insoluble telmisartan was nanoground by using top down method i.e. media milling method. Here the media used is ZnO2 beads. A variety of surface active agents were tested for their stabilizing effects. Formulation factors evaluated were ratio of polymer to drug, whereas process parameters were milling time and concentration of ZnO2 beads. Different concentration of stabilizers such as poloxamer 188, poloxamer 407, HPMC E 15, PVP K30 and combination of stabilizers were used for preparation of telmisartan nanosuspension. Responses measured in this study include particle size measurement, particle size distribution and zeta potential.
Objective: The objective of present research work was to develop formulation of orodispersible tablets of Ivabradine HCl and evaluate it for different evaluation parameters. Methods:The tablets were prepared by direct compression method. The formulation of the tablets were evaluated before compression for characterization of flow properties and after compression for different parameters of orodispersible tablet formulation.Results: Ivabradine hydrochloride orodispersible tablets were developed with considerable increase in drug release as compared to marketed formulations; nine formulations were developed and studied. The difference in drug release values was found to be 100.88 ± 0.10 respectively. The drug was characterized according to different compendial methods, on the basis of identification by HPLC, pH, organoleptic properties and other tests. Parameters evaluated were within prescribed limits and indicated good free flowing properties. The F6 batch with disintegration time 21 ± 3.0 and dissolution 99.29% was selected as optimized formulation. This was compared with conventional marketed formulation and was found superior. Batch F6 was also subjected to stability studies for two months and was tested for its hardness, wetting time, disintegration time, drug contents and dissolution behaviour monthly. Conclusions:By appropriate selection of excipients, it was possible to develop orodispersible tablets of Ivabradine HCl.
Methotrexate is the treatment of choice for rheumatoid arthritis, having significant side effects on oral administration, prompting researchers to consider transdermal administration. Transfersomes can overcome the challenges of transdermal administration of drugs because of their deformable nature, allowing for greater skin penetration than other formulations. However, due to an enormous number of product and process variables, the manufacturing of transfersomes proved a pain. The goal of the research study was to use a Plackett‐Burman design to evaluate an important product and process variables connected with the preparation of methotrexate transfersomes. The influence of six product and process variables on %entrapment efficiency and vesicle deformability was investigated and according to p‐values, and the Pareto chart, the concentration of lipid, edge activator, and methotrexate were found critical variables influencing vesicle features having positive and negative effects on variables. In the future, experimental design may be used to optimize these critical parameters for further exploration in the development of methotrexate transfersomes.
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