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Albendazole belongs to BCS-II category whose systemic and local anthelmintic effectiveness is restricted due to its low water solubility–related dissolution properties. The present investigation was aimed to prepare salts of albendazole using various weak organic acids such as succinic acid, tartaric acid, benzoic acid, and citric acid as counterions. The solvent evaporation was used to prepare the salts. The results of differential scanning calorimetry, Fourier-transform infrared spectroscopy, and powder X-ray diffraction suggested the formation of a new crystalline solid phase due to reaction between ABZ and organic acids. The results of 1H NMR studies indicted the participation of protons attached to nitrogen atoms (N–-H +) in the salt formation process. A significantly higher amount of drug release was observed in in vitro dissolution study from all the prepared salts compared to a pure drug in 0.1 N HCl. Contrary to that, no significant improvement was observed in in vitro dissolution study performed in 6.8 pH phosphate buffer. The prepared novel salts successfully improved the saturation solubility and dissolution properties of albendazole.

This study aimed to develop and optimize lutein-loaded solid lipid nanoparticles (Lu-SLN) for ocular delivery. The objective was to achieve the mean particle size of Lu-SLN less than 100 nm, sustain the drug release up to 8 h, and evaluate the corneal permeation parameters of the optimized batch. Lu-SLN were prepared by hot homogenization and cold dilution method. The Plackett-Burman screening design and 32 full factorial design were adopted sequentially to study the effect of various formulation and process variables, and further optimized with the help of desirability function. The statistical designs revealed that the amount of Gelucire® 44/14 and homogenization speed had a significant effect (P

The present study was aimed to develop and optimize linezolid loaded chitosan nanoparticles for pulmonary delivery. The objective was to achieve the mean particle size of nanoparticles less than 300 nm and the mass median aerodynamic diameter (MMAD) less than 5 μm and sustain the drug release up to 24 h. Linezolid nanoparticles were prepared by ionic gelation technique employing chitosan and sodium tripolyphosphate (STPP). A 32 full factorial design and desirability function were sequentially used to quantify the effect of independent variables on dependent variables and optimize the formulation. The preliminary studies suggested that the concentration of chitosan and concentration of STPP had an appreciable effect on mean particle size and percentage entrapment efficiency and hence were selected as independent variables in a factorial design. Statistical analysis of 32 full factorial design revealed that each independent variable had a significant effect (p

The present investigation was carried out to design, optimize, and evaluate lurasidone hydrochloride nanocrystals for improving its solubility and dissolution characteristics. Nanocrystals were prepared by media milling technique using zirconium oxide beads with 0.1 mm diameter. Various stabilizers, viz. poloxamer 188, PVP K30, SLS, HPMC E15, and PVP S 630 D, were evaluated to stabilize the nanocrystals. The Pareto chart obtained through Plackett-Burman screening design revealed that HPMC E 15 showed the highest standardized effect (p value

The aim of this study is to improve the bioavailability of a poorly water-soluble drug glibenclamide (GLB), by preparing drug nanocrystals using wet milling by zirconia beads. To improve the dissolution characteristics, various formulation and process variables were identified and optimized by employing a 32 factorial design at two stages. Based on preliminary studies, the formulation variables selected were polymer-to-drug ratio and surfactant-to-drug ratio and the process variables selected were milling speed and milling time. The particle size, zeta potential, saturation solubility, and percentage drug released at 10 min were selected as dependent variables at both stages. F ratio suggested that the predetermined response parameters were significantly dependent on the independent variables. An optimum desirability of 0.9925 was achieved using response profiler by Statistica® 8.0. The optimized formulation prepared as per levels obtained through desirability showed a close agreement between the predicted and expected values. X-ray diffraction studies concluded that the crystallinity of prepared nanocrystals was intact and the increased dissolution could be ascribed to conversion of unmilled drug to nanocrystals. In vivo studies carried out on male Wistar rats suggested a higher AUEC(0–8h) for GLB nanocrystals as compared to pure GLB which could be ascribed to significant improvement of release from GLB nanocrystals as compared to pure GLB. It could be concluded that prepared GLB nanocrystals showed better bioavailability as compared to pure GLB and could offer improved drug therapy.

Ezetimibe (EZE), a water insoluble drug, depicts variable bioavailability. The objective of the present investigation was to improve dissolution characteristics of EZE, which might offer improved bioavailability. The solid dispersions were prepared using poloxamer 407 (L 127) and polyvinyl pyrrolidone by melt and solvent method, respectively. Phase solubility studies indicated linear relationship between drug solubility and carrier concentration. In vitro release studies revealed improvement in the dissolution characteristics of EZE in solid dispersions. Solid dispersion with L 127 gave better rate and extent of dissolution. The best fit model indicating the probable mechanism of drug release from solid dispersions was found to be Korsemeyer–Peppas. The results of characterization of solid dispersions by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction revealed reduction in drug crystallinity which might be responsible for improved dissolution properties. The tablets of solid dispersion, containing L 127 prepared by direct compression, exhibited better drug release as compared to marketed formulation.

The present work is aimed to develop and optimize pulsatile delivery during dissolution of an improved formulation of valsartan to coordinate the drug release with circadian rhythm. Preliminary studies suggested that β cyclodextrin could improve the solubility of valsartan and showed AL type solubility curve. A 1:1 stoichiometric ratio of valsartan to β cyclodextrin was revealed from phase solubility studies and Job's plot. The prepared complex showed significantly better dissolution efficiency (p