The purpose of the current study is to develop nanostructured lipid carriers (NLCs) for the delivery of the antihyperlipidemic drug simvastatin (SIM) to increase its extremely low oral bioavailability (5%) and prolong its antihyperlipidemic effect. NLCs were prepared via emulsification-solvent evaporation technique followed by ultrasonication, and the effect of composition of the nanocarriers on the particle size, size distribution, surface charge, entrapment efficiency, drug release kinetics and physical stability was extensively studied. NLCs exhibited nanosized (200 nm) spherical morphologies with narrow size distribution and high drug entrapment efficiency (>75%), sustained drug release pattern, and negative surface charge (zeta potential of −35–40 mV) that imparts sufficient electrostatic physical stability. When tested in vivo, SIM-NLCs of the optimal composition demonstrated improved and prolonged reduction in the total cholesterol and non-high density lipoprotein cholesterol levels, as compared to the drug suspension. After oral administration of a single dose of SIM-NLC, 4-fold increase in bioavailability was observed, as compared to the SIM suspension. Hence, NLCs might provide efficient nanodevices for the management of hyperlipidemia and promising drug delivery systems to enhance SIM oral bioavailability.

The purpose of the current study is to develop nanostructured lipid carriers (NLCs) for the delivery of the antihyperlipidemic drug simvastatin (SIM) to increase its extremely low oral bioavailability (5%) and prolong its antihyperlipidemic effect. NLCs were prepared via emulsification-solvent evaporation technique followed by ultrasonication, and the effect of composition of the nanocarriers on the particle size, size distribution, surface charge, entrapment efficiency, drug release kinetics and physical stability was extensively studied. NLCs exhibited nanosized (200 nm) spherical morphologies with narrow size distribution and high drug entrapment efficiency (>75%), sustained drug release pattern, and negative surface charge (zeta potential of −35–40 mV) that imparts sufficient electrostatic physical stability. When tested in vivo, SIM-NLCs of the optimal composition demonstrated improved and prolonged reduction in the total cholesterol and non-high density lipoprotein cholesterol levels, as compared to the drug suspension. After oral administration of a single dose of SIM-NLC, 4-fold increase in bioavailability was observed, as compared to the SIM suspension. Hence, NLCs might provide efficient nanodevices for the management of hyperlipidemia and promising drug delivery systems to enhance SIM oral bioavailability.

The purpose of the current study is to develop nanostructured lipid carriers (NLCs) for the delivery of the antihyperlipidemic drug simvastatin (SIM) to increase its extremely low oral bioavailability (5%) and prolong its antihyperlipidemic effect. NLCs were prepared via emulsification-solvent evaporation technique followed by ultrasonication, and the effect of composition of the nanocarriers on the particle size, size distribution, surface charge, entrapment efficiency, drug release kinetics and physical stability was extensively studied. NLCs exhibited nanosized (200 nm) spherical morphologies with narrow size distribution and high drug entrapment efficiency (>75%), sustained drug release pattern, and negative surface charge (zeta potential of −35–40 mV) that imparts sufficient electrostatic physical stability. When tested in vivo, SIM-NLCs of the optimal composition demonstrated improved and prolonged reduction in the total cholesterol and non-high density lipoprotein cholesterol levels, as compared to the drug suspension. After oral administration of a single dose of SIM-NLC, 4-fold increase in bioavailability was observed, as compared to the SIM suspension. Hence, NLCs might provide efficient nanodevices for the management of hyperlipidemia and promising drug delivery systems to enhance SIM oral bioavailability.

The purpose of the current study is to develop nanostructured lipid carriers (NLCs) for the delivery of the antihyperlipidemic drug simvastatin (SIM) to increase its extremely low oral bioavailability (5%) and prolong its antihyperlipidemic effect. NLCs were prepared via emulsification-solvent evaporation technique followed by ultrasonication, and the effect of composition of the nanocarriers on the particle size, size distribution, surface charge, entrapment efficiency, drug release kinetics and physical stability was extensively studied. NLCs exhibited nanosized (200 nm) spherical morphologies with narrow size distribution and high drug entrapment efficiency (>75%), sustained drug release pattern, and negative surface charge (zeta potential of −35–40 mV) that imparts sufficient electrostatic physical stability. When tested in vivo, SIM-NLCs of the optimal composition demonstrated improved and prolonged reduction in the total cholesterol and non-high density lipoprotein cholesterol levels, as compared to the drug suspension. After oral administration of a single dose of SIM-NLC, 4-fold increase in bioavailability was observed, as compared to the SIM suspension. Hence, NLCs might provide efficient nanodevices for the management of hyperlipidemia and promising drug delivery systems to enhance SIM oral bioavailability.

Purpose: To enhance the dissolution of albendazole (ABZ) using spray-drying technique. Method: ABZ binary mixtures with Kollicoat IR® (KL) and polyvinyl pyrrolidone (PVP) in various drug to polymer ratios (1: 1, 1: 2 and 1; 4) were prepared by spray-drying. The spray-dried particles were characterized for particle shape, and dissolution rate as well as by differential scanning calorimetry(DSC) and Fourier transform infrared (FTIR). Results: Scanning electron micrographs showed a homogeneous distribution of ABZ in the polymer matrix for ABZ-PVP spray-dried system in ratios of 1: 2 and 1: 4, while it was observed only upon using a ratio of ABZ: KL 1: 4 in case of ABZ-KL systems. FT-IR spectra of both physical mixtures and spraydried mixtures did not show any change for all ABZ-polymer systems, thus indicating the compatibility of the carriers with ABZ. ABZ exhibited a noticeable enhanced dissolution rate from its spray-dried coacervate with PVP and this was independent of the drug/polymer ratio. Drug release was 78, 81 and 81 % from the spray-dried ABZ-PVP systems of drug: polymer ratio of 1:1, 1:2 and 1: 4, respectively, within 5 min. Drug showed complete dissolution within 15 min. On the other hand, enhancement of dissolution rate varied with ABZ: Kl ratio. Conclusion: Enhancement of ABZ dissolution for both types of spray-dried particles is due to the reduction in drug particle sizes, wetting of the dissolution medium by the hydrophilic carriers and the amorphosization of the drug crystals by the carriers.

Purpose: To enhance the dissolution of albendazole (ABZ) using spray-drying technique. Method: ABZ binary mixtures with Kollicoat IR® (KL) and polyvinyl pyrrolidone (PVP) in various drug to polymer ratios (1: 1, 1: 2 and 1; 4) were prepared by spray-drying. The spray-dried particles were characterized for particle shape, and dissolution rate as well as by differential scanning calorimetry(DSC) and Fourier transform infrared (FTIR). Results: Scanning electron micrographs showed a homogeneous distribution of ABZ in the polymer matrix for ABZ-PVP spray-dried system in ratios of 1: 2 and 1: 4, while it was observed only upon using a ratio of ABZ: KL 1: 4 in case of ABZ-KL systems. FT-IR spectra of both physical mixtures and spraydried mixtures did not show any change for all ABZ-polymer systems, thus indicating the compatibility of the carriers with ABZ. ABZ exhibited a noticeable enhanced dissolution rate from its spray-dried coacervate with PVP and this was independent of the drug/polymer ratio. Drug release was 78, 81 and 81 % from the spray-dried ABZ-PVP systems of drug: polymer ratio of 1:1, 1:2 and 1: 4, respectively, within 5 min. Drug showed complete dissolution within 15 min. On the other hand, enhancement of dissolution rate varied with ABZ: Kl ratio. Conclusion: Enhancement of ABZ dissolution for both types of spray-dried particles is due to the reduction in drug particle sizes, wetting of the dissolution medium by the hydrophilic carriers and the amorphosization of the drug crystals by the carriers.

The aim of this study was to formulate and characterize fast dissolving films containing dextromethorphan hydrobromide (DM) for oral use. Hydroxylpropyl methylcellulose E15 (HPMC) was used as the film forming polymer and crosspovidone (CPV), microcrystalline cellulose (MCC) were used as superdisintegrants. In this study, medicated films were prepared by solvent casting method. The physicochemical characterizations were done by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) for DM-loaded fast dissolving films and their corresponding physical mixtures as well as the individual components to investigate the drug polymer interaction. The obtained DSC and FTIR results indicated that DM was molecularly dispersed in the matrix of HPMC. The prepared films were also characterized for their tensile strength, percentage of elongation, taste palatability, surface pH, weight and their content uniformity. In addition, DM-loaded oral films were elegant enough, transparent, flexible, smooth, homogeneous and palatable. It was found also that both of film disintegration and drug release increased as the concentration of disintegrant in the film increased.

Famotidine (FM) is a potent H2-receptor antagonist used for the treatment of peptic ulcer. It has a low and variable bioavailability which is attributed to its low water solubility. In this study, the dissolution of the drug was enhanced by a preparation of solid dispersion using two hydrophilic carriers, namely Gelucire 50/13 and Pluronic F-127. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), which indicated that there were no signs of interaction of the drug with the carriers used in the case of solid dispersions containing higher polymeric contents (1:3 and 1:5). FM solid dispersions in the matrices of Gelucire 50/13 and Pluronic F-127 (1:3) were used to prepare pellets. The scanning electron microscope (SEM) images of pellets showed that the pellets have spherical shape and their size depends on the carrier used. The dissolution of the drug from either solid dispersion or pellets was performed. The dissolution study depicted that, the presence of the drug in solid dispersion enhanced its dissolution in comparison with the drug itself. Also, the drug release from the manufactured pellets was found to be improved in the case of solid dispersions (drug : carrier 1:3). A complete drug release occurred after 30 min from pellets containing solid dispersions, while only about 30% of the loaded FM was released from pellets containing untreated drug after 2 h.

Temperature dependent solubility data of tadalafil (TDL) in diethylene glycol monoethyl ether (Transcutol) + water co-solvent mixtures are not available in literature. Therefore, the aim of present study was to determine the temperature dependent solubility data of crystalline TDL in mono-solvents and various Transcutol + water co-solvent mixtures from 298.15 to 333.15 K at atmospheric pressure. The experimental solubilities of crystalline TDL were measured using the shake flask method. The experimental solubilities were correlated with the Apelblat model. The solubilities of crystalline TDL were regressed by Apelblat equation with a relative deviation in the range of 0.02 to 6.81% in all co-solvent mixtures investigated at 298.15 to 333.15 K. The root mean square deviations were observed in the range of 0.013 to 0.058. However, the correlation coefficients were observed in the range of 0.996 to 0.999. The solubility of crystalline TDL was found to be increased with increase in temperature and mass fraction of Transcutol in co-solvent mixtures. The mole fraction solubility of crystalline TDL was observed highest in pure Transcutol (8.76×10−3 at 298.15 K) as compared to water (5.74×10−7 at 298.15 K). Around 15,263 fold enhancements in solubility of crystalline TDL in Transcutol were observed as compared to its aqueous solubility at 298.15 K. The dissolution of TDL in most of the co-solvent mixtures was assumed to be non-spontaneous, endothermic and an entropy driven process. Overall, the results of these studies indicated that Transcutol could be used as a co-solvent in formulation development especially in terms of liquid dosage forms of crystalline TDL.

In present study, the solubility data of tadalafil in mono-solvents and various polyethylene glycol 400 (PEG 400) + water co-solvent mixtures from 298.15 to 333.15 K was measured. The experimental mole fraction solubility data of TDL from 298.15 to 333.15 K was measured and correlated. The experimental solubilities of TDL were regressed by the modified Apelblat model with absolute relative deviation in the range of 0.0006-2.2000 % in all co-solvent mixtures. However, the correlation coefficients were observed in the range of 0.9955-0.9998. The mean absolute errors by Yalkowsky model were observed in the range of 0.332-0.442. The mole fraction solubility of TDL was found to be highest in pure PEG 400 (1.86 × 10- 2 at 298.15 K) as compared to water (5.7 × 10- 7 at 298.15 K). The thermophysical parameters such as enthalpies and entropies for TDL dissolution indicated that the dissolution of TDL is endothermic and an entropy-driven process.