The aim of this study was to measure and correlate the temperature dependent solubility data of tadalafil (TDL) in water, ethanol, propylene glycol (PG), polyethylene glycol-400 (PEG-400), and Transcutol from (298.15 to 333.15) K at atmospheric pressure using the shake flask method. The experimental solubilities were regressed by Apelblat equation with a relative deviation in the range of (1.20 to 5.74) % in all solvents investigated at (298.15 to 333.15) K. The root mean square deviation between experimental and calculated solubility was observed less than 1.10 in all solvents investigated. The correlation coefficients in water, ethanol, PG, PEG-400, and Transcutol were observed in the range of 0.997 to 0.999. The solubility of TDL was found to be increased with an increase in temperature in all solvents investigated. The mole fraction solubility of TDL was found to be higher in PEG-400 (1.86•10–2 at 298.15 K) and Transcutol (8.76•10–3 at 298.15 K) as compared to water (5.74•10–7 at 298.15 K), ethanol (1.77•10–4 at 298.15 K) and PG (4.1•10–4 at 298.15 K).

The aim of this study was to measure and correlate the temperature dependent solubility data of tadalafil (TDL) in water, ethanol, propylene glycol (PG), polyethylene glycol-400 (PEG-400), and Transcutol from (298.15 to 333.15) K at atmospheric pressure using the shake flask method. The experimental solubilities were regressed by Apelblat equation with a relative deviation in the range of (1.20 to 5.74) % in all solvents investigated at (298.15 to 333.15) K. The root mean square deviation between experimental and calculated solubility was observed less than 1.10 in all solvents investigated. The correlation coefficients in water, ethanol, PG, PEG-400, and Transcutol were observed in the range of 0.997 to 0.999. The solubility of TDL was found to be increased with an increase in temperature in all solvents investigated. The mole fraction solubility of TDL was found to be higher in PEG-400 (1.86•10–2 at 298.15 K) and Transcutol (8.76•10–3 at 298.15 K) as compared to water (5.74•10–7 at 298.15 K), ethanol (1.77•10–4 at 298.15 K) and PG (4.1•10–4 at 298.15 K).

This study was designed to evaluate the suitability of Pluronic F-127, different grades of Carbopol and cellulosic polymers as gel bases containing tolmetin, a non-steroidal anti-inflammatory drug. In vitro release characteristics, effect of enhancers, viscosity and the mechanism of drug release for different gel bases was studied as well as the anti-inflammatory activity were evaluated. The results showed that the HPMC gel has the superior percent of drug release than the others. The percent released of drug from Carbopol and the Pluronic F-127 gels is concentration defendants. It was found that the drug release from the tested gel bases obeyed the diffusion mechanism. The use of propylene glycol and urea in different concentrations (3.0, 5.0 and 10 % w/v) had enhanced the percent of drug release significantly (p 0.05). The anti-inflammatory activity of the drug in Carbopol gel formulation showed excellent anti-inflammatory activity. These finding highlight the potential local application of tolmetin gel as topical anti-inflammatory medication.

This study was aimed to prepare and characterize fast dissolving films containing antiemetic drug, Metoclopramide hydrochloride (MH), for oral use to avoid more stimulation of emesis by using other dosage forms such as tablets or syrups. Methylcellulose (MC) was used as the film forming polymer and croscarmelose Sodium (CCS) and sodium starch glycolate (SSG) were used as super disintegrants. 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 MH-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 MH was molecularly dispersed in the matrix of MC. The prepared films were also characterized for their tensile strength, percentage of elongation, taste palatability, surface pH, weight and their content uniformity. In addition, MH-loaded oral films were elegant enough, transparent, flexible, smooth, homogeneous and palatable. The films were disintegrated within seconds and the drug was released within 3 min. It was found also that neither addition of superdisintegrant nor their concentrations have an effect on the drug dissolution.

This study was aimed to prepare and characterize fast dissolving films containing antiemetic drug, Metoclopramide hydrochloride (MH), for oral use to avoid more stimulation of emesis by using other dosage forms such as tablets or syrups. Methylcellulose (MC) was used as the film forming polymer and croscarmelose Sodium (CCS) and sodium starch glycolate (SSG) were used as super disintegrants. 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 MH-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 MH was molecularly dispersed in the matrix of MC. The prepared films were also characterized for their tensile strength, percentage of elongation, taste palatability, surface pH, weight and their content uniformity. In addition, MH-loaded oral films were elegant enough, transparent, flexible, smooth, homogeneous and palatable. The films were disintegrated within seconds and the drug was released within 3 min. It was found also that neither addition of superdisintegrant nor their concentrations have an effect on the drug dissolution.

Self-emulsifying drug delivery systems (SEDDS) have been widely employed to improve the oral bioavailability of poorly soluble drugs. In the past few years, SEDDS were extensively investigated to overcome various barriers encountered in the oral delivery of hydrophilic macromolecules (e.g., protein/peptide therapeutics and plasmid DNA (pDNA)), as well as in lowering the effect of food on drugs' bioavailability. However, the main mechanism(s) by which SEDDS could achieve such promising effects remains not fully understood. This review summarizes the recent progress in the use of SEDDS for protecting protein therapeutics and/or pDNA against enzymatic degradation and increasing the oral bioavailability of various drug substances regardless of the dietary condition. Understanding the underlying mechanism(s) of such promising applications will aid in the future development of rationally designed SEDDS. Entrapment of hydrophilic macromolecules in the oil phase of the formed emulsion is critical for protection of the loaded cargoes against enzymatic degradation and the enhancement of oral bioavailability. On the other hand, drug administration as a preconcentrated solution in the SEDDS preconcentrate allows the process of drug absorption to occur independently of the dietary condition, and thus reducing interindividual variability that results from concomitant food intake.

Self-emulsifying drug delivery systems (SEDDS) have been widely employed to improve the oral bioavailability of poorly soluble drugs. In the past few years, SEDDS were extensively investigated to overcome various barriers encountered in the oral delivery of hydrophilic macromolecules (e.g., protein/peptide therapeutics and plasmid DNA (pDNA)), as well as in lowering the effect of food on drugs' bioavailability. However, the main mechanism(s) by which SEDDS could achieve such promising effects remains not fully understood. This review summarizes the recent progress in the use of SEDDS for protecting protein therapeutics and/or pDNA against enzymatic degradation and increasing the oral bioavailability of various drug substances regardless of the dietary condition. Understanding the underlying mechanism(s) of such promising applications will aid in the future development of rationally designed SEDDS. Entrapment of hydrophilic macromolecules in the oil phase of the formed emulsion is critical for protection of the loaded cargoes against enzymatic degradation and the enhancement of oral bioavailability. On the other hand, drug administration as a preconcentrated solution in the SEDDS preconcentrate allows the process of drug absorption to occur independently of the dietary condition, and thus reducing interindividual variability that results from concomitant food intake.

Self-emulsifying drug delivery systems (SEDDS) have been widely employed to improve the oral bioavailability of poorly soluble drugs. In the past few years, SEDDS were extensively investigated to overcome various barriers encountered in the oral delivery of hydrophilic macromolecules (e.g., protein/peptide therapeutics and plasmid DNA (pDNA)), as well as in lowering the effect of food on drugs' bioavailability. However, the main mechanism(s) by which SEDDS could achieve such promising effects remains not fully understood. This review summarizes the recent progress in the use of SEDDS for protecting protein therapeutics and/or pDNA against enzymatic degradation and increasing the oral bioavailability of various drug substances regardless of the dietary condition. Understanding the underlying mechanism(s) of such promising applications will aid in the future development of rationally designed SEDDS. Entrapment of hydrophilic macromolecules in the oil phase of the formed emulsion is critical for protection of the loaded cargoes against enzymatic degradation and the enhancement of oral bioavailability. On the other hand, drug administration as a preconcentrated solution in the SEDDS preconcentrate allows the process of drug absorption to occur independently of the dietary condition, and thus reducing interindividual variability that results from concomitant food intake.

Self-emulsifying drug delivery systems (SEDDS) have been widely employed to improve the oral bioavailability of poorly soluble drugs. In the past few years, SEDDS were extensively investigated to overcome various barriers encountered in the oral delivery of hydrophilic macromolecules (e.g., protein/peptide therapeutics and plasmid DNA (pDNA)), as well as in lowering the effect of food on drugs' bioavailability. However, the main mechanism(s) by which SEDDS could achieve such promising effects remains not fully understood. This review summarizes the recent progress in the use of SEDDS for protecting protein therapeutics and/or pDNA against enzymatic degradation and increasing the oral bioavailability of various drug substances regardless of the dietary condition. Understanding the underlying mechanism(s) of such promising applications will aid in the future development of rationally designed SEDDS. Entrapment of hydrophilic macromolecules in the oil phase of the formed emulsion is critical for protection of the loaded cargoes against enzymatic degradation and the enhancement of oral bioavailability. On the other hand, drug administration as a preconcentrated solution in the SEDDS preconcentrate allows the process of drug absorption to occur independently of the dietary condition, and thus reducing interindividual variability that results from concomitant food intake.

Taste-masked microspheres of lornoxicam (LOX) were prepared by spray drying technique using hydroxypropyl methyl cellulose (HPMC) or polyvinyl pyrrolidone (PVP) as polymers in different mass ratios. The effect of polymers and drug-polymer mass ratios on the taste-masking and release properties of co-spray dried microparticles (CSDM) was investigated. CSDM masked the bitter taste of the LOX and enhanced its dissolution rate as compared to pure drug. This improvement in drug dissolution was attributed to both the solubilizing effect of the polymers and physical change in the drug crystal. CSDM formulae with drug, HPMC and PVP (1:4:4) were selected for the preparation of intra-oral tablets (IOTs) because it showed the highest drug release. Three superdisintegrants were used for the preparation of LOX IOTs. IOTs containing croscarmellose sodium released the drug faster than that containing sodium starch and this was probably due to the binding effect of PVP. The anti-inflammatory effects of the prepared LOX IOTs were studied using rat hind paw edema method. The results revealed that IOTs containing croscarmellose sodium showed significant inflammation size reduction in rat hind paw. Palatability studies on human volunteers showed acceptable taste and mouth feel of developed formulation.