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.

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.

In this study, new tablet formulations of spray-dried binary systems (SD) of meloxicam (MLX) with either Kollicoat IR® or polyvinylpyrrolidone (PVP) were prepared and characterized in comparison with a commercial tablet product (Mobic®). Physicochemical characterization of prepared microparticles was carried out by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) for MLX binary systems as well as the untreated drug and polymers to investigate the possibility of drug polymer interaction. Prepared and commercial tablets as well as SD were evaluated for their in vitro release rate in phosphate buffer (pH 7.4). Physicochemical characterization indicated that the drug is dispersed in the carrier and there is possibility of physical intermolecular hydrogen bonding between MLX and both Kollicoat IR® and PVP. Moreover, the prepared tablets showed higher dissolution rates compared with the innovator product. In addition, prepared tablets exhibited acceptable hardness, friability and drug content.

In this study, new tablet formulations of spray-dried binary systems (SD) of meloxicam (MLX) with either Kollicoat IR® or polyvinylpyrrolidone (PVP) were prepared and characterized in comparison with a commercial tablet product (Mobic®). Physicochemical characterization of prepared microparticles was carried out by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) for MLX binary systems as well as the untreated drug and polymers to investigate the possibility of drug polymer interaction. Prepared and commercial tablets as well as SD were evaluated for their in vitro release rate in phosphate buffer (pH 7.4). Physicochemical characterization indicated that the drug is dispersed in the carrier and there is possibility of physical intermolecular hydrogen bonding between MLX and both Kollicoat IR® and PVP. Moreover, the prepared tablets showed higher dissolution rates compared with the innovator product. In addition, prepared tablets exhibited acceptable hardness, friability and drug content.

The aim of current work is to compare the impact of nano-cavity size of natural cyclodextrins (CDs) and nano-micelle size of certain non-ionic surfactants on the solubility of isoxsuprine HCl (IXP HCl). The results showed that the solubility of IXP HCl increased with β-CD more than with α-CD which might be due to the larger cavity size of β-CD than that of α-CD. In case of surfactants, it was found that the solubilizing power of surfactants increased with surfactant having shorter hydrocarbon chain in a homologous series. While, in case of polyoxyethylene fatty alcohol ethers, the longer the hydrophilic chain and shorter lipophilic chain, the solubility capacity was greater. These results conclude that micellar solubilization of IXP HCl by non-ionic surfactants was occurred. Comparatively, the solubilizing efficiency of CDs toward IXP HCl was greater than non-ionic surfactants.

The aim of current work is to compare the impact of nano-cavity size of natural cyclodextrins (CDs) and nano-micelle size of certain non-ionic surfactants on the solubility of isoxsuprine HCl (IXP HCl). The results showed that the solubility of IXP HCl increased with β-CD more than with α-CD which might be due to the larger cavity size of β-CD than that of α-CD. In case of surfactants, it was found that the solubilizing power of surfactants increased with surfactant having shorter hydrocarbon chain in a homologous series. While, in case of polyoxyethylene fatty alcohol ethers, the longer the hydrophilic chain and shorter lipophilic chain, the solubility capacity was greater. These results conclude that micellar solubilization of IXP HCl by non-ionic surfactants was occurred. Comparatively, the solubilizing efficiency of CDs toward IXP HCl was greater than non-ionic surfactants.

The aim of current work is to compare the impact of nano-cavity size of natural cyclodextrins (CDs) and nano-micelle size of certain non-ionic surfactants on the solubility of isoxsuprine HCl (IXP HCl). The results showed that the solubility of IXP HCl increased with β-CD more than with α-CD which might be due to the larger cavity size of β-CD than that of α-CD. In case of surfactants, it was found that the solubilizing power of surfactants increased with surfactant having shorter hydrocarbon chain in a homologous series. While, in case of polyoxyethylene fatty alcohol ethers, the longer the hydrophilic chain and shorter lipophilic chain, the solubility capacity was greater. These results conclude that micellar solubilization of IXP HCl by non-ionic surfactants was occurred. Comparatively, the solubilizing efficiency of CDs toward IXP HCl was greater than non-ionic surfactants.