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.

Purpose: To prepare solid lipid nanoparticles employing softisan 100 (SOFTI) or tristearin (TS) as solid lipid carriers for celecoxib (CXB) to overcome its dissolution challenge. Methods: The solid lipid nanoparticles (SLN) of CXB were prepared by ultrasonic melt-emulsification technique. SLN was characterized using differential scanning calorimetry (DSC), Fourier transform infra spectroscopy (FTIR), as well as for entrapment efficiency, particle size, zeta potential and CXB release. Results: The SLN formulations exhibited high CXB entrapment efficiency (91.6 % for SOFTI and 94.6 % for TS) while mean particle size was 181.0 ± 4.6 and 346.3 ± 3.8 nm for SOFTI and TS, respectively. The DSC thermograms showed the disappearance of CXB peak due to its molecular distribution in the lipid nanoparticles while FTIR spectra revealed physical interaction of CXB with the tested lipids. The tendency of SOFTI to liberate CXB in 24 h was higher than that of TS (55.5 ± 1.07 vs 49.2 ± 2.94 %, p 0.05). Drug release was by non-Fickian mechanism. Conclusion: Formulation of CXB in SLN using TS or SOFTI produces sustained drug release delivery that can overcome the dissolution limitation of the drug and thus, improve its therapeutic efficacy.

Purpose: To study the effect of compritol ATO888 and kollidon SR blend on the release of chlorpheniramine maleate (CPM) from its matrix tablets prepared by direct compression. Methods: Different ratios of compritol and kollidon SR (containing 50 % matrix component) in 1:1, 1:2, 1:3 and 3:1 ratios were formulated using direct compression. The formulations were organoleptically tested and investigated for CPM release. Results: The release kinetics showed Fickian diffusion mode for kollidone and anomalous release mechanism for compritol matrices. Combining compritol as a lipophilic material and kollidone produced a matrix with controlled drug release. Retardation of drug release rate depended on the ratio of compritol to kollidon. The lower the compritol component, the slower the drug release rate. CPM in matrix tablets containing compritol:kollidone SR in a ratio of 1: 3 achieved optimized sustained release, where 44 % of the drug was released within 8 h (versus 94.5 % for compritol and 54.2 % for kollidon matrix systems). The kinetics of drug release followed Fickian diffusion at low compritol concentration in the blend, reflecting the importance of pore formation. However, when compritol proportion was increased, drug release followed non-Fickian anomalous kinetics due to the water-repelling effect of compritol. Conclusion: Compritol content of CPM matrix tablets can be used to modulate drug release rate as well as release kinetics.

Purpose: To study the effect of compritol ATO888 and kollidon SR blend on the release of chlorpheniramine maleate (CPM) from its matrix tablets prepared by direct compression. Methods: Different ratios of compritol and kollidon SR (containing 50 % matrix component) in 1:1, 1:2, 1:3 and 3:1 ratios were formulated using direct compression. The formulations were organoleptically tested and investigated for CPM release. Results: The release kinetics showed Fickian diffusion mode for kollidone and anomalous release mechanism for compritol matrices. Combining compritol as a lipophilic material and kollidone produced a matrix with controlled drug release. Retardation of drug release rate depended on the ratio of compritol to kollidon. The lower the compritol component, the slower the drug release rate. CPM in matrix tablets containing compritol:kollidone SR in a ratio of 1: 3 achieved optimized sustained release, where 44 % of the drug was released within 8 h (versus 94.5 % for compritol and 54.2 % for kollidon matrix systems). The kinetics of drug release followed Fickian diffusion at low compritol concentration in the blend, reflecting the importance of pore formation. However, when compritol proportion was increased, drug release followed non-Fickian anomalous kinetics due to the water-repelling effect of compritol. Conclusion: Compritol content of CPM matrix tablets can be used to modulate drug release rate as well as release kinetics.

Nimesulide sustained release matrix pellets containing 10 % w/w of the drug were prepared using an extrusion-spheronization technique. Different polymers, ethyl cellulose, Kollicoat, mannitol, lactose and polyethylene glycol (PEG 2000), were mixed at different weight ratios (5, 10 and 20 % w/w) with Avicel PH 101. Mixer torque rheometer (MTR) was used to quantitatively determine the suitable pellets’ moisture content before the extrusion process. The studies revealed that magnitude of torque decreased as the polymer concentration increased. The in vitro release of nimesulide from pellets was dependent upon the type and concentration of the added polymer, which affected the peak torque of the wet mass. In conclusion, the formulation of nimesulide sustained release matrix pellets successfully controlled the drug release, which might be beneficial in lowering the risk of side effects and improving patient convenience as an advantage of the pellets as a drug delivery system.