The aim of the present work was to prepare and evaluate sublingual fast dissolving films containing Metoprolol Tartrate-loaded niosomes. Niosomes were utilized to allow for prolonged release of the drug, whereas, the films were used to increase the drug’s bioavailability via the sublingual route. Niosomes were prepared using Span 60 and Cholesterol at different drug to surfactant ratios. The niosomes were characterized for size, zeta-potential and entrapment efficiency. The selected niosomal formulation was incorporated into polymeric films using HPMC and MC as film-forming polymers and Avicel as superdisintegrant. The physical characteristics (appearance, texture, pH, uniformity of weight and thickness, disintegration time, palatability) of the prepared films were studied, in addition to evaluating the in vitro drug release, stability, and in vivo pharmacokinetics in rabbits. The release of the drug from the medicated film was fast (99.9% of the drug was released within 30 min), while the drug loaded into the niosomes, either incorporated into the film or not, showed only 22.85% drug release within the same time. The selected sublingual film showed significantly higher rate of drug absorption and higher drug plasma levels compared to that of commercial oral tablet. The plasma levels remained detectable for 24 h following sublingual administration, compared to only 12 h after administration of the oral tablet. In addition, the absolute bioavailability of the drug (i.e. relative to intravenous administration) following sublingual administration was found to be significantly higher (91.06  13.28%), as compared to that after oral tablet administration (39.37  11.4%). These results indicate that the fast dissolving niosomal film could be a promising delivery system to enhance the bioavailability and prolong the therapeutic effect of Metoprolol Tartrate.

The aim of the present work was to prepare and evaluate sublingual fast dissolving films containing Metoprolol Tartrate-loaded niosomes. Niosomes were utilized to allow for prolonged release of the drug, whereas, the films were used to increase the drug’s bioavailability via the sublingual route. Niosomes were prepared using Span 60 and Cholesterol at different drug to surfactant ratios. The niosomes were characterized for size, zeta-potential and entrapment efficiency. The selected niosomal formulation was incorporated into polymeric films using HPMC and MC as film-forming polymers and Avicel as superdisintegrant. The physical characteristics (appearance, texture, pH, uniformity of weight and thickness, disintegration time, palatability) of the prepared films were studied, in addition to evaluating the in vitro drug release, stability, and in vivo pharmacokinetics in rabbits. The release of the drug from the medicated film was fast (99.9% of the drug was released within 30 min), while the drug loaded into the niosomes, either incorporated into the film or not, showed only 22.85% drug release within the same time. The selected sublingual film showed significantly higher rate of drug absorption and higher drug plasma levels compared to that of commercial oral tablet. The plasma levels remained detectable for 24 h following sublingual administration, compared to only 12 h after administration of the oral tablet. In addition, the absolute bioavailability of the drug (i.e. relative to intravenous administration) following sublingual administration was found to be significantly higher (91.06  13.28%), as compared to that after oral tablet administration (39.37  11.4%). These results indicate that the fast dissolving niosomal film could be a promising delivery system to enhance the bioavailability and prolong the therapeutic effect of Metoprolol Tartrate.

The main aim of this work was to develop rectal suppositories for better delivery of metoprolol tartrate (MT). The various bases used were fatty, water soluble and emulsion bases. The physical properties of the prepared suppositories were characterized such as weight variation, hardness, disintegration time, melting range and the drug content uniformity. The in vitro release of MT from the prepared suppositories was carried out. The evaluation of the pharmacological effects of MT on the blood pressure and heart rate of the healthy rabbits after the rectal administration compared to the oral tablets was studied. Moreover, the formulation with the highest in vitro release and the highest pharmacological effects would be selected for a further pharmacokinetics study compared to the oral tablets. The results revealed that the emulsion bases gave the highest rate of the drug release than the other bases used. The reduction effect of the emulsion MT suppository base on the blood pressure and heart rate was found to be faster and greater than that administered orally. The selected emulsion suppository base (F11) showed a significant increase in the AUC (1.88-fold) in rabbits as compared to the oral tablets. From the above results we can conclude that rectal route can serve as an efficient alternative route to the oral one for systemic delivery of MT which may be due to the avoidance of first-pass effect in the liver.

The main aim of this work was to develop rectal suppositories for better delivery of metoprolol tartrate (MT). The various bases used were fatty, water soluble and emulsion bases. The physical properties of the prepared suppositories were characterized such as weight variation, hardness, disintegration time, melting range and the drug content uniformity. The in vitro release of MT from the prepared suppositories was carried out. The evaluation of the pharmacological effects of MT on the blood pressure and heart rate of the healthy rabbits after the rectal administration compared to the oral tablets was studied. Moreover, the formulation with the highest in vitro release and the highest pharmacological effects would be selected for a further pharmacokinetics study compared to the oral tablets. The results revealed that the emulsion bases gave the highest rate of the drug release than the other bases used. The reduction effect of the emulsion MT suppository base on the blood pressure and heart rate was found to be faster and greater than that administered orally. The selected emulsion suppository base (F11) showed a significant increase in the AUC (1.88-fold) in rabbits as compared to the oral tablets. From the above results we can conclude that rectal route can serve as an efficient alternative route to the oral one for systemic delivery of MT which may be due to the avoidance of first-pass effect in the liver.

The main aim of this work was to develop rectal suppositories for better delivery of metoprolol tartrate (MT). The various bases used were fatty, water soluble and emulsion bases. The physical properties of the prepared suppositories were characterized such as weight variation, hardness, disintegration time, melting range and the drug content uniformity. The in vitro release of MT from the prepared suppositories was carried out. The evaluation of the pharmacological effects of MT on the blood pressure and heart rate of the healthy rabbits after the rectal administration compared to the oral tablets was studied. Moreover, the formulation with the highest in vitro release and the highest pharmacological effects would be selected for a further pharmacokinetics study compared to the oral tablets. The results revealed that the emulsion bases gave the highest rate of the drug release than the other bases used. The reduction effect of the emulsion MT suppository base on the blood pressure and heart rate was found to be faster and greater than that administered orally. The selected emulsion suppository base (F11) showed a significant increase in the AUC (1.88-fold) in rabbits as compared to the oral tablets. From the above results we can conclude that rectal route can serve as an efficient alternative route to the oral one for systemic delivery of MT which may be due to the avoidance of first-pass effect in the liver.

Titanium implants can fail due to inappropriate biomechanics at the bone–implant interface that leads to suboptimal osseointegration. Titania nanotubes (TNTs) fabricated on Ti implants by the electrochemical process have emerged as a promising modification strategy to facilitate osseointegration. TNTs enable augmentation of bone cell functions at the bone–implant interface and can be tailored to incorporate multiple functionalities including the loading of active biomolecules into the nanotubes to target anabolic processes in bone conditions such as osteoporotic fractures. Advanced functions can be introduced, including biopolymers, nanoparticles and electrical stimulation to release growth factors in a desired manner. This review describes the application of TNTs for enhancing osteogenesis at the bone–implant interface, as an alternative approach to systemic delivery of therapeutic agents.

Non-ionic surfactant vesicles containing fluconazole (FLZ) were prepared using, span 60 or span 80 and cholesterol in weight ratios of 1:1, 2:1 and 1:2. The prepared vesicles were characterized for size, entrapment efficiency, and in vitro drug release. The drug encapsulation efficiencies varied from 40.0% to 84.35%. The particle size ranged from 140 to 280 nm. Higher encapsulation was obtained by the span 60: cholesterol ratio of 2:1, which showed the best drug release. The selected niosomal formulations were incorporated into poloxamer 407 and chitosan gel formulations. Drug release from niosomal dispersions and niosomal gels, permeation of drug from niosomal gels through goat cornea and its antifungal activity were evaluated. Results showed that the surfactant: cholesterol ratio had a significant effect on the encapsulation efficiency and the size of vesicles. The niosomes prepared with 2:1 surfactant: cholesterol showed superior release over the other niosomal formulations. The drug release and permeation from poloxamer gel were higher than that from chitosan gel. Permeation study showed that, the flux of drug was dependent on the viscosity of the gel. The selected niosomal gels had excellent antifungal activity where the poloxamer niosomal gel was more effective compared to chitosan niosomal gel.

Niosomes have been reported as a possible approach to improve low skin permeation shown by conventional vehicles. In this study, a noisome-based delivery system of meloxicam (MX) was developed and characterized for in vitro performance. Niosomes were prepared by reverse-phase evaporation method (REV) using different non ionic surfactants and cholesterol in different molar ratios (1:1, 2:1, 3:1,1: 2 and 1:3) and different drug loading (5, 10 and 15 mg). The used surfactants included Tweens (20, 40 and 80), Brij (35 and 58) and Myrj 52. The prepared systems were characterized for entrapment efficiency, and in-vitro release. Accordingly, selected systems were evaluated for vesicle size, and formulated into different hydrogel bases (sodium carboxymethyl cellulose, hydroxypropyl cellulose, and sodium alginate). Invitro drug release from the different formulations was studied over a period of 8 hr. Effect of formulation additives on drug release was also investigated. The anti-inflammatory activity of the selected formulations was evaluated by the paw edema test. Results showed high encapsulation efficiency which ranged from about 81.93% to 99.23%. The highest entrapment efficiency was obtained with 1:1 surfactant: cholesterol ratio and 15 mg drug loading, so niosomes prepared by this ratio were selected for further studies. Particle size ranged from 4.047 to 12.334 μm for different niosomal systems. In vitro drug release from different gel formulations containing 0.3% MX was compared to that from the same formulations containing 0.3% niosomally entrapped drug. In all formulations the drug release was more sustained in case of niosomally entrapped drug. Incorporation of glycerol and propylene glycol as formulation additives into gel formulations markedly enhanced the drug release, but the release from gels containing niosomally entrapped drug was still delayed

Niosomes have been reported as a possible approach to improve low skin permeation shown by conventional vehicles. In this study, a noisome-based delivery system of meloxicam (MX) was developed and characterized for in vitro performance. Niosomes were prepared by reverse-phase evaporation method (REV) using different non ionic surfactants and cholesterol in different molar ratios (1:1, 2:1, 3:1,1: 2 and 1:3) and different drug loading (5, 10 and 15 mg). The used surfactants included Tweens (20, 40 and 80), Brij (35 and 58) and Myrj 52. The prepared systems were characterized for entrapment efficiency, and in-vitro release. Accordingly, selected systems were evaluated for vesicle size, and formulated into different hydrogel bases (sodium carboxymethyl cellulose, hydroxypropyl cellulose, and sodium alginate). Invitro drug release from the different formulations was studied over a period of 8 hr. Effect of formulation additives on drug release was also investigated. The anti-inflammatory activity of the selected formulations was evaluated by the paw edema test. Results showed high encapsulation efficiency which ranged from about 81.93% to 99.23%. The highest entrapment efficiency was obtained with 1:1 surfactant: cholesterol ratio and 15 mg drug loading, so niosomes prepared by this ratio were selected for further studies. Particle size ranged from 4.047 to 12.334 μm for different niosomal systems. In vitro drug release from different gel formulations containing 0.3% MX was compared to that from the same formulations containing 0.3% niosomally entrapped drug. In all formulations the drug release was more sustained in case of niosomally entrapped drug. Incorporation of glycerol and propylene glycol as formulation additives into gel formulations markedly enhanced the drug release, but the release from gels containing niosomally entrapped drug was still delayed

Nonionic surfactant vesicles containing celecoxib (CXB) as an anti-inflammatory drug were prepared using, Span 60 or Span 40 and cholesterol in the ratios of 1:0, 1:1 and 1:2. Prepared vesicles were characterized for encapsulation efficiency, particle size and drug release. The drug encapsulation efficiencies varied from 60.55 to 80.35%. The vesicle size ranged from 170 to 235 nm. The high encapsulation was achieved by the ratio 1:1 of span 60: cholesterol and this formula showed significant in vitro release of the drug (80%) as compared to other forms (P 0.05). Among niosomal gels investigated, poloxamer 407 niosomal gel showed significant drug release (72% after 12 h) over the other forms (P 0.05). The results also showed that the release of CXB from the niosomes and niosomal gels obeyed the Higuchi’s diffusion model. The anti-inflammatory activity of the drug from different niosomal gel formulations was also studied using Carrageenan induced rat paw edema method. The results showed that there is significant anti-inflammatory activity (75.45%) of the poloxamer niosomal gel on rat paw edema (P 0.05).