“…These results may be due to the entrapment of the drug in vesicular system within the formed film. These data are in agreement with previously reported data of celecoxib niosomal gel 61 and meloxicam niosomal hydrogel. 32 …”
Section: Resultssupporting
confidence: 94%
“…Similar melting transition results were obtained on thermal analysis of both cholesterol and span 60. 32 , 61 Concerning the corresponding physical mixture of MT and MC, cholesterol, or span 60, the characteristic endothermic peak of the drug was still seen with low intensity, only for span 60. These results indicate that the drug is in crystalline form with no degradation and that these components could be considered compatible with MT.…”
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 hydroxypropyl methyl cellulose E15 and methyl cellulose as film-forming polymers and Avicel as superdisintegrant. The physical characteristics (appearance, texture, pH, uniformity of weight and thickness, disintegration time, and 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 minutes), 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 with that of commercial oral tablet. The plasma levels remained detectable for 24 hours following sublingual administration, compared with only 12 hours after administration of the oral tablet. In addition, the absolute bioavailability of the drug (ie, relative to intravenous administration) following sublingual administration was found to be significantly higher (91.06%±13.28%), as compared with 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.
“…These results may be due to the entrapment of the drug in vesicular system within the formed film. These data are in agreement with previously reported data of celecoxib niosomal gel 61 and meloxicam niosomal hydrogel. 32 …”
Section: Resultssupporting
confidence: 94%
“…Similar melting transition results were obtained on thermal analysis of both cholesterol and span 60. 32 , 61 Concerning the corresponding physical mixture of MT and MC, cholesterol, or span 60, the characteristic endothermic peak of the drug was still seen with low intensity, only for span 60. These results indicate that the drug is in crystalline form with no degradation and that these components could be considered compatible with MT.…”
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 hydroxypropyl methyl cellulose E15 and methyl cellulose as film-forming polymers and Avicel as superdisintegrant. The physical characteristics (appearance, texture, pH, uniformity of weight and thickness, disintegration time, and 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 minutes), 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 with that of commercial oral tablet. The plasma levels remained detectable for 24 hours following sublingual administration, compared with only 12 hours after administration of the oral tablet. In addition, the absolute bioavailability of the drug (ie, relative to intravenous administration) following sublingual administration was found to be significantly higher (91.06%±13.28%), as compared with 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.
“…Physical mixture of acyclovir sodium or vancomycin hydrochloride and different niosomal components showed nearly the same thermal behavior as the individual components (Supplementary Information, Figures S5 and S6). It was observed that when Span ® 60 presents in the physical mixture, only a sharp endothermic peak for Span ® 60 can be seen at the same position, whereas small peaks were observed for other materials in the mixture 32 . Thermograms of the physical mixtures demonstrate that there were no interactions between the drugs and other materials in the solid state.Figure 8DSC thermograms of vancomycin hydrochloride pure drug powder ( A ), cholesterol ( B ), Span ® 60 ( C ), unloaded niosomes ( D ) and vancomycin-loaded niosomes ( E ).Figure 9DSC thermograms of acyclovir sodium pure drug powder ( A ), cholesterol ( B ), Span ® 60 ( C ), unloaded niosomes ( D ) and acyclovir-loaded niosomes ( E ).Figure 10DSC thermograms of acyclovir-loaded niosomes ( A ), vancomycin-loaded niosomes ( B ) and acyclovir- and vancomycin-loaded mixed niosomes ( C ).
…”
Drug incompatibilities are considered as one of the most critical problems in intensive care units. In the current study, the ability of nanomaterials to prevent drug incompatibilities in clinical settings has been investigated. As a proof-of-concept, the ability of niosomes to prevent physical and chemical incompatibilities that occur upon mixing acyclovir and vancomycin during management of acute meningitis has been explored. Nanosized spherical particles loaded separately with either vancomycin or acyclovir, with high entrapment efficiency (ca. 46–56%), could be prepared, and sustained release of their entrapped cargoes have been demonstrated over time. We have shown that precipitation, degradation and loss of biological activity of drugs occurred upon mixing solutions of the free drugs. On the contrary, drugs loaded separately inside niosomal structures exhibited high stability, exceptional physical and chemical compatibilities for up to 48 h with complete preservation of the antimicrobial activity of vancomycin. This study opens a venue for a new spectrum of applications of nanomaterials in preventing clinically significant drug incompatibilities, aiming at the reduction of adverse reactions, cost and hospitalization period, and improvement of patient compliance and therapeutic outcomes.
“…Cellulose dialysis membrane of molecular weight cutoff 12,000–14,000 Da (Spectrum Laboratories Inc., Rancho Dominguez, CA) was soaked in double-distilled water overnight before use for the experiment. An accurate amount of elastosomes vesicular dispersion, equivalent to 2.5 mg drug, was placed in the presoaked dialysis bag which was then clamped and placed in a beaker containing 50 mL of phosphate-buffered saline (PBS) pH 7.4, as a receptor compartment to simulate body physiological conditions (Auda et al., 2016 ; El-Say et al., 2016 ). The temperature was maintained at 32 °C with continuous stirring at 100 rpm using a magnetic stirrer (MSH-20 D Hotplate Stirrer Unit).…”
Diacerein (DCN) is a hydrophobic osteoarthritis (OA) drug with short half-life and low oral bioavailability. Furthermore, DCN oral administration is associated with diarrhea which represents obstacle against its oral use. Hence, this article aimed at developing elastosomes (edge activator (EA)-based vesicular nanocarriers) as a novel transdermal system for delivering DCN efficiently and avoiding its oral problems. For achieving this goal, elastosomes were prepared according to 41.21 full factorial design using different EAs in varying amounts. The prepared formulae were characterized regarding their entrapment efficiency percentage (EE%), particle size (PS), polydispersity index (PDI), zeta potential (ZP) and deformability index (DI). Desirability function was employed using Design-Expert® software to select the optimal elastosomes (E1) which showed EE% of 96.25 ± 2.19%, PS of 506.35 ± 44.61 nm, PDI of 0.46 ± 0.09, ZP of −38.65 ± 0.91 mV, and DI of 12.74 ± 2.63 g. In addition, E1 was compared to DCN-loaded bilosomes and both vesicles exhibited superior skin permeation potential and retention capacity compared to drug suspension. In-vivo histopathological study was performed which ensured the safety of E1 for topical application. Furthermore, the pharmacokinetic study conducted in albino rabbits demonstrated that there was no significant difference in the rate and extent of DCN absorption from topically applied E1 compared to oral suspension. Multiple level C in-vitro in-vivo correlation showed good correlation between in-vitro release and in-vivo drug performance for E1 and DCN oral suspension. Overall, results confirmed the admirable potential of E1 to be utilized as novel carrier for transdermal delivery of DCN and bypassing its oral side effects.
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